Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research

Guangzhou, China

Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research

Guangzhou, China
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He L.-L.,Jinan University | Yao Z.-H.,Jinan University | Yao Z.-H.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | Wu X.-M.,Jinan University | And 6 more authors.
Chinese Pharmaceutical Journal | Year: 2016

OBJECTIVE: To establish the ultra performance liquid chromatography (UPLC) fingerprint of Xianling Gubao Capsules (XLGB), and evaluate the product quality by chemometrics analysis method. METHODS: The method was developed on an ACQUITY UPLC BEH Shield RP18 column (2.1 mm×50 mm, 1.7μm) by gradient elution with acetonitrile-water [both containing 0.1% formic acid] as mobile phase at a flow rate of 0.5 mL· min-1. The column temperature was maintained at 30℃, and the detection wavelength was set at 246 nm during 0-4.6 min and 270 nm during 4.6-18 min. The main characteristic peaks were identified and assigned to individual herbs by comparing the retention time and UV absorption characteristics, combined with peak purity analysis. Furthermore, 16 batches of XLGB were evaluated by similarity assay, PCA, and PLS-DA. RESULTS: The UPLC fingerprint of XLGB was established and 27 main characteristic peaks were identified. The similarity of 16 batches of XLGB was about 0.959 to 0.988, and epimedin C, bakuchiol, psoralenoside, and isopsoralenoside from Epimedium breviornu Maxim and Psoralea corylifolia L were the main compounds causing the similarity difference. CONCLUSION: The method can be used for the quality control of XLGB with good specificity and efficiency, and this work provides the experimental basis to improve the overall quality control of XLGB. Copyright 2016 by the Chinese Pharmaceutical Association.


Yao Z.-H.,Jinan University | Yao Z.-H.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | Pan Y.-M.,Jinan University | Pan Y.-M.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | And 11 more authors.
Chinese Pharmaceutical Journal | Year: 2010

OBJECTIVE: To develop a HPLC fingerprint chromatogram of a traditional Chinese medicine (TCM) prescription named Xiaoyanlidan Tablet (XYLD) for the evaluation of the quality of its products. METHODS: The method was developed on a C 18 column (4. 6 mm x250 mm, 5 μm) by gradient elution with acetonitrile-water (both containing 0.1% (V/V) formic acid) as mobile phase at a flow rate of 1.00 mL·min -1 with the detection wavelength at 254 nm and column temperature at 25°C. The HPLC fingerprint chromatogram of XYLD was set up and the origin of main peaks were clarified by comparing with overlapping chromatograms of three compositive crude herbs. Furthermore, some of the main peaks were identified by comparing the retention time with those of chemical reference substance. The similarity assay of 24 batches of XYLD from 3 different manufactures was carried out to evaluate their quality by TCM fingerprint similarity evaluation system. RESULTS: The HPLC fingerprint chromatogram of XYLD was established with good stability, precision and reproducibility. Among forty detected peaks in the HPLC fingerprint chromatogram of XYLD, the source of thirty-one peaks was revealed and seven of them were identified. The similarity of XYLD tablet was above 0.954 within the products by the same manufacture. However, the similarity was about 0.845 to 0.987. The similarity droped to 0.478 to 0.896 within the cut chromatogram (eluates before dehydroandrographolide, 0 to 69 min). CONCLUSION: The HPLC fingerprint chromatogram represented the profile of multiple chemical substances in XYLD tablet, which would contribute to its quality control.


Su M.,Chinese University of Hong Kong | Chung H.Y.,Chinese University of Hong Kong | Li Y.,Jinan University | Li Y.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research
Chemico-Biological Interactions | Year: 2011

High incidence of lymph node spread and distant metastasis make poor prognosis in human nasopharyngeal carcinoma (NPC). Therefore, better treatments for NPC are needed. This study investigated the anticancer activity of 6-O-angeloylenolin, a plant-derived sesquiterpene lactone, on human nasopharyngeal cancer (CNE) cells. 6-O-Angeloylenolin was found to significantly inhibit the proliferation of CNE cells. The rate of inhibition was comparable to that of cisplatin, a well known chemotherapeutic agent used to treat NPC. Further mechanistic studies revealed that 6-O-angeloylenolin caused cell-cycle arrest in the S and G2/M phases and, subsequently, the induction of apoptosis. Rapid repressions of cyclin D1, cyclin D3, p27, cdc25c and p-cdc25c (Ser216) were observed after 1-h treatment, followed by decreases in the expression of CDK4, cdc2 and p-cdc2 (Tyr15) after 12 h. Down-regulations of p-Rb (Ser780), p21Waf1/Cip1, cyclin A, and cyclin E were also detected as later events. Two early events that marked the occurrence of apoptosis were phosphatidylserine exposure and mitochondria membrane potential depletion, which occurred after 12 h of treatment, while a sub-G1 peak was also detected after 36-h treatment. Apoptosis induction was further confirmed by other apoptotic features, including nuclear fragmentation, and PARP cleavage. Moreover, 6-O-angeloylenolin caused the release of cytochrome c and AIF to the cytosol by regulating the expression of the Bcl-2 family proteins. However, pretreatment of the general caspase inhibitor failed to attenuate the apoptosis induction effect, suggesting that apoptosis induction of 6-O-angeloylenolin was independent of caspase activation. While 6-O-angeloylenolin also triggered the activation of Akt, ERK and JNK, only the JNK inhibitor significantly decreased the extent of cell death and apoptosis in CNE cells. Taken together, these results suggest the potential applicability of 6-O-angeloylenolin as a candidate for NPC treatment. © 2010 Elsevier Ireland Ltd. All rights reserved.


Hu Y.-M.,Jinan University | Hu Y.-M.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | Wang G.-C.,Jinan University | Wang G.-C.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | And 6 more authors.
Helvetica Chimica Acta | Year: 2012

Four C(8),C(12)-diastereoisomers, (8S,12S)-isoandrographolide (1), (8S,12R)-isoandrographolide (2), (8R,12R)-isoandrographolide (3), and (8R,12S)-isoandrographolide (4) were isolated from the aerial parts of Andrographis paniculata. The structures of the new compounds 1-3 were established on the basis of the spectroscopic data including UV, IR, NMR, HR-ESI-MS, and X-ray diffraction analysis. Copyright © 2012 Verlag Helvetica Chimica Acta AG, Zürich, Switzerland.


Wang G.-C.,Jinan University | Wang G.-C.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | Li J.-G.,Jinan University | Li J.-G.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | And 10 more authors.
Journal of Natural Products | Year: 2012

Seven new clerodane diterpenoids (1-7) were isolated from roots of Croton crassifolius, along with six known compounds. The structures were elucidated by extensive spectroscopic methods (IR, UV, HRESIMS, 1D NMR, and 2D NMR), and the structures of 1, 3, 4, and 7 were confirmed by single-crystal X-ray diffraction analyses. Compounds 1-13 were evaluated for in vitro antiviral activity against herpes simplex virus type 1 using the cytopathic effect reduction assay. © 2012 The American Chemical Society and American Society of Pharmacognosy.


Lu X.,Jinan University | Wan S.,Jinan University | Jiang J.,Jinan University | Jiang J.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | And 14 more authors.
European Journal of Medicinal Chemistry | Year: 2011

We have designed and synthesized a series of novel apocynin analogues, and evaluated their biological activity. Compound 10, an apocynin dimer analogue, compound 12, the lipoic acid (LA) and apocynin conjugate, were the most potent in protecting cells from lipopolysaccharide (LPS)-induced cytotoxicity, had significant activity scavenging ROS induced by LPS, and greatly decreased LPS-induced P67phox protein expression. SAR analysis suggests that modification of apocynin can increase its activity. Our results demonstrate that arming apocynin with a powerful antioxidant such as lipoic acid is a valid strategy to design new apocynin analogues with enhanced biological activity. © 2011 Elsevier Masson SAS. All rights reserved.


Su M.,Chinese University of Hong Kong | Wu P.,Jinan University | Li Y.,Jinan University | Li Y.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | Chung H.Y.,Chinese University of Hong Kong
Natural Product Communications | Year: 2010

Volatile oils from Centipeda minima extracted by steam distillation (SD) and supercritical fluid extraction (SFE) were investigated for their antiproliferative effects on the human nasopharyngeal cancer CNE cells. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay results showed that CNE cells were more susceptible to the SFE oil than to the SD oil. The IC 50 values of the SFE oil were 56.6, 8.7 and 5.2 μg/mL after 24-, 48- and 72-h of treatment, respectively, whereas those of the SD oil were 123.5 μg/mL (24 h), 97.1 μg/mL (48 h) and 83.3 μg/mL (72 h). Mechanistic investigation revealed that SFE oil induced CNE cell death via induction of apoptosis by regulating the expression of the Bcl-2 family of proteins, resulting in the dysfunction of mitochondria, leading to the release of cytochrome c into the cytosol, which then activated caspase-9, and subsequently cleaved caspases-3 and -7. This study provided strong evidence for the anti-NPC potential of the SFE oil from C. minima.


Wei Z.-C.,Jinan University | Yao Z.-H.,Jinan University | Yao Z.-H.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | Wang Q.-Y.,Jinan University | And 6 more authors.
Chinese Traditional and Herbal Drugs | Year: 2015

To establish the UPLC fingerprint for effective quality control of Sarcandrae Herba. The fingerprint of Sarcandrae Herba was developed with ultra-performance liquid chromatography, and the Acquity UPLC HSS T3 column (50 mm × 2.1 mm, 1.8 μm) was used in the gradient elution with a mobile phase of acetonitrile-water (both containing 0.1% formic acid): The flow rate was 0.5 mL/min, the column temperature was 35℃, and the detection wavelength was at 330 nm. Similarity evaluation combined with hierarchical clustering analysis (HCA) and principal components analysis (PCA) were used to evaluate the quality of herbs from different areas. The fingerprint of Sarcandrae Herba was established with good precision, reproducibility, and stability obtaining within 23 min, and nine peaks in the fingerprint were designed. Eighteen samples could be classified into two clusters. The PCA result was consistent with the HCA. A brief list of five differential compounds is presented, including rosmarinic acid, newchlorogenic acid, and so on. The establishment of UPLC fingerprint of Sarcandrae Herba and the application of chemical pattern recognition can provide a more comprehensive reference for the quality control of herbs. ©, 2015, Chinese Traditional and Herbal Drugs. All right reserved.


Zhang X.,Jinan University | Zhang X.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | Wang G.,Jinan University | Wang G.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | And 5 more authors.
Natural Product Communications | Year: 2011

Two new biflavonoids, 4′-methoxydaphnodorin D 1 and 4′-methoxydaphnodorin D 2, along with six known biflavonoids, were isolated from the roots of Wikstroemia indica. The structures of the new compounds were determined by extensive NMR and HRESIMS spectroscopic analyses in combination with CD measurements.


Huang W.-H.,Jinan University | Huang W.-H.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | Li G.-Q.,Jinan University | Li G.-Q.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drug Research | And 12 more authors.
Heterocycles | Year: 2014

The root of Croton crassifolius was evaluated for its anti-angiogenic properties and anti-angiogenic components. The ethanol extract of the herb and its successive four subfractions were investigated in zebrafish model by quantitative endogenous alkaline phosphatase assay. Both petroleum ether (PE) and ethyl acetate fractions (EtOAc) showed potent anti-angiogenic activities. Two new clerodane diterpenoids, crassifolin I (1) and crassifolin H (2) were isolated from EtOAc fraction. Their structures were elucidated by extensive spectroscopic methods (IR, UV, HRESIMS, 1D and 2D NMR), and compound 1 was confirmed by single-crystal X-ray diffraction analysis. The further activities study showed that crassifolin H possessed anti-angiogenic activity by reducing vessel formation to 59.3% of the control value at concentrate © 2014 The Japan Institute of Heterocyclic Chemistry.

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