State Key Laboratory of Chinese Medicine and Molecular Pharmacology Incubation

Shenzhen, China

State Key Laboratory of Chinese Medicine and Molecular Pharmacology Incubation

Shenzhen, China
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Gu G.-H.,Peking University | Yang D.-J.,State Key Laboratory of Chinese Medicine and Molecular Pharmacology Incubation | Wang S.-Y.,State Key Laboratory of Chinese Medicine and Molecular Pharmacology Incubation | Zeng W.,Peking University | And 2 more authors.
Acta Chromatographica | Year: 2017

A high-performance liquid chromatography-diode-array detection method was developed and validated to determine simultaneously eleven major alkaloids in Corydalis decumbens (Thunb.) Pers. The alkaloids detected were corlumidine, protopine, coptisine, tetrahydrojatrorrhizine, palmatine, berberine, sanguinarine, papaverine hydrochloride, tetrahydropalmatine, bicuculline, and corydaline. Chromatographic separation was achieved using a C-18 column with a mobile phase composed of A (0.2% acetic acid solution, adjusted with triethylamine to pH 5.0) and B (acetonitrile), with stepwise gradient elution. Ultraviolet diode-array detection was used; chromatograms were examined at the wavelength of 280 nm. The regression equations showed a good linear relationship between the peak area of each marker and concentration (r = 0.9994-0.9999). The recovery values ranged between 93.66% and 100.54%. The method was fully validated with respect to detection and quantification limits, precision, reproducibility, and accuracy. The described high-performance liquid chromatography (HPLC) method was successfully used for the differentiation and quantification of the eleven major alkaloids in C. decumbens (Thunb.) Pers. and can be considered an effective procedure for the analyses of this important class of natural compounds. © 2016 The Author(s).


Chen W.-F.,Hong Kong Polytechnic University | Chen W.-F.,Qingdao University | Gao Q.-G.,Hong Kong Polytechnic University | Dai Z.-J.,University of Hong Kong | And 4 more authors.
Menopause | Year: 2012

Objective: The present study was designed to determine whether ginsenoside Rg1 could exert selective estrogenic effects by using both cell lines and an animal model. Methods: The endometrial Ishikawa cells and preosteoblastic MC3T3-E1 cells were treated with a different dose of Rg1. Immature CD-1 mice and ovariectomized (OVX) C57BL/6J mice were used to study the short-term and long-term estrogenic effects of Rg1, respectively. Results: Rg1 significantly increased estrogen receptor-dependent alkaline phosphatase activity, activated estrogen response element-luciferase activity, and induced the phosphorylation of mitogen-activated protein kinase kinase, extracellular-regulated kinase, and estrogen receptor-α in Ishikawa cells. In contrast, Rg1 did not induce any estrogenic responses in MC3T3-E1 cells. Administration of Rg1 to immature CD-1 mice did not alter their uterine weight or the estrogen-regulated gene expressions in the uterus. Treatment of OVX C57BL/6J mice with Rg1 via mini-osmotic pumps for 3 months did not alter the uterine weight or induce any transcriptional activation of estrogen receptor in the uterus. Rg1 induced Bcl-2 messenger RNA expression in the left ventricular tissue and striatum but failed to alter the bone mineral density in the femur and tibia of the OVX mice. Conclusions: Rg1 exerted potent estrogenic effects in endometrial cells in vitro as well as in heart and brain tissues in vivo. However, it did not exert any estrogenic effects on reproductive tissues in vivo, nor did it stimulate bone tissues in vitro or in vivo. Our results suggest that the estrogenic effects of Rg1 are distinct from those of estradiol and are cell type and tissue selective. © 2012 The North American Menopause Society.


Wong K.-C.,Hong Kong Polytechnic University | Pang W.-Y.,Hong Kong Polytechnic University | Wang X.-L.,CAS Shenzhen Institutes of Advanced Technology | Wang X.-L.,Shenyang Pharmaceutical University | And 8 more authors.
British Journal of Nutrition | Year: 2013

Drynaria fortunei (Kunze) J. Sm. (DF), a Chinese herb commonly used for the treatment of bone fracture, was previously shown to exert anabolic effects on bone. However, its active ingredients as well as the mechanisms of action are far from clear. The present study aimed to characterise the bone anabolic effects of DF flavonoid fraction (DFTF) in ovariectomised (OVX) mice and to determine if DFTF and its isolated compounds exert oestrogen-like effects in rat osteoblast-like UMR-106 cells. Young OVX C57/BL6J mice were treated orally with DFTF (0·087, 0·173 or 0·346 mg/g per d), 17β-oestradiol (2 μg/g per d) or its vehicle for 6 weeks. Serum and urine samples were collected for biochemical marker analysis. Bones were collected for computed tomography analysis. UMR-106 cells were treated with DFTF and isolated compounds naringin, (2S)-5,7,3′,5′-tetrahydroxy- flavonone 7-O-neohesperidoside (compound 1) and 5,7-dihydroxychromone 7-O-neohesperidoside (compound 2). DFTF exerted dose-dependent effects in improving bone mineral densities as well as bone strength at the femur, tibia and lumbar spine L1 in OVX mice. DFTF and the three isolated compounds stimulated osteoblastic cell proliferation and alkaline phosphatase activities in a dose-dependent manner. In addition, they stimulated the ratio of osteoprotegrin and receptor-activator NF-κB ligand mRNA expression, suggesting their involvement in inhibiting osteoclastogenesis. These stimulatory effects on osteoblastic functions were abolished in the presence of oestrogen receptor (ER) antagonist, ICI 182780. The present results suggested that DFTF is effective in protecting against OVX-induced bone loss in mice, and its actions in regulating osteoblastic activities appear to be mediated by ER. © 2013 The Authors.


Wong K.C.,Hong Kong Polytechnic University | Law M.C.,Hong Kong Polytechnic University | Wong M.S.,Hong Kong Polytechnic University | Wong M.S.,State Key Laboratory of Chinese Medicine and Molecular Pharmacology Incubation | And 2 more authors.
Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences | Year: 2014

(-)-Epiafzelechin is a flavan-3-ol commonly found in plant source. Biological studies suggested that (-)-epiafzelechin may have anti-inflammatory, anti-oxidant and bone-protective effect. However, it's in vivo efficacy remains to be demonstrated. A specific detection method for (-)-epiafzelechin was successfully developed by using UPLC-MS/MS to quantify the amount of (-)-epiafzelechin present in mice plasma after a liquid-liquid extraction by ethyl acetate. The separation was achieved by using a reversed-phase C18 column with a 16min gradient elution protocol consisting of water (0.1%, v/v, formic acid) and 0-70% ACN (0.1%, v/v, formic acid). The lower limit of quantitation for (-)-epiafzelechin was found to be 12.5ng/mL. This method exhibited a good linearity (r2=0.992). The intra-day and inter-day precision were within 12%, while the accuracy was between 97.6 and 113. 4%. A quantity of 10mg/kg synthetic (-)-epiafzelechin was administered to C57BL/6J mice by intravenous (i.v.) and intraperitoneal (i.p.) injections and the blood was collected at different time points. The plasma was then analyzed by the UPLC-MS/MS method, and the plasma drug concentration-time curves for i.v. and i.p. (-)-epiafzelechin injection were constructed. The maximum concentrations (Cmax) of (-)-epiafzelechin in blood by i.v. and i.p. injection were found to be 10.6 and 6.0μg/mL, respectively, while the time for reaching Cmax in i.p. injection was found to be 15min. The distribution half-lives of (-)-epiafzelechin after i.v. and i.p. injection were found to be 7.0 and 12.6min, respectively. Some of the PK parameters were found to be similar in both i.v. and i.p. injections of (-)-epiafzelechin owing to its high solubility in water. © 2014.


Dong X.-L.,Hong Kong Polytechnic University | Zhang Y.,Hong Kong Polytechnic University | Zhang Y.,University of Shanghai for Science and Technology | Wong M.-S.,Hong Kong Polytechnic University | Wong M.-S.,State Key Laboratory of Chinese Medicine and Molecular Pharmacology Incubation
Life Sciences | Year: 2014

Aims The study is designed to determine whether estrogen and vitamin D endocrine systems interact to regulate calcium (Ca) balance as well as changes in mRNA expression of epithelial Ca transport proteins involved in intestinal and renal Ca transport in aging animals in response to ovariectomy and low dietary Ca intake. Main methods Eleven-month-old female sham or ovariectomized (OVX) rats were divided into four groups and fed with either a low-Ca (LCD; 0.1% Ca, 0.65% P) or a high-Ca (HCD; 1.2% Ca, 0.65% P) diet for 12 weeks. Ca balance and mRNA expression of Ca transport proteins in the intestine and kidney from rats were systematically studied. Key findings OVX rats fed with LCD resulted in a negative Ca balance. LCD suppressed serum Ca in OVX but not sham rats, resulting in an induction of serum PTH and 1,25(OH)2D3 levels. The surge in serum 1,25(OH)2D3 levels in LCD-fed OVX rats was associated with an increase in mRNA expression of intestinal transient receptor potential cation channel (TRPV6) and calbindin D9k (CaBP9k) as well as renal vitamin D receptor (VDR), but such an induction was unable to restore Ca balance in vivo. In contrast, the negative Ca balance was associated with suppression of intestinal plasma membrane Ca pump (PMCA1b) and renal transient receptor potential cation channel (TRPV5), calbindin D28k (CaBP28k) and PMCA1b mRNA expression in aged OVX rats. Significance Negative Ca balance in aged female OVX rats is associated with estrogen-dependent and vitamin D-independent downregulation of epithelial Ca transport protein mRNA expression. © 2013 Elsevier Inc.


Sham T.-T.,Hong Kong Polytechnic University | Chan C.-O.,Hong Kong Polytechnic University | Chan C.-O.,State Key Laboratory of Chinese Medicine and Molecular Pharmacology Incubation | Wang Y.-H.,Shanghai University of Traditional Chinese Medicine | And 5 more authors.
BioMed Research International | Year: 2014

Hyperlipidemia, characterized by the abnormal blood lipid profiles, is one of the dominant factors of many chronic diseases such as diabetes, obesity, and cardiovascular diseases (CVD). For the low cost, effectiveness, and fewer side effects, the popularity of using traditional Chinese medicine (TCM) to handle hyperlipidemia is increasing and its role in health care has been recognized by the public at large. Despite the importance of TCM herbs and formulations, there is no comprehensive review summarizing their scientific findings on handling hyperlipidemia. This review summarizes the recent experimental and clinical results of nine representative single Chinese herbs and seven classic TCM formulae that could improve lipid profiles so as to help understand and compare their underlying mechanisms. Most of single herbs and formulae demonstrated the improvement of hyperlipidemic conditions with multiple and diverse mechanisms of actions similar to conventional Western drugs in spite of their mild side effects. Due to increasing popularity of TCM, more extensive, well-designed preclinical and clinical trials on the potential synergistic and adverse side effects of herb-drug interactions as well as their mechanisms are warranted. Hyperlipidemic patients should be warned about the potential risks of herb-drug interactions, particularly those taking anticoagulants and antiplatelet drugs. © 2014 Tung-Ting Sham et al.


Mukwaya E.,University of Shanghai for Science and Technology | Xu F.,University of Shanghai for Science and Technology | Wong M.-S.,State Key Laboratory of Chinese Medicine and Molecular Pharmacology Incubation | Wong M.-S.,Hong Kong Polytechnic University | And 3 more authors.
Pharmaceutical Biology | Year: 2014

Context: Chinese herbal medicine (CHM) has been widely used in clinical practice to treat bone disease for thousands of years. They are cost-effective with fewer side effects and are more suitable for long-term use compared with chemically synthesized medicines. Objective: Chinese herbal formula prescribed among the CHMs is safe, and it is an alternative medicine for bone-related diseases such as osteoporosis. Methods: Science Direct and Google Scholar were used to search articles published. The input key words were CHM, osteoporosis, Chinese herbal formula, traditional Chinese medicine, single herb, multiple-herbs, and bone health. CHMs (single herb and formula) lacking sufficient proof and evidence in the literature were excluded and only those with high citation were retained. Results: A brief review was summarized to indicate the application and the potential mechanism of single herb formula and multi-herb formula in treating the common bone-related diseases such as inflammation, fracture, osteopenia, and osteoporosis. Conclusion: In order to ensure safety and efficacy of all these CHMs, the prescriptions with single herb and multi-component formula must be verified and ensured by reliable pharmacological and toxicological methods. Much more effort needs to be done for studying the standardization, safety evaluation, and mechanism exploration of herb formula as well as confirming the compatibility of these herbs which make one. © 2014 Informa Healthcare USA, Inc. All rights reserved: reproduction in whole or part not permitted.


Gao Q.-G.,Hong Kong Polytechnic University | Chan H.-Y.,Hong Kong Polytechnic University | Man C.W.-Y.,Hong Kong Polytechnic University | Wong M.-S.,Hong Kong Polytechnic University | Wong M.-S.,State Key Laboratory of Chinese Medicine and Molecular Pharmacology Incubation
Journal of Steroid Biochemistry and Molecular Biology | Year: 2014

Recent studies indicated that both estren and Rg1 appear to be able to activate mitogen-activated protein kinase (MAPK) pathway in estrogen responsive cells. Rg1 could lead to MAPK activation through ligand-independent activation of estrogen receptor (ER), while estren could activate the Src-MAPK pathway in an ERE-independent manner. Thus, it is important to understand the mechanistic insights on the difference in transcriptional activation between estren and Rg1. The present study also addressed the differential abilities of Rg1 and estren in terms of the ability to activate ER and the ability to induce ER translocation in MCF-7 cells. Our data indicated that Rg1 could increase pS2 gene expression, and could recruit the co-activator steroid receptor co-activator-1 (SRC-1) to the pS2 promoter. Rg1 could also induce ERα nuclear translocation as well as ERα phosphorylation at Ser118 principally in the cytoplasm in MCF-7 cells. We deduced that estren induced ERE-dependent transcriptional activity and activated ERα at Ser118 occurred in the nucleus of MCF-7 cells. However, it was found to decrease pS2 gene expression and failed to induce the recruitment of SRC-1 to the pS2 promoter in MCF-7 cells. Our results suggest that the abilities of Rg1 and estren to regulate pS2 gene expression, to recruit co-activators as well as to induce sub-cellular distribution of ERα are dramatically different. © 2014 Elsevier Ltd.


Cheng J.,East China Normal University | Cheng J.,City University of Hong Kong | Gu Y.-J.,Hong Kong Polytechnic University | Cheng S.H.,City University of Hong Kong | And 2 more authors.
Journal of Biomedical Nanotechnology | Year: 2013

Gold nanoparticles have been widely explored as cancer therapeutics and diagnostic agents in recent years. With their unique subcellular size and good biocompatibility, gold nanoparticles are a promising drug delivery vehicle. In this study, folic acid-coated gold nanoparticles conjugated with fluorophore FITC through amine terminated poly(ethylene glycol) were prepared and confocal microscopy together with bright-field differential interference contrast imaging data showed that folic acid-coated gold nanoparticles accumulated mainly in cytoplasm of primary human fibroblasts, without causing any observable cytotoxicity upon exposure for 48 hours. Through the further development of a drug delivery system that conjugates doxorubicin onto the surface of gold nanoparticles with a poly(ethylene glycol) spacer via an SMCC linker, we demonstrated that multidrug resistance in cancer cells can be significantly overcome by a combination of highly efficient cellular entry and enhanced cytotoxicity of Au-SMCC-DOX nanoconjugates, as revealed both by confocal microscopy imaging and cytotoxicity assay. The prepared Au-SMCC-DOX nanoconjugates demonstrated enhanced drug accumulation and retention in multidrug resistant hepG2-R cancer cells when it was compared with free doxorubicin, with a cytoplasm accumulation profile. The results indicated that gold nanoparticles are a kind of promising drug delivery vehicle with good biocompatibility and suitable for further applications in drug delivery for improved chemotherapy, especially for overcoming multidrug resistance. Copyright © 2013 American Scientific Publishers All rights reserved.


Wong K.-C.,Hong Kong Polytechnic University | Lee K.-S.,Hong Kong Polytechnic University | Luk H.-K.,Hong Kong Polytechnic University | Wan H.-Y.,Hong Kong Polytechnic University | And 6 more authors.
American Journal of Chinese Medicine | Year: 2014

Er-xian Decoction (EXD), containing Herba epimedii Maxim (HEP) and Curculigo orchioides Gaertn (XM) as principal drugs, is a traditional Chinese medicine (TCM) formula prescribed for the treatment of postmenopausal osteoporosis. In the present study, the in vivo anti-osteoporosis effects of EXD, HEP and XM on four-month-old ovariectomized (OVX) Sprague-Dawley rats were investigated. Micro-computed tomography analysis showed that EXD could significantly improve the micro-architectural parameters (BMD, BV/TV, Tb.N, Tb.Th, and Tb.Sp) of trabecular bone in the distal femur and proximal tibia in OVX rats (p < 0.05). The biomechanical parameters of the distal femur in rats treated with EXD were also improved significantly (p < 0.05 vs. OVX group). The in vivo efficacy of EXD was found to be superior to HEP or XM alone in improving the bone properties of OVX rats. Treatment of rat osteoblastic-like UMR-106 cells with EXD, HEP, and XM significantly promoted the cell proliferation rate (p < 0.05) with the most promising effects observed in cells treated with EXD (p < 0.001). The proliferative effect in UMR-106 cells induced by EXD, HEP, and XM were abolished in the presence of the estrogen antagonist, ICI182780, suggesting that their effects were mediated by estrogen receptor (ER). Additionally, EXD could activate ER-α and ER-β mediated estrogen-response element (ERE)-dependent luciferase activity as well as phosphorylate ER-α at serine 118 in UMR-106 cells. Taken together, EXD offered better osteoprotective effects than its single principal herb, and the beneficial effects of EXD in preventing bone deteriorations are, at least partially, through the ER signaling pathway. © 2014 World Scientific Publishing Company.

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