- 1. A gain-of-function mutation of Arabidopsis lipid transfer protein 5 disturbs pollen tube tip growth and fertilization.
During compatible pollination of the angiosperms, pollen tubes grow in the pistil transmitting tract (TT) and are guided to the ovule for fertilization. Lily (Lilium longiflorum) stigma/style Cys-rich adhesin (SCA), a plant lipid transfer protein (LTP), is a small, secreted peptide involved in pollen tube adhesion-mediated guidance. Here, we used a reverse genetic approach to study biological roles of Arabidopsis thaliana LTP5, a SCA-like LTP. The T-DNA insertional gain-of-function mutant plant for LTP5 (ltp5-1) exhibited ballooned pollen tubes, delayed pollen tube growth, and decreased numbers of fertilized eggs. Our reciprocal cross-pollination study revealed that ltp5-1 results in both male and female partial sterility. RT-PCR and beta-glucuronidase analyses showed that LTP5 is present in pollen and the pistil TT in low levels. Pollen-targeted overexpression of either ltp5-1 or wild-type LTP5 resulted in defects in polar tip growth of pollen tubes and thereby decreased seed set, suggesting that mutant ltp5-1 acts as a dominant-active form of wild-type LTP5 in pollen tube growth. The ltp5-1 protein has additional hydrophobic C-terminal sequences, compared with LTP5. In our structural homology/molecular dynamics modeling, Tyr-91 in ltp5-1, replacing Val-91 in LTP5, was predicted to interact with Arg-45 and Tyr-81, which are known to interact with a lipid ligand in maize (Zea mays) LTP. Thus, Arabidopsis LTP5 plays a significant role in reproduction....(more)
Chae K, et al. Plant Cell 2009 Dec;21(12):3902-14.
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- 2. Mussel inspired polydopamine functionalized poly(ether ether ketone) tube for online solid-phase microextraction-high performance liquid chromatography and its application in analysis of protoberberine alkaloids in rat plasma.
A novel and simple poly(ether ether ketone) (PEEK) tube-based solid-phase microextraction (SPME)-HPLC method was developed in this work. A mussel inspired polydopamine method was used to functionalize the chemically resistant surface of PEEK tube and a poly(acrylamide-ethylene glycol dimethacrylate) monolith was synthesized inside the PEEK tube and chemically bonded with its surface. The stability of the polydopamine layer was investigated and found to be well enduring to most of commonly used organic solvents and strong acidic conditions. The PEEK tube-based monolith was coupled with HPLC system through a six-port valve, and the performance of the online SPME-HPLC system was demonstrated by analyzing three protoberberine alkaloids in aqueous samples, namely jatrorrhizine (Jat), palmatine (Pal) and berberine (Ber). These analytes were well extracted and separated within 10 min, and enrichment factors of about 400 were obtained. The limit of detection of the proposed method was decreased to 0.01 ng/mL by using UV detection. Finally, the online SPME-HPLC method was applied for determining Jat, Pal and Ber in rat plasma samples. Reproducibility was obtained by evaluating the intra- and inter-day precisions with RSDs less than 6.1% and 8.5%, respectively, and recoveries of the analytes in spiked plasma samples ranged from 89.8% to 96.7%. The proposed method was also applied to determine the concentration of Jat, Pal and Ber in rat plasma after oral administration of Cortex Phellodendri Chinensis.
Copyright © 2013 Elsevier B.V. All rights reserved....(more)
Zhang W, et al. J Chromatogr A 2013 Feb 22;1278:29-36.
Related Products: Cortex Phellodendri Extract
- 3. Comparison the neuropreotective effect of Cortex Phellodendri chinensis and Cortex Phellodendri amurensis against beta-amyloid-induced neurotoxicity in PC12 cells.
Cortex Phellodendron chinensis (CPC) and Cortex Phellodendron amurensis (CPA) derived from the dried bark of Phellodendron chinense Schneid. or Phellodendron amurense Rupr., respectively, are used interchangeably in clinical practice under the name "Huang Bai" for centuries in Chinese medicine for the treatment of various inflammatory conditions. Previous study in our laboratory demonstrated that CPC and CPA had different anti-diarrheal, anti-bacterial and anti-inflammatory effects. In this present study, we aimed to compare the protective effect of ethanol extract of Cortex Phellodendri chinensis (ECPC) and Cortex Phellodendri Amurensis (ECPA) against beta-amyloid (Aβ)-induced neurotoxicity in PC12 cells, a typical model of Alzheimer's disease. The results showed that ECPC and ECPA contain four common chemical markers such as berberine, but palmatine and jatrorrhizin were not found in CPC in contrast to the presence in CPA. In addition, both ECPC and ECPA can significantly increase the cell viability in Aβ-treated PC12 cells. Moreover, ECPC and ECPA can markedly elevate the ratio of the protein and mRNA levels of Bcl-2/Bax, while remarkably decrease the release of cytochrome c, and the protein and mRNA expression of caspase-3. Interestingly, ECPA has better protective effect than ECPC against Aβ-induced neurotoxicity in PC12 cells. These results indicate that both ECPC and ECPA have potential protective effect against Aβ-induced neurotoxicity in PC12 cells, and ECPA is more potential of the two species to be used in traditional medicine as a neuroprotective agent for the treatment of AD. The neuroprotective effect of the two species may be mediated, at least in part, via suppressing of the cellular apoptosis.
Copyright © 2012 Elsevier GmbH. All rights reserved....(more)
Xian YF, et al. Phytomedicine 2013 Jan 15;20(2):187-93.
Related Products: Cortex Phellodendri Extract
- 4. [Observation of the curative effect of qingchang huashi recipe for treating active ulcerative colitis of inner-accumulation of damp-heat syndrome].
OBJECTIVE:
To observe the clinical effects of Qingchang Huashi Recipe (QHR) for treating active ulcerative colitis (UC) patients of inner-accumulation of damp-heat syndrome (IADHS), and to evaluate its safety.
METHODS:
Using a central random system, 60 patients with mild-to-moderately initial onset or relapsed active UC of IADHS were assigned to the test group (30 cases) and the control group (30 cases). Patients in the test group took QHR (Rhizoma Coptidis 6 g, Radix Scutellariae 10 g, Radix Pulsatillae 10 g, Radix Aucklandiae 10 g, parched Radix Angelicae sinensis 10 g, Radix Paeoniae alba 20 g, Cortex Cinnamomi 3 g, Radix Glycyrrhizae 6 g, and so on), 1 dose each time, decocted twice, mixed to 300 mL, taken in two portions. The components were modified according to the condition of illness. Enema of Guanchang Recipe (GCR) was combined (Cortex Phellodendri 30 g, Radix Sophorae flavescentis 10 g, Radix Sanguisorbae 30 g, Rhizoma bletillae 9 g, Radix notoginseng 3 g, Xilei powder 1.5 g), decocted twice, mixed and concentrated to 120 mL, applied before sleep every evening, with an interval of 12 days after 12 successive days). Those in the control group took Mesalazine Enteric-coated Tablet (MECT, 0.25 g/tablet), 1 g each time, 4 times daily. The therapeutic course for all was 8 weeks. The symptom integral, the colonoscopic results, the pathological efficacy, and the remission rate were compared between the two groups. The medication safety was monitored.
RESULTS:
By the end of the treatment the improvement of symptoms was superior in the test group to that of the control group (P<0.05). The colonoscopic and pathological results were improved in the two groups, but with no statistical difference (P>0.05). There was no statistical difference in the mucosal healing rate (50.0% vs 43.3%) and the remission rate (36.7% vs 30.0%) between the two groups. Only 1 patient of the control group had moderate increase of ALT during the whole test.
CONCLUSIONS:
QHR was effective and safe in treating active UC patients of IADHS. Besides, its effect on improving the symptoms was better than that of MECT....(more)
He HH, et al. Zhongguo Zhong Xi Yi Jie He Za Zhi 2012 Dec;32(12):1598-601. Chinese.
Related Products: Cortex Phellodendri Extract
- 5. Establishment of a search library about benzylisoquinoline alkaloids based on selective separation on the binaphthyl column and standard analysis on C18 column.
A search library about benzylisoquinoline alkaloids was established based on preparation of alkaloid fractions from Rhizoma coptidis, Cortex phellodendri, and Rhizoma corydalis. In this work, two alkaloid fractions from each herbal medicine were first prepared based on selective separation on the "click" binaphthyl column. And then these alkaloid fractions were analyzed on C18 column by liquid chromatography coupled with tandem mass spectrometry. Many structure-related compounds were included in these alkaloids fractions, which led to easy separation and good MS response in further work. Therefore, a search library of 52 benzylisoquinoline alkaloids was established, which included eight aporphine, 19 tetrahydroprotoberberine, two protopine, two benzyltetrahydroisoquinoline, and 21 protoberberine alkaloids. The information of the search library contained compound names, structures, retention times, accurate masses, fragmentation pathways of benzylisoquionline alkaloids, and their sources from three herbal medicines. Using such a library, the alkaloids, especially those trace and unknown components in some herbal medicine could be accurately and quickly identified. In addition, the distribution of benzylisoquinoline alkaloids in the herbal medicines could be also summarized by searching the source samples in the library.
© 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim....(more)
Liu Q, et al. J Sep Sci 2012 Dec;35(23):3317-25.
Related Products: Cortex Phellodendri Extract
- 6. [A theoretical and experimental study on the Fuzzy evaluation model of biological performance of Chinese materia medica with an either cold or hot herbal property].
OBJECTIVE:
The concepts of cold and hot herbal properties in traditional Chinese medicine (TCM), reflecting the efficacy trends of medicinal herbs, have the Fuzzy characteristics. It is suited for the application of Fuzzy mathematics in research of herbal properties. For a comprehensive evaluation of herbal properties, this work constructed and made a practice of the Fuzzy discrimination model regarding the biological performance of Chinese materia medica.
METHODS:
Firstly, TCM formulas of cold or hot property were employed for setting the reference values and calculating the membership functions of cold and hot Fuzzy sets with Fisher discriminant. Then the model parameters of cold performance function (CPF) and hot performance function (HPF) were acquired. Second, the experimental data from studies on changes in multisystem indicators of animals given the classical cold formula (Sanhuang Fang) and hot formula (Jiangfugui Fang) were collected to calculate CPF and HPF. Then an experiment of administration of hot property herbs, Rougui (Cortex Cinnamomi) and Xianmao (Rhizoma Curculiginis), and cold property herbs, Huangbai (Cortex Phellodendri) and Zhizi (Fructus Gardeniae) to normal animals and animals with glucocorticoid-induced yang-deficiency or yin-deficiency state was designed. The relative changes in animal states were analyzed by the evaluation model to find the way in which herbal properties are represented.
RESULTS:
The HPF values of biological performance were higher than the CPF values in administration of Rougui to animals of normal (0.528>0.221), yang-deficiency (0.203>-0.490) and yin-deficiency (1.750>-0.479) states, and in administration of Xianmao to animals of normal (0.474>-1.601) and yang-deficiency (0.288>-1.923) states, which represented the hot property. The HPF values of biological performance were lower than the CPF values in administration of Huangbai to animals of normal (-0.870<0.798) and yang-deficiency (-0.339<0.194) states, and in administration of Zhizi to animals of yin-deficiency (-1.802<0.354) state, which represented the cold property.
CONCLUSION:
The herbal properties and the biological performance characteristics of herbal formulas are ascertained by using the Fuzzy evaluation model. The personalities, as well as commonalities of herbal properties are key areas for focus because of the multi-approach biological performance of cold and hot property....(more)
Jin R, et al. Zhong Xi Yi Jie He Xue Bao 2012 Oct;10(10):1106-19. Chinese.
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- 7. Preparation of a stationary phase with quaternary ammonium embedded group for selective separation of alkaloids based on ion-exclusion interaction.
A stationary phase (named QA C10) with quaternary ammonium embedded between a propyl and a decyl chain was synthesized by immobilization of N,N-dimethyldecylamine on chloropropyl-silica surface. A set of representative neutral, basic, and acidic compounds was employed to evaluate its chromatographic properties. The results illustrated that QA C10 was a mixed-mode stationary phase possessing both hydrophobic and ionic characteristics. The QA C10 stationary phase was further used for selective separation of alkaloids from Cortex phellodendri. Under acidic condition, alkaloids could be eluted in first 8 min, while other neutral and acidic fractions were retained better on QA C10 column. Then, obtained alkaloid fraction was analyzed by LC-MS/MS and 22 alkaloids were identified. Our study confirmed the advantages and application potential of the QA C10 stationary phase for alkaloids separation.
© 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim....(more)
Liu Q, et al. J Sep Sci 2012 Oct;35(20):2685-92.
Related Products: Cortex Phellodendri Extract
- 8. Solid Phase Excitation-Emission Fluorescence Method for the Classification of Complex Substances: Cortex Phellodendri and Other Traditional Chinese Medicines as Examples.
A novel, simple and direct fluorescence method for analysis of complex substances and their potential substitutes has been researched and developed. Measurements involved excitation and emission (EEM) fluorescence spectra of powdered, complex, medicinal herbs, Cortex Phellodendri Chinensis (CPC) and the similar Cortex Phellodendri Amurensis (CPA); these substances were compared and discriminated from each other and the potentially adulterated samples (Caulis mahoniae (CM) and David poplar bark (DPB)). Different chemometrics methods were applied for resolution of the complex spectra, and the excitation spectra were found to be the most informative; only the rank-ordering PROMETHEE method was able to classify the samples with single ingredients (CPA, CPC, CM) or those with binary mixtures (CPA/CPC, CPA/CM, CPC/CM). Interestingly, it was essential to use the geometrical analysis for interactive aid (GAIA) display for a full understanding of the classification results. However, these two methods, like the other chemometrics models, were unable to classify composite spectral matrices consisting of data from samples of single ingredients and binary mixtures; this suggested that the excitation spectra of the different samples were very similar. However, the method is useful for classification of single-ingredient samples and, separately, their binary mixtures; it may also be applied for similar classification work with other complex substances....(more)
Gu Y, et al. J Phys Chem A 2012 Sep 4.
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- 9. The different inhibitory effects of Huang-Lian-Jie-Du-Tang on cyclooxygenase 2 and 5-lipoxygenase.
BACKGROUND:
Huang-Lian-Jie-Du-Tang (HLJDT), a famous traditional Chinese prescription with wide anti-inflammatory applications, is an aqueous extract of four herbal materials: Rhizoma coptidis, Radix scutellariae, Cortex phellodendri, and Fructus gardeniae. Its effects on the cyclooxygenase (COX)-2 and 5-lipoxygenase (5-LOX) pathways are thought to be responsible for its anti-inflammatory activity. However, our previous work found that the inhibitory effects of HLJDT act on the 5-LOX pathway but not on the COX pathway. The possibility that HLJDT inhibits COX-2- or 5-LOX-catalyzed eicosanoid generation by downregulating enzyme expression requires further investigation.
AIM OF THE STUDY:
To observe the effects of HLJDT and its four major components (baicalin, baicalein, berberine and geniposide) on COX-2- or 5-LOX-catalyzed eicosanoid generation and to distinguish the effects of HLJDT on enzyme activity from those on enzyme expression.
METHODS:
The topical anti-inflammatory activities and inhibition of eicosanoid formation of HLJDT and its components were observed in an arachidonic acid (AA)-induced mouse ear edema model. Macrophage-based systems were established to observe the effects of the drugs on enzyme activity and enzyme expression of COX-2 and 5-LOX. Further experiments were carried out to confirm these effects at the mRNA and protein levels.
RESULTS:
Topical treatment of HLJDT significantly inhibited AA-induced mouse ear edema and reduced PGE(2) and LTB(4) release in the edematous ears. Baicalein, geniposide, and berberine also ameliorated the symptoms and suppressed eicosanoid generation with varying efficacies. Cell-based assays showed that HLJDT and baicalein inhibited the PGE(2) levels by decreasing COX-2 enzyme expression without affecting COX-2 enzyme activity in RAW 246.7 murine macrophages. The other experiments on rat peritoneal macrophages indicated that HLJDT and baicalein exerted significant inhibition on LTB(4) production by decreasing 5-LOX enzyme activity. The real-time PCR and western blotting data demonstrated that HLJDT and baicalein reduced COX-2 expression at the mRNA and protein levels, whereas no inhibition on 5-LOX expression was observed.
CONCLUSIONS:
HLJDT can suppress eicosanoid generation via both the COX and LOX pathways, which definitely contributes to its topical anti-inflammatory activity. We have confirmed that its dual inhibition on the COX and LOX pathways mainly result from the downregulation of COX-2 expression and direct inhibition of 5-LOX activity, respectively. Baicalein worked as a potent active component in most of the tests. These findings about the different inhibitory effects of HLJDT on COX-2 and 5-LOX help to better understand the mechanism of HLJDT and promote safer applications of drug.
Copyright © 2012 Elsevier Ireland Ltd. All rights reserved....(more)
Li L, et al. J Ethnopharmacol 2012 Sep 28;143(2):732-9.
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- 10. [Study of cortex phellodendri chinensis decoction experiment based on the spectral imaging technology].
The purpose of decoction traditional Chinese medicine is to make full exhalation of medicinal materials active ingredients, thus it has the maximum effect of traditional Chinese medicine to treat disease. In order to detect the dissolution change of medicinal materials active ingredients in decoction process, this paper applys spectral imaging technology, with Chinese traditional medicine cortex phellodendri as an example, discussing its fluorescence intensity at different time in decoction process. And the analysis results reflect edgewise the dissolution rule of cortex phellodendri active ingredients....(more)
Liang L, et al. Guang Pu Xue Yu Guang Pu Fen Xi 2012 May;32(5):1359-61. Chinese.
Related Products: Cortex Phellodendri Extract
- 11. Formation and conformation of baicalin-berberine and wogonoside-berberine complexes.
It is well-known that baicalin-berberine complex (1) precipitates in the water decoction of numerous Chinese Medicinal formulae containing Radix Scutellariae and Rhizoma Coptidis or Cortex Phellodendri. In the current study, ionic interaction between the carboxylate ion of baicalin and the quaternary ammonium ion of berberine was revealed to be responsible for the formation of 1 and wogonoside-berberine (2) by using FAB-MS and NMR titration experiments. In addition, nuclear Overhauser effect spectroscopy (NOESY) correlations observed in 1 and 2 suggested quite different conformation of the two complexes, which was further supported by the fact that the [α](D) of the canadine obtained by reduction of 1 is of an opposite sign to that obtained from 2. Partition coefficients (n-octanol/water) determination demonstrated 12-20 times larger partition coefficient of each complex (1, 2) than that of each single compound (baicalin, wogonoside, and berberine), indicating the significant role of the formation of the complex in the bioavailability enhancement of these pharmacologically active constituents....(more)
Wang JR, et al. Chem Pharm Bull (Tokyo) 2012;60(6):706-11.
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- 12. An isoquinoline alkaloid from the Chinese herbal plant Corydalis yanhusuo W.T. Wang inhibits P-glycoprotein and multidrug resistance-associate protein 1.
Overexpression of P-glycoprotein (P-gp) and multidrug resistance-associate protein 1 (MRP1) is a major mechanism leading to multidrug resistance (MDR) of cancer cells. These transporters expel anti-cancer drugs and greatly impair therapeutic efficacy of chemotherapy. A Chinese herbal plant Yanhusuo (Corydalis yanhusuo W.T. Wang, YHS) is frequently used in functional food and traditional Chinese medicine to improve the efficacy of chemotherapy. The objective of this work was to study effects of glaucine, an alkaloid component of YHS, on P-gp and MRP1 in resistant cancer cells. The resistant cancer cell line, MCF-7/ADR and corresponding parental sensitive cells were employed to determine reversal properties of glaucine. Glaucine inhibits P-gp and MRP1-mediated efflux and activates ATPase activities of the transporters, indicating that it is a substrate and inhibits P-gp and MRP1 competitively. Furthermore, glaucine suppresses expression of ABC transporter genes. It reverses the resistance of MCF-7/ADR to adriamycin and mitoxantrone effectively.
Copyright © 2012 Elsevier Ltd. All rights reserved....(more)
Lei Y, et al. Food Chem 2013 Feb 15;136(3-4):1117-21.
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- 13. [Study on acting mechanism of anti-morphine conditioned place preference between aqueous extract of Corydalis yanhusuo and L-THP and comparison of their effects].
OBJECTIVE:
To study the acting mechanism of anti-morphine conditioned place preference (CPP) between aqueous extract of Corydalis yanhusuo and L-THP and compare their effects.
METHOD:
The CPP model was established by injecting morphine in rats with a increasing dose for 10 days, with the initial dose of 10 g x kg(-1) and the final dose of 100 g x kg(-1), 10 mg x kg(-1) was increased each day, thus 100 mg x kg(-1) was injected by d 10. Having been treated with differential doses (2, 1 and 0.5 g x kg(-1)) of C. yanhusuo (containing L-THP: 0.153, 0.077 and 0.038 mg x kg(-1) respectively) and L-THP (3.76, 1.88 and 0.94 mg x kg(-1)) for six days, the CPP effect in rats was detected. Both colorimetry and immunohistochemistry methods were adopted to detect the content of glutamate neurotransmitter in each brain region and the expression of NR2B in VTA-NAc-PFC neuroanatomical circuit.
RESULT:
Compared with the physiological saline treatment group, C. yanhusuo (2, 1 g x kg(-1)) and L-THP (3.76 and 1.88 mg x kg(-1)) groups showed a notably shorter retention period of rats in white boxes (morphine-accompanied boxes) (P < 0.05 or P < 0.01) and remarkably lower glutamic acid content in VTA, NAc and PFC and NR2B expression.
CONCLUSION:
Both C. yanhusuo and L-THP can substantially inhibit the effect of morphine CPP, reduce the increasing glutamic acid content in VTA-NAc-PFC neuroanatomical circuit and down-regulated NR2B expression, which may be one of mechanisms on reducing the effect of morphine CPP. C. yanhusuo preparations containing L-THP (1 x ) showed 24-fold effect of L-THP monomer of single application in terms of the behaviouristics of inhibitory effect on CPP as well as the similarity in terms of transmitter glutamic acid of in VTA-NAc-PFC neuroanatomical circuit and pharmacological mechanism of NR2B....(more)
Luo SY, et al. Zhongguo Zhong Yao Za Zhi 2012 Nov;37(22):3457-61. Chinese.
Related Products: Corydalis Yanhusuo Extract
- 14. [Influence of storage conditions on the seed development of Corydalis yanhusuo].
OBJECTIVE:
To explore the influence of the storage conditions on the seed development of Corydalis yanhusuo.
METHODS:
The embryo formation process of the wild Corydalis yanhusuo was observed,and the germination rate of wild Corydalis yanhusuo seeds stored under different conditions was measured.
RESULTS:
The seed development of the wild Corydalis yanhusuo depended on the storage conditions. The seeds subjected to stratification had the highest germination percentage. Those stored in dry conditions would lose the vitality completely. The seeds in isothermal storage had very low germination rates. As revealed by slices, only the seeds after stratification treatment had the ability to form a complete embryo.
CONCLUSION:
The Corydalis yanhusuo seed is a kind of seed without fully developed embryo, and needs further after-ripening for its development. Its vitality has a great seasonal and annual dependence....(more)
Hu K, et al. Zhong Yao Cai 2012 Jul;35(7):1022-5. Chinese.
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- 15. A systems biology approach to understanding the mechanisms of action of chinese herbs for treatment of cardiovascular disease.
Traditional Chinese Medicine (TCM) involves a broad range of empirical testing and refinement and plays an important role in the health maintenance for people all over the world. However, due to the complexity of Chinese herbs, a full understanding of TCM's action mechanisms is still unavailable despite plenty of successful applications of TCM in the treatment of various diseases, including especially cardiovascular diseases (CVD), one of the leading causes of death. Thus in the present work, by incorporating the chemical predictors, target predictors and network construction approaches, an integrated system of TCM has been constructed to systematically uncover the underlying action mechanisms of TCM. From three representative Chinese herbs, i.e., Ligusticum chuanxiong Hort., Dalbergia odorifera T. Chen and Corydalis yanhusuo WT Wang which have been widely used in CVD treatment, by combinational use of drug absorption, distribution, metabolism and excretion (ADME) screening and network pharmacology techniques, we have generated 64 bioactive ingredients and identified 54 protein targets closely associated with CVD, of which 29 are common targets (52.7%) of the three herbs. The result provides new information on the efficiency of the Chinese herbs for the treatment of CVD and also explains one of the basic theories of TCM, i.e., "multiple herbal drugs can treat one disease". The predicted potential targets were then mapped to target-disease and target-signal pathway connections, which revealed the relationships of the active ingredients with their potential targets, diseases and signal systems. This means that for the first time, the action mechanism of these three important Chinese herbs for the treatment of CVD is uncovered, by generating and identifying both their active ingredients and novel targets specifically related to CVD, which clarifies some of the common conceptions in TCM, and thus provides clues to modernize such specific herbal medicines....(more)
Li B, et al. Int J Mol Sci 2012 Oct 19;13(10):13501-20.
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- 16. [Water-soluble non-alkaloid chemical constituents contained in Corydalis yanhusuo by trimethylsilyl derivatization GC-MS].
OBJECTIVE:
To study the water-soluble non-alkaloid chemical constituents of Corydalis yanhusuo.
METHOD:
The 80% alcohol extracts of C. yanhusuo passed through DA201 macroporous resin. Eluted fractions were collected and passed though 732 ...(more)
Liu Z, et al. Zhongguo Zhong Yao Za Zhi 2012 Jul;37(14):2108-12. Chinese.
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- 17. [Chemical constituents from Corydalis yanhusuo].
OBJECTIVE:
To investigate the chemical constituents of Corydalis yanhusuo.
METHOD:
The compounds were isolated and purified by column chromatography over macroporous absorption resin, silica gel, and Sephadex LH-20. Their structures were elucidated on the basis of physicochemical properties and spectral data.
RESULT:
22 compounds were isolated and identified as corydaline (1), tetrahydropalmatine (2), protopine (3), tetrahydrocorysamine (4), tetrahydrocoptisine (5) , tetrahydroberberine (6), tetrahydrocolumbamine (7), noroxyhydrastine (8), dehydrocorydaline (9), glaucine (10), columbamine (11), 8-oxocoptisine (12), 13-methyl-columbamine (13), coptisine (14), palmatine (15), herberine (16), oxoglaucine (17), 13-methyl-palmatrubine (18), dehydrocorybulbine (19), stepharanine (20), adenosine (21), and N5 -acetylornithine (22).
CONCLUSION:
Compounds 13, 20, 21, and 22 were isolated from this plant for the first time....(more)
Lu Z, et al. Zhongguo Zhong Yao Za Zhi 2012 Jan;37(2):235-7. Chinese.
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- 18. l-Tetrahydropalmatine, an active component of Corydalis yanhusuo W.T. Wang, protects against myocardial ischaemia-reperfusion injury in rats.
l-Tetrahydropalmatine (l-THP) is an active ingredients of Corydalis yanhusuo W.T. Wang, which protects against acute global cerebral ischaemia-reperfusion injury. In this study, we show that l-THP is cardioprotective in myocardial ischaemia-reperfusion injury and examined the mechanism. Rats were treated with l-THP (0, 10, 20, 40 mg/kg b.w.) for 20 min before occlusion of the left anterior descending coronary artery and subjected to myocardial ischaemia-reperfusion (30 min/6 h). Compared with vehicle-treated animals, the infarct area/risk area (IA/RA) of l-THP (20, 40 mg/kg b.w.) treated rats was reduced, whilst l-THP (10 mg/kg b.w.) had no significant effect. Cardiac function was improved in l-THP-treated rats whilst plasma creatine kinase activity declined. Following treatment with l-THP (20 mg/kg b.w.), subunit of phosphatidylinositol 3-kinase p85, serine(473) phosphorylation of Akt and serine(1177) phosphorylation of endothelial NO synthase (eNOS) increased in myocardium, whilst expression of inducible NO synthase (iNOS) decreased. However, the expression of HIF-1α and VEGF were increased in I(30 min)R(6 h), but decreased to normal level in I(30 min)R(24 h), while treatment with l-THP (20 mg/kg b.w.) enhanced the levels of these two genes in I(30 min)R(24 h). Production of NO in myocardium and plasma, activity of myeloperoxidase (MPO) in plasma and the expression of tumour necrosis factor-α (TNF-α) in myocardium were decreased by l-THP. TUNEL assay revealed that l-THP (20 mg/kg b.w.) reduced apoptosis in myocardium. Thus, we show that l-THP activates the PI3K/Akt/eNOS/NO pathway and increases expression of HIF-1α and VEGF, whilst depressing iNOS-derived NO production in myocardium. This effect may decrease the accumulation of inflammatory factors, including TNF-α and MPO, and lessen the extent of apoptosis, therefore contributing to the cardioprotective effects of l-THP in myocardial ischaemia-reperfusion injury....(more)
Han Y, et al. PLoS One 2012;7(6):e38627.
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- 19. Two new quaternary protoberberine alkaloids from Corydalis yanhusuo.
Two new quaternary protoberberine alkaloids, namely corydayanine (1) and yanhusuine (2), were isolated from the tubers of Corydalis yanhusuo. On the basis of extensive chemical and spectroscopic evidences, especially 1D and 2D NMR and HRMS experiments, their structures were elucidated as 5,6-dihydro-3,9-dihydroxy-2,10-dimethoxy-13-methyl-dibenzo[a,g] quinolizinium alkaloid and 5,6-dihydro-12-hydroxy-2,3,9-trimethoxy-13-methyl-dibenzo[a,g] quinolizinium alkaloid, respectively....(more)
Zhou Q, et al. J Asian Nat Prod Res 2012;14(5):476-81.
Related Products: Corydalis Yanhusuo Extract
- 20. Dehydrocorydaline inhibits breast cancer cells proliferation by inducing apoptosis in MCF-7 cells.
Dehydrocorydaline is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. We discovered that it possessed anti-tumor potential during screening of anti-tumor natural products from Chinese medicine. In this study, its anti-tumor potential was investigated with breast cancer line cells MCF-7 in vitro. The anti-proliferative effect of dehydrocorydaline was determined by MTT assay and the mitochondrial membrane potential (Δ Ψ m) was monitored by JC-1 staining. DNA fragments were visualized by Hoechst 33342 staining and DNA ladder assay. Apoptotic related protein expressions were measured by Western blotting. Dehydrocorydaline significantly inhibited MCF-7 cell proliferation in a dose- dependent manner, which could be reversed by a caspase-8 inhibitor, Z-IETD-FMK. Dehydrocorydaline increased DNA fragments without affecting ΔΨm. Western blotting assay showed that dehydrocorydaline dose-dependently increased Bax protein expression and decreased Bcl-2 protein expression. Furthermore, dehydrocorydaline induced activation of caspase-7,-8 and the cleavage of PARP without affecting caspase-9. These results showed that dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP....(more)
Xu Z, et al. Am J Chin Med 2012;40(1):177-85. Erratum in: Am J Chin Med. 2012;40(6):1323.
Related Products: Corydalis Yanhusuo Extract
- 21. Application of an in vitro DDASS to evaluate oral absorption of two chemicals simultaneously: establishment of a level A in vitro-in vivo correlation.
The aim of this study was to evaluate the oral absorption of two chemicals simultaneously using a drug dissolution/absorption simulating system (DDASS), and to establish a correlation between DDASS and in vivo absorption to clarify the prediction of this in vitro model. Ferulic acid (FA) and tetrahydropalmatine (THP), the components of Angelicae Sinensis Radix and Corydalis Yanhusuo Rhizoma, respectively, were chosen as model compounds. Three groups including FA, THP, and FA and THP together (FA + THP) were studied in DDASS. The corresponding in vivo pharmacokinetics study was performed in rats. Then the correlation was analysed between DDASS permeation in vitro and rat absorption data in vivo. A strong level A correlation (r > 0.84) was obtained after a correlation coefficient test (p < 0.05 or 0.01). Moreover, when FA and THP were used together in DDASS, the cumulative permeation of FA increased by 38.5%, while THP permeation decreased by 25.8%. In rats, the area under the concentration-time curve from time to infinity for FA increased 2.6-fold, while THP decreased 19.6%. The changes in rat intestinal permeation modeled by the DDASS were consistent with the absorption changes in rats. We conclude that DDASS is a valid in vitro model to evaluate oral absorption of two drug components simultaneously and reflect the in vivo characteristics of drug absorption accurately....(more)
Hou J, et al. Drug Dev Ind Pharm 2012 Nov;38(11):1305-12.
Related Products: Corydalis Yanhusuo Extract
- 22. Effect of fermented bilberry extracts on visual outcomes in eyes with myopia: a prospective, randomized, placebo-controlled study.
Abstract Purpose: To investigate clinically the effects of yeast-fermented bilberry extract on visual outcomes in myopic eyes. Methods: In a prospective, randomized, placebo-controlled, cross-over study, we examined 30 eyes of 30 middle-aged healthy volunteers (mean age±standard deviation, 39.5±7.2 years) with myopia [manifest spherical equivalent, -2.40±1.88 diopters (D)], who were randomly assigned to 1 of 2 oral regimens: fermented bilberry extract (400 mg/day) or placebo. We quantitatively assessed visual acuity, refraction, pupil constriction rate, accommodation, and mesopic contrast sensitivity (CS), before and 1 month after treatment. Only the right eyes were tested. The amplitude of accommodation and CS were measured with an accommodometer (D'ACOMO; WOC) and a CS unit (VCTS-6500; Vistech), respectively. From the CS, the area under the log contrast sensitivity function (AULCSF) was calculated. Results: The mean amplitude of accommodation increased significantly, from 4.62±1.88 D before treatment, to 5.33±2.03 D after treatment in the study group (Wilcoxon signed-rank test, P=0.002). Moreover, the mesopic AULCSF was significantly increased, from 1.04±0.16 before, to 1.13±0.17 after, treatment (P=0.009). However, we found no significant changes in accommodation or AULCSF in the control group (P>0.05), or any significant changes in any other parameters in either group (P>0.05). Conclusions: The present data show that fermented bilberry extract is effective in causing increases in subjective accommodation and in mesopic CS in myopic eyes....(more)
Kamiya K, et al. J Ocul Pharmacol Ther 2013 Apr;29(3):356-9.
Related Products: Cranberry (Bilberry) Extract
- 23. Degradation Index for quality evaluation of commercial dietary supplements of bilberry extract.
In recent years, many anthocyanin-containing dietary supplements of various dosages and formulations have been sold through advertising their large number of beneficial effects. On the other hand, there is an increased risk of distributing deteriorated supplements to consumers due to lax regulations, because in Japan these supplements are classified as food. Spectrophotometric methods are commonly used to control the quality of supplements. However, these methods have limitations with regard to assessing deterioration. In this study, we evaluated a new index for detection of deteriorated products. The stability of 3 formulations and the quality of 20 supplements were investigated by ultra-high performance liquid chromatography, which is superior to spectrophotometry for identifying and quantifying individual anthocyanins. The stability was not only affected by storage temperature but also by formulation. We defined "Degradation Index" (DI) as an indicator of the deterioration of supplements. Of 20 supplements investigated, the DI of 5 supplements was more than 3-fold the value of Bilberon-25, and the worst one was 12.7-fold. These results suggest that DI could be a useful quality control index for detecting deteriorated supplements....(more)
Yamamoto M, et al. J Food Sci 2013 Mar;78(3):S477-83.
Related Products: Cranberry (Bilberry) Extract
- 24. In premenopausal women with recurrent UTI, antibiotics were more effective than capsules of cranberry extract for the prevention of UTI, but resistance was higher in the antibiotic group.
Related Products: Cranberry (Bilberry) Extract
- 25. Inhibition of adhesion of uropathogenic Escherichia coli bacteria to uroepithelial cells by extracts from cranberry.
Cranberry extract has been reported as a therapeutic agent, mainly in urinary tract infections due to its anti-adhesive capacity. In order to compare the effects of proanthocyanidin (procyanidin) (PAC)-standardized cranberry extracts and commercial PAC A2, we first investigated the presence of genes encoding known adhesins on 13 strains of uropathogenic strains coming from patients with cystisis. After this characterization, the anti-adhesive effects of PAC A2 were assayed on selected uropathogenic Escherichia coli strains before testing cranberry extracts. Before checking inhibitory effect on bacterial adhesion to cells, we showed that neither PAC A2 or three cranberry extracts (A, B, and C) specifically inhibited the growth and did not supply any potential nutrient to E. coli strains, including the unrelated control strain. PAC A2 exhibited an inhibitory effect on the adhesion of two selected uropathogenic strains of E. coli. This work also showed that a preliminary exposure of bacteria to PAC A2 significantly reduced the adhesion. This phenomenon has been also observed with a lesser impact when uroepithelial cells were pretreated with PAC A2. Moreover, the assays were more robust when bacteria were in fast growing conditions (exponential phase): the adhesion to uroepithelial cells was greater. Significant reduction of adhesion to urepithelial cells was observed: around 80% of inhibition of adhesion with the cranberry extracts at equivalent PAC concentration of 50 μg/mL. The effects of the different assayed extracts were not obviously different except for extract B, which inhibited approximately 55% of adhesion at an equivalent PAC concentration of 5 μg/mL....(more)
Ermel G, et al. J Med Food 2012 Feb;15(2):126-34.
Related Products: Cranberry (Bilberry) Extract
- 26. Sealing liquid-filled pectinate capsules with a shellac coating.
Liquid-filled pectinate capsules have a large potential for the controlled and site-specific delivery of liquid drugs. Earlier studies have shown that pure pectinate capsules can store drugs only for a few minutes. Here, we show that the retention time can be extended to several hours by coating the capsules with the natural resin shellac. A bilberry extract containing anthocyanins with promising therapeutic properties was used as model drug to characterize the permeability of the capsules by in vitro drug release measurements. Characterizing the structure of the double-layered capsule membranes by NMR microscopy, we optimized the capsule production by adjusting the pH-value in the coating process and the gelation time of the pectinate hydrogel layer. A comparison of the layer thicknesses with drug release measurements reveals that capsules with the thinnest shellac layers provide the best entrapment. Additional squeezing experiments show that the shellac layer makes the capsules also mechanically more stable....(more)
Henning S, et al. J Microencapsul 2012;29(2):147-55.
Related Products: Cranberry (Bilberry) Extract
- 27. Preparation and comparative release characteristics of three anthocyanin encapsulation systems.
Bilberries (Vaccinium myrtillus L.) and their major polyphenolic constituents, anthocyanins, have preventive activities inter alia against colon cancer and inflammatory bowel diseases. However, anthocyanins are sensitive to environmental conditions; thus their bioavailability in the gastrointestinal tract is an important determinant of their in vivo activity. In the study reported here, the potential benefits of encapsulating an anthocyanin rich bilberry extract (BE) on anthocyanin stability were investigated. Nonencapsulated BE and three different BE loaded microcapsule systems were incubated in simulated gastric fluid (SGF) and fed state simulated intestinal fluid (FeSSIF). After exposure to these media, released anthocyanins were identified and quantified by HPLC with UV/Vis detection. Although a rapid release of anthocyanins was observed within the first 20 min, encapsulation of anthocyanins doubled the amount of available anthocyanins after 150 min of incubation. These results illustrate the ability of encapsulation to inhibit early degradation of anthocyanins in the intestinal system....(more)
Oidtmann J, et al. J Agric Food Chem 2012 Jan 25;60(3):844-51.
Related Products: Cranberry (Bilberry) Extract
- 28. Study on the influence of cranberry extract ?uravit S·O·S(®) on the properties of uropathogenic Escherichia coli strains, their ability to form biofilm and its antioxidant properties.
Consumption of cranberries is known to exert positive health effects, especially against urinary tract infections. For this reason, presumably, they are widely used in folk medicine. Different aspects of cranberry phenolics activity were studied in individual papers but complex study in this matter is missing. The aim of the present study is to provide complex data concerning various aspects of cranberry extract activity. We studied the effects of subinhibitory concentrations of commercially available extract (uravit S·O·S(®)) against two Escherichia coli strains isolated from urine of patients with pyelonephritis. Additionally the main extract anthocyanins were characterized. The activity of extract against lipid peroxidation and its radical scavenging ability were also assessed. uravit S·O·S(®) decreased the hydrophobicity of one of the studied E. coli strains, reduced swimming motility and adhesion to epithelial cells of both studied strains, it also limited the ability of bacteria to form biofilm. Expression of curli was not affected by cranberry extract, the assessment of P fimbriae expression was not reliable due to extract-induced agglutination of erythrocytes. Cranberry extract caused filamentation in both studied E. coli strains. It also showed pronounced antioxidant and radical scavenging properties. The properties of the studied cranberry extract show that it could be effectively used in prevention and/or elimination of urinary tract infections, specially the recurrent ones....(more)
Wojnicz D, et al. Phytomedicine 2012 Apr 15;19(6):506-14.
Related Products: Cranberry (Bilberry) Extract
- 29. American cranberry (Vaccinium macrocarpon) extract affects human prostate cancer cell growth via cell cycle arrest by modulating expression of cell cycle regulators.
Prostate cancer is one of the most common cancers in the world, and its prevalence is expected to increase appreciably in the coming decades. As such, more research is necessary to understand the etiology, progression and possible preventative measures to delay or to stop the development of this disease. Recently, there has been interest in examining the effects of whole extracts from commonly harvested crops on the behaviour and progression of cancer. Here, we describe the effects of whole cranberry extract (WCE) on the behaviour of DU145 human prostate cancer cells in vitro. Following treatment of DU145 human prostate cancer cells with 10, 25 and 50 μg ml¹ of WCE, respectively for 6 h, WCE significantly decreased the cellular viability of DU145 cells. WCE also decreased the proportion of cells in the G2-M phase of the cell cycle and increased the proportion of cells in the G1 phase of the cell cycle following treatment of cells with 25 and 50 μg ml¹ treatment of WCE for 6 h. These alterations in cell cycle were associated with changes in cell cycle regulatory proteins and other cell cycle associated proteins. WCE decreased the expression of CDK4, cyclin A, cyclin B1, cyclin D1 and cyclin E, and increased the expression of p27. Changes in p16(INK4a) and pRBp107 protein expression levels also were evident, however, the changes noted in p16(INK4a) and pRBp107 protein expression levels were not statistically significant. These findings demonstrate that phytochemical extracts from the American cranberry (Vaccinium macrocarpon) can affect the behaviour of human prostate cancer cells in vitro and further support the potential health benefits associated with cranberries....(more)
Déziel B, et al. Food Funct 2012 May;3(5):556-64.
Related Products: Cranberry (Bilberry) Extract
- 30. Vaccinium myrtillus ameliorates unpredictable chronic mild stress induced depression: possible involvement of nitric oxide pathway.
Chronic unpredictable stressors can produce a situation similar to clinical depression and such animal models can be used for the preclinical evaluation of antidepressants. Nitric oxide, a secondary messenger molecule, has been implicated in neurotransmission, synaptic plasticity, learning, aggression and depression. Vaccinium myrtillus (bilberry) extract is a potent inhibitor of reactive oxygen/nitrogen species and cytokine production. The present study investigated the role of nitric oxide in the antidepressant action of Vaccinium myrtillus in unpredictable chronic mild stress-induced depression in mice. Animals were subjected to different stress paradigms daily for a period of 21 days to induce depressive-like behavior. Pretreatment with L-arginine significantly reversed the protective effect of bilberry (500 mg/kg) on chronic stress-induced behavioral (immobility period, sucrose preference) and biochemical (lipid peroxidation and nitrite levels; endogenous antioxidant activities) in stressed mice. Furthermore, L-NAME (10 mg/kg) pretreatment with a sub-effective dose of bilberry (250 mg/kg) significantly potentiated the protective effect of bilberry extract. The study revealed that modulation of the nitric oxide pathway might be involved in antidepressant-like effects of Vaccinium myrtillus in stressed mice....(more)
Kumar B, et al. Phytother Res 2012 Apr;26(4):488-97.
Related Products: Cranberry (Bilberry) Extract
- 31. Capability of Lactobacillus plantarum IFPL935 to catabolize flavan-3-ol compounds and complex phenolic extracts.
Lactobacillus plantarum IFPL935 was incubated with individual monomeric flavan-3-ols and dimeric A- and B-type procyanidins to identify new metabolites and to determine the effect of compound structural features on bacterial growth and catabolism. Complex extracts rich in A-type proanthocyanidins and phenolic acids from cranberry were also tested. The results showed that L. plantarum IFPL935 exhibited higher resistance to nongalloylated monomeric flavan-3-ols, A-type dimeric procyanidins, and cranberry extract than to (-)-epicatechin-3-O-gallate and B-type dimeric procyanidins. Despite these findings, the strain was capable of rapidly degrading (-)-epicatechin-3-O-gallate, but not A- or B-type dimeric procyanidins. However, it was able to produce large changes in the phenolic profile of the cranberry extract mainly due to the catabolism of hydroxycinnamic and hydroxybenzoic acids. Of most relevance was the fact that L. plantarum IFPL935 cleaved the heterocyclic ring of monomeric flavan-3-ols, giving rise to 1-(3',4'-dihydroxyphenyl)-3-(2″,4″,6″-trihydroxyphenyl)propan-2-ol, activity exhibited by only a few human intestinal bacteria....(more)
Sánchez-Patán F, et al. J Agric Food Chem 2012 Jul 25;60(29):7142-51.
Related Products: Cranberry (Bilberry) Extract
- 32. Tanshinone derivatives: a patent review (January 2006 - September 2012).
INTRODUCTION:
Tanshinone IIA (TSIIA), cryptotanshinone and tanshinone I are major bioactive constituents of Danshen, a Chinese herbal medicine. Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of TSIIA and it is currently used for treating cardiovascular diseases in China.
AREAS COVERED:
The article presents a review of the anti-atherosclerosis, cardioprotective effects, neuroprotection and anti-tumor activities of TSIIA and a review of patents on tanshinone derivatives from January 2006 to September 2012.
EXPERT OPINION:
Mechanistic studies have discovered that TSIIA modulates ion channels, kinases, hormone receptors, apoptosis proteins, growth factors, cytokines, microRNA, tumor suppressor and many other targets, revealing an intricate biological network modulated by TSIIA. Many patents have attempted to overcome the low water solubility of TSIIA and tanshinone I by attaching a polar substituent or by a prodrug strategy. However, biological activities of these tanshinone derivatives need to be further evaluated. Given the extensive in vitro and in vivo biological activities of TSIIA, this compound is a promising candidate to be further developed as a novel therapeutics for treating atherosclerosis, cardiovascular diseases, neurodegenerative diseases and cancer....(more)
Tian XH, et al. Expert Opin Ther Pat 2013 Jan;23(1):19-29.
Related Products: Cryptotanshinone
- 33. Enzyme kinetic and molecular docking studies for the inhibitions of miltirone on major human cytochrome P450 isozymes.
Previous studies have shown that major tanshinones isolated from Danshen (Salvia miltiorrhiza) inhibited human and rat CYP450 enzymes-mediated metabolism of model probe substrates, with potential in causing herb-drug interactions. Miltirone, another abietane type-diterpene quinone isolated from Danshen, has been reported for its anti-oxidative, anxiolytic and anti-cancer effects. The aim of this study was to study the effect of miltirone on the metabolism of model probe substrates of CYP1A2, 2C9, 2D6 and 3A4 in pooled human liver microsomes. Miltirone showed moderate inhibition on CYP1A2 (IC(50)=1.73 μM) and CYP2C9 (IC(50)=8.61 μM), and weak inhibition on CYP2D6 (IC(50)=30.20 μM) and CYP3A4 (IC(50)=33.88 μM). Enzyme kinetic studies showed that miltirone competitively inhibited CYP2C9 (K(i)=1.48 μM), and displayed mixed type inhibitions on CYP1A2, CYP2D6 and CYP3A4 with K(i) values of 3.17 μM, 24.25 μM and 35.09 μM, respectively. Molecular docking study further confirmed the ligand-binding conformations of miltirone in the active sites of these human CYP450 isoforms, and provided some information on structure-activity relationships for the CYPs inhibition by tanshinones. Taken together, CYPs inhibitions of miltirone were weaker than dihydrotanshinone, but stronger than cryptotanshinone, tanshinone I and tanshinone IIA....(more)
Zhou X, et al. Phytomedicine 2013 Feb 15;20(3-4):367-74.
Related Products: Cryptotanshinone
- 34. Cryptotanshinone and dihydrotanshinone I exhibit strong inhibition towards human liver microsome (HLM)-catalyzed propofol glucuronidation.
Danshen is one of the most famous herbs in the world, and more and more danshen-prescribed drugs interactions have been reported in recent years. Evaluation of inhibition potential of danshen's major ingredients towards UDP-glucuronosyltransferases (UGTs) will be helpful for understanding detailed mechanisms for danshen-drugs interaction. Therefore, the aim of the present study is to investigate the inhibitory situation of cryptotanshinone and dihydrotanshinone I towards UGT enzyme-catalyzed propofol glucuronidation. In vitro the human liver microsome (HLM) incubation system was used, and the results showed that cryptotanshinone and dihydrotanshinone I exhibited dose-dependent inhibition towards HLM-catalyzed propofol glucuronidation. Dixon plot and Lineweaver-Burk plot showed that the inhibition type was best fit to competitive inhibition type for both cryptotanshinone and dihydrotanshinone I. The second plot using the slopes from the Lineweaver-Burk plot versus the concentrations of cryptotanshinone or dihydrotanshinone I was employed to calculate the inhibition parameters (Ki) to be 0.4 and 1.7μM, respectively. Using the reported maximum plasma concentration (Cmax), the altered in vivo exposure of propofol increased by 10% and 8.2% for the co-administration of dihydrotanshinone I and cryptotanshinone, respectively. All these results indicated the possible danshen-propofol interaction due to the inhibition of dihydrotanshinone I and cryptotanshinone towards the glucuronidation reaction of propofol....(more)
Cong M, et al. Fitoterapia 2013 Mar;85:109-13.
Related Products: Cryptotanshinone
- 35. TanshinoneIIA and cryptotanshinone protect against hypoxia-induced mitochondrial apoptosis in H9c2 cells.
Mitochondrial apoptosis pathway is an important target of cardioprotective signalling. Tanshinones, a group of major bioactive compounds isolated from Salvia miltiorrhiza, have been reported with actions against inflammation, oxidative stress, and myocardial ischemia reperfusion injury. However, the actions of these compounds on the chronic hypoxia-related mitochondrial apoptosis pathway have not been investigated. In this study, we examined the effects and molecular mechanisms of two major tanshonones, tanshinone IIA (TIIA) and cryptotanshinone (CT) on hypoxia induced apoptosis in H9c2 cells. Cultured H9c2 cells were treated with TIIA and CT (0.3 and 3 μΜ) 2 hr before and during an 8 hr hypoxic period. Chronic hypoxia caused a significant increase in hypoxia inducible factor 1α expression and the cell late apoptosis rate, which was accompanied with an increase in caspase 3 activity, cytochrome c release, mitochondria membrane potential and expression of pro-apoptosis proteins (Bax and Bak). TIIA and CT (0.3 and 3 μΜ), in concentrations without affecting the cell viability, significantly inhibited the late apoptosis and the changes of caspase 3 activity, cytochrome c release, and mitochondria membrane potential induced by chronic hypoxia. These compounds also suppressed the overexpression of Bax and reduced the ratio of Bax/Bcl-2. The results indicate that TIIA and CT protect against chronic hypoxia induced cell apoptosis by regulating the mitochondrial apoptosis signaling pathway, involving inhibitions of mitochondria hyperpolarization, cytochrome c release and caspase 3 activity, and balancing anti- and pro-apoptotic proteins in Bcl-2 family proteins....(more)
Jin HJ, et al. PLoS One 2013;8(1):e51720.
Related Products: Cryptotanshinone