Guangzhou General Pharmaceutical Research Institute

Guangzhou, China

Guangzhou General Pharmaceutical Research Institute

Guangzhou, China
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Yang D.-L.,Sun Yat Sen University | Xu J.-W.,Sun Yat Sen University | Zhu J.-G.,Guizhou University | Zhu J.-G.,Guangzhou University | And 19 more authors.
Biochemical and Biophysical Research Communications | Year: 2017

Several studies have implicated estrogen and the estrogen receptor (ER) in the pathogenesis of benign prostatic hyperplasia (BPH); however, the mechanism underlying this effect remains elusive. In the present study, we demonstrated that estrogen (17β-estradiol, or E2)-induced activation of the G protein-coupled receptor 30 (GPR30) triggered Ca2+ release from the endoplasmic reticulum, increased the mitochondrial Ca2+ concentration, and thus induced prostate epithelial cell (PEC) apoptosis. Both E2 and the GPR30-specific agonist G1 induced a transient intracellular Ca2+ release in PECs via the phospholipase C (PLC)-inositol 1, 4, 5-triphosphate (IP3) pathway, and this was abolished by treatment with the GPR30 antagonist G15. The release of cytochrome c and activation of caspase-3 in response to GPR30 activation were observed. Data generated from the analysis of animal models and human clinical samples indicate that treatment with the GPR30 agonist relieves testosterone propionate (TP)-induced prostatic epithelial hyperplasia, and that the abundance of GPR30 is negatively associated with prostate volume. On the basis of these results, we propose a novel regulatory mechanism whereby estrogen induces the apoptosis of PECs via GPR30 activation. Inhibition of this activation is predicted to lead to abnormal PEC accumulation, and to thereby contribute to BPH pathogenesis. © 2017 Elsevier Inc.


Xu Y.-F.,Guangzhou University of Chinese Medicine | Liang Z.-J.,Guangzhou University of Chinese Medicine | Kuang Z.-J.,Guangzhou University of Chinese Medicine | Chen J.-J.,Guangzhou General Pharmaceutical Research Institute | And 7 more authors.
Experimental and Therapeutic Medicine | Year: 2017

Suo Quan Wan (SQW) has been used to treat lower urinary tract symptoms (LUTS) in elderly patients for hundreds of years in China. β-adrenoceptors (β-ARs), particularly β3-adrenoceptor (β3-AR), was reported to be important in the bladder dysfunction of the elderly. The present study was conducted to explore the effect of β-AR, and particularly the β3-adrenoceptor, in aging rat bladder function in vitro and to test the therapeutic effect of SQW on LUTS in an aging rat model based on the β3-adrenoceptor. Briefly, the bladder detrusor muscles of young (age, 3 months) and aging (age, 15 months) female rats were separated. A β-AR non-selective agonist, isoprenaline (ISO), subtype β3-AR agonist (BRL37344A) and β3-AR antagonist (SR59230A) were used to define the tension change of detrusor muscles between young and aging rats in vitro. For blank controls, 12 young rats were marked, and 48 aging female rats were randomly divided into four groups as follows: Model, SQW high, SQW middle and SQW low. Following oral administration of SQW for 6 weeks in aging rats, urodynamic and bladder detrusor tests were used to evaluate the therapeutic effect of SQW. The expression of β3-AR mRNA was investigated using reverse transcription-quantitative polymerase chain reaction. Using ISO and BRL37344A in vitro, maximum relaxation (Emax), intrinsic activity (IA), and log (50% effective concentration) (PD2) were significantly decreased in aging rats compared with that in young rats (P<0.05). Significant changes were also observed in the β3-AR antagonist experiment, which blocked ISO-induced relaxation, with significant decreases observed in Emax, IA and PD2, and a significant increase observed in PA2 for the aging rats compared with the young controls (P<0.05). SQW was demonstrated to enhance bladder control, storage and contraction ability. Furthermore, SQW was able to increase the sensitivity and expression of β3-AR in an aging rat. In conclusion, the decrease in β3-AR sensitivity in aging rats and the expression resulted in bladder detrusor dysfunction. In addition, the therapeutic effect of SQW against LUTS relies on the former's effect on the urethral sphincter, bladder detrusor and β3-AR. © 2017, Spandidos Publications. All rights reserved.


Guo Q.-P.,Guangzhou General Pharmaceutical Research Institute | Jin R.-M.,Shanghai University of Traditional Chinese Medicine
Chinese Journal of Pharmacology and Toxicology | Year: 2016

To compare the liver toxicity of matrine and oxymatrine, and to explore their toxic mechanism. METHODS Thirty ICR mice were randomly divided into normal control, matrine 200 mg-kg-1 and oxymatrine 200 mg kg-1 groups, 10 mice per group. After single ig administration of corresponding drugs or water, animal mortality was calculated at the ∼\5 day. The content of glutamic-pyruvic transaminase (GPT), glutamic-oxalacetic transamin (GOT), alkaline phosphatase (ALP) and lactate dehydrogenase (LDH) in serum were detected. Histopathological changes of the liver were examined by HE stain. The content of superoxide dismutase(SOD) and glutathione (GSH) in liver homogenates were detected by ELISA. Hepatocyte apoptosis was detected by Tunel stain. RESULTS The mortality rate of mice in two groups was 80% and 0, respectively. GPT, GOT and ALP contents of dead mice in matrine group were significantly higher than that in normal control group(P<0.05). In oxymatrine group, only the content of ALP was increased (PO.05). Four of the eight dead mice in matrine group exhibited liver cell necrosis (PO.05), while only 1/10 mice in oxymatrine group had a mild liver cell necrosis (P>0.05). The content of SOD and GSH of dead mice in matrine group was lower than that in control group ( P< 0.05, P<0.01). The content of GSH in oxymatrine group was also decreased (PO.05). The apoptosis rate of liver cells in dead mice in matrine group was increased (PO.05). CONCLUSION A large dose of matrine and oxymatrine can produce liver toxicity. At an equal dosage, the liver toxicity of matrine is significantly higher than that of oxymatrine. The toxic mechanism is related to oxidative stress and apoptosis.


Guo Q.,Shanghai University of Traditional Chinese Medicine | Guo Q.,Postdoctoral Workstation of Hutchison Whampoa Guangzhou Baiyunshan Chinese Medicine Co. | Yang W.,Guangzhou General Pharmaceutical Research Institute | Xiao B.,Guangzhou General Pharmaceutical Research Institute | And 5 more authors.
Toxin Reviews | Year: 2015

The aim of this study was to systematically study zebrafish model to predict drug-induced liver injury (DILI) with the drug acetaminophen (APAP) and find the sensitive early biomarkers. The concentration-toxicity relationship was determined at concentrations 1, 2, 4, 8, 16-mmol/L of APAP. APAP caused a concentration-dependent mortality of zebrafish. APAP caused a time-dependent mortality. Mild to severe vacuolar degeneration of liver cells were observed. APAP increased serum alanine aminotransferase (ALT), lactate dehydrogenase (LDH) and xanthine oxidase (XOD) levels significantly, while it delevated argininosuccinic acid lyase (ASAL) and total bile acid (TBA) levels. TBA and ASAL were more sensitive than ALT in this process. Zebrafish may be a convenient, practical and valuable biological model to predict DILI. © 2014 Informa Healthcare USA, Inc. All rights reserved: reproduction in whole or part not permitted.


Liu S.,Chinese Academy of Sciences | Liu S.,Hainan University | Yang W.,Guangzhou General Pharmaceutical Research Institute | Liu S.-B.,Chinese Academy of Sciences | And 6 more authors.
Natural Product Communications | Year: 2014

One new diterpenoid, 11α,12βH-dolabella-4,8(17)-dien-3α, 7β,18-triol (1) and one new sesquilignan, 9-methoxy-7′,8′-cis- 7″,8″-cis-buddlenol B (2), together with three known compounds, (+)-diasyringaresinol (3), N-methyl-5- hydroxy-Δ3-pyrrolin-2- one (4) and marmin (5), have been isolated from Aglaia odorata var. microphyllina. Their structures were determined using 1D and 2D NMR spectroscopy. Compound 1 exhibited cytotoxic activity against the K562 cell line with an IC50 value of 12.5 μg/mL.


Zou Y.,CAS Guangzhou Institute of Chemistry | Zou Y.,Guangzhou University | Huang Q.,CAS Guangzhou Institute of Chemistry | Huang Q.,University of Chinese Academy of Sciences | And 8 more authors.
Organic and Biomolecular Chemistry | Year: 2013

A series of trans- or cis-stilbenes have been synthesized in good to excellent yields via a functional group-dependent decarboxylation process from the corresponding 2,3-diaryl acrylic acids in a neutral CuI/1,10-phen/PEG-400 system under microwave conditions. The in situ generation of the recyclable catalytic complex, the use of environmentally benign solvent PEG-400, the operational simplicity, the short reaction times, as well as the functional group-dependent chemo- and stereo-selectivity have made the decarboxylation process a highly efficient and applicable protocol. © 2013 The Royal Society of Chemistry.


Liu X.,Southern Medical University | Wang W.,Guangzhou RiboBio Co. | Samarsky D.,Guangzhou RiboBio Co. | Liu L.,Southern Medical University | And 16 more authors.
Nucleic Acids Research | Year: 2014

RNAi technology is taking strong position among the key therapeutic modalities, with dozens of siRNA-based programs entering and successfully progressing through clinical stages of drug development. To further explore potentials of RNAi technology as therapeutics, we engineered and tested VEGFR2 siRNA molecules specifically targeted to tumors through covalently conjugated cyclo(Arg-Gly-Asp-d-Phe-Lys[PEG-MAL]) (cRGD) peptide, known to bind αvβ3 integrin receptors. cRGD-siRNAs were demonstrated to specifically enter and silence targeted genes in cultured αvβ3 positive human cells (HUVEC). Microinjection of zebrafish blastocysts with VEGFR2 cRGD-siRNA resulted in specific inhibition of blood vessel growth. In tumor-bearing mice, intravenously injected cRGD-siRNA molecules generated no innate immune response and bio-distributed to tumor tissues. Continuous systemic delivery of two different VEGFR2 cRGD-siRNAs resulted in down-regulation of corresponding mRNA (55 and 45%) and protein (65 and 45%) in tumors, as well as in overall reduction of tumor volume (90 and 70%). These findings demonstrate strong potential of cRGD-siRNA molecules as anti-tumor therapy. © 2014 The Author(s).


Yang Y.-Y.,Chinese Academy of Sciences | Yang W.,Guangzhou General Pharmaceutical Research Institute | Zuo W.-J.,Chinese Academy of Sciences | Zeng Y.-B.,Chinese Academy of Sciences | And 3 more authors.
Journal of Asian Natural Products Research | Year: 2013

Two new acridone alkaloids, 3-methoxy-1,4,5-trihydroxy-10-methylacridone (1) and 2,3-dimethoxy-1,4,5-trihydroxy-10-methylacridone (2), were isolated from the ethanol extract of the branch of Atalantia buxifolia. Their structures were elucidated by spectroscopic methods including 1D and 2D NMR. Compounds 1 and 2 exhibited significant antibacterial activity against Staphylococcus aureus and weak inhibitory effect on acetylcholinesterase. © 2013 Taylor & Francis Group, LLC.


PubMed | Chinese Academy of Sciences, Guangdong Shuanglin Bio pharmaceutical Co., Witspool Biopharmaceutical Co., Guangzhou RiboBio Co. and 2 more.
Type: Journal Article | Journal: Nucleic acids research | Year: 2014

RNAi technology is taking strong position among the key therapeutic modalities, with dozens of siRNA-based programs entering and successfully progressing through clinical stages of drug development. To further explore potentials of RNAi technology as therapeutics, we engineered and tested VEGFR2 siRNA molecules specifically targeted to tumors through covalently conjugated cyclo(Arg-Gly-Asp-d-Phe-Lys[PEG-MAL]) (cRGD) peptide, known to bind v3 integrin receptors. cRGD-siRNAs were demonstrated to specifically enter and silence targeted genes in cultured v3 positive human cells (HUVEC). Microinjection of zebrafish blastocysts with VEGFR2 cRGD-siRNA resulted in specific inhibition of blood vessel growth. In tumor-bearing mice, intravenously injected cRGD-siRNA molecules generated no innate immune response and bio-distributed to tumor tissues. Continuous systemic delivery of two different VEGFR2 cRGD-siRNAs resulted in down-regulation of corresponding mRNA (55 and 45%) and protein (65 and 45%) in tumors, as well as in overall reduction of tumor volume (90 and 70%). These findings demonstrate strong potential of cRGD-siRNA molecules as anti-tumor therapy.

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