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Wang R.,Jiangxi University of Traditional Chinese Medicine | Peng L.,Jinan University | Zhao J.,Jinan University | Zhang L.,Jinan University | And 4 more authors.
International Journal of Molecular Sciences | Year: 2015

Gardenamide A (GA) protects the rat retinal ganglion (RGC-5) cells against cell apoptosis induced by H2O2. The protective effect of GA was completely abrogated by the specific phosphoinositide 3-kinase (PI3K) inhibitor LY294002, and the specific protein kinase B (Akt) inhibitor Akt VIII respectively, indicating that the protective mechanism of GA is mediated by the PI3K/Akt signaling pathway. The specific extracellular signal-regulated kinase (ERK1/2) inhibitor PD98059 could not block the neuroprotection of GA. GA attenuated the levels of reactive oxygen species (ROS) and malondialdehyde (MDA) induced by H2O2. Western blotting showed that GA promoted the phosphorylation of ERK1/2, Akt and endothelial nitric oxide synthase (eNOS), respectively, and effectively reversed the H2O2-inhibited phosphorylation of these three proteins. LY294002 completely inhibited the GA-activated phosphorylation of Akt, while only partially inhibiting eNOS. This evidence implies that eNOS may be activated directly by GA. PD98059 attenuated only partially the GA-induced phosphorylation of ERK1/2 with/without the presence of H2O2, indicating that GA may activate ERK1/2 directly. All these results put together confirm that GA protects RGC-5 cells from H2O2 insults via the activation of PI3K/Akt/eNOS signaling pathway. Whether the ERK1/2 signaling pathway is involved requires further investigations. © 2015 by the authors; licensee MDPI, Basel, Switzerland.


Wang R.,Jiangxi University of Traditional Chinese Medicine | Zhao J.,Jinan University | Zhang L.,Jinan University | Peng L.,Jinan University | And 4 more authors.
International Journal of Molecular Sciences | Year: 2016

CHR20 and CHR21 are a pair of stable diastereoisomers derived from genipin. These stereoisomers are activators of neuronal nitric oxide synthase (nNOS) and endothelial nitric oxide synthase (eNOS). In the rat retinal ganglion (RGC-5) cell model these compounds are non-toxic. Treatment of RGC-5 with 750 μM of sodium nitroprusside (SNP) produces nitrosative stress. Both genipin derivatives, however, protect these cells against SNP-induced apoptic cell death, although CHR21 is significantly more potent than CHR20 in this regard. With Western blotting we showed that the observed neuroprotection is primarily due to the activation of protein kinase B (Akt)/eNOS and extracellular signal-regulated kinase (ERK1/2) signaling pathways. Therefore, LY294002 (a phosphatidylinositol 3-kinase (PI3K) inhibitor) or PD98059 (a MAPK-activating enzyme inhibitor) abrogated the protective effects of CHR20 and CHR21. Altogether, our results show that in our experimental setup neuroprotection by the diasteromeric pair is mediated through the PI3K/Akt/eNOS and ERK1/2 signaling pathways. Further studies are needed to establish the potential of these compounds to prevent ntric oxide (NO)-induced toxicity commonly seen in many neurodegenerative diseases. © 2016 by the authors; licensee MDPI, Basel, Switzerland.


Wang R.,Sun Yat Sen University | Yang J.,Jinan University | Peng L.,Jinan University | Zhao J.,Jinan University | And 5 more authors.
Neuroscience | Year: 2015

Gardenamide A (GA) is a stable genipin derivative with neuroprotective properties. It rescued pheochromocytoma cell (PC12) sympathetic cultures and retinal neuronal cells from apoptosis insult induced by serum deprivation. GA attenuated the accumulation of intracellular reactive oxygen species (ROS) and the loss of mitochondrial membrane potential. Western blotting with specific phospho-antibodies indicated that GA increased the phosphorylation of both the protein kinase B (Akt) and the extracellular signal-regulated kinase (ERK1/2) in PC12 cells. The GA neuroprotective effect was inhibited by either the specific phosphoinositide 3-kinase (PI3K) inhibitor LY294002 or the mitogen-activated protein kinase (MAPK) pathway inhibitor PD98059. These results propose that the neuroprotective effect of GA on PC12 neuronal cell cultures was mediated through both the PI3K/Akt and ERK1/2 signaling pathways. Therefore, GA may serve as a pharmacological tool to investigate neuroprotective mechanisms of neurons afflicted by different insults. © 2014 IBRO.


Zhao J.,Jinan University | Peng L.,Jinan University | Zheng W.,University of Macao | Wang R.,Jiangxi University of Traditional Chinese Medicine | And 4 more authors.
International Journal of Molecular Sciences | Year: 2015

Two amantadine (ATD)-gardenamide A (GA) ligands have been designed and synthesized. The bonding of ATD with GA through a methylene carbonyl brigde (L1) enhances the neuroprotective effect against corticosterone (CORT)-induced impairments in PC12 cells; while the bonding through a succinyl brigde (L2) does not. L1 reduces the level of reactive oxygen species (ROS) and cell apoptosis generated by CORT. It restores CORT-changed cell morphology to a state that is closed to normal PC12 cells. One mechanism of L1 to attenuate CORT-induced cell apoptosis is through the adjustment of both caspase-3 and Bcl-2 proteins. Like GA, both nNOS and eNOS might be involved in the neuroprotective mechanism of L1. All the evidences suggest that L1 may be a potential agent to treat depression. © 2015 by the authors; licensee MDPI, Basel, Switzerland.


Yang M.-X.,Jinan University | Yang M.-X.,Zhongshan Torch Polytechnic College | Liang Y.-G.,UNO Scientific Co. | Chen H.-R.,Jinan University | And 3 more authors.
Chinese Traditional and Herbal Drugs | Year: 2014

Objective: To investigate the chemical constituents from the leaves of wild Aquilaria sinensis. Methods: The powder of the dried leaves was percolated with 70% acetone. Various chromatographic methods were employed to isolate the compounds and their structures were established by spectroscopic analysis. Results: Thirteen compounds were isolated and identified as 6-E-octadecenoic acid (1), ethyl linoleate (2), apiolin-7, 4'-dimethyl ether (3), 4-cyanobenzaldehyde (4), luteolin-7, 3', 4'-trimethyl ether (5), genkwanin (6), p-phthalic acid di (4-octyl) ester (7), 6-hydroxy-7, 4'-dimethoxyflavone (8), 5-hydroxy-7, 2', 4', 5'- tetramethoxyflavone (9), 5, 4'-dihydroxy-7, 3'-dimethoxyflavone (10), quercetin (11), kaempferol (12), and 4-hydroxybenzoic acid (13). Conclusion: Thirteen compounds have been identified from wild A. sinensis leaves. Compounds 4, 8, and 9 are firstly isolated from the plants of Thymelaeaceae.


Yang Z.-Y.,Jinan University | Lu D.-Y.,Jinan University | Yao S.,University of Sichuan | Zhang R.-R.,Jinan University | And 3 more authors.
Journal of Food and Drug Analysis | Year: 2013

An HPLC-DAD-ESI-MS method was employed for the chromatographic fingerprint analysis of Cistanche deserticola (Roucongrong in Chinese). Eleven batches of samples were analyzed to establish the reference fingerprint of C. deserticola. Eight peaks in the fingerprint of all the 11 batches of samples were assigned as "characteristic peaks", and identified by comparing their retention time and mass spectra with those of the reference substances. The similarity of the 11 batches of samples was evaluated by a simulative mean chromatogram. The results indicated that the samples from different origins shared similar HPLC fingerprints. In addition, an HPLC-DAD method was developed for simultaneous determination of the contents of the eight compounds in C. deserticola. All eight compounds showed good linear regression (R2 > 0.9998) within test ranges and the recovery of the method was in the range of 93.65-109.79%, indicating that the developed method combining chromatographic fingerprint with quantification analysis could readily be applied for the quality control of C. deserticola.


Zheng J.,Jinan University | Deng L.,Jinan University | Chen M.,Jinan University | Xiao X.,Jinan University | And 10 more authors.
European Journal of Medicinal Chemistry | Year: 2013

Thorough simplification of vinca alkaloids based on pharmacophore similarity has been conducted. A concise process for the syntheses of target compounds was successfully developed with yields from poor to excellent (19-98%). Cell growth inhibitory activities of these synthesized compounds were evaluated in five cancer cell lines including MCF-7, MDA-MB-231, HepG2, HepG2/ADM and K562. Almost all compounds exhibited moderate antitumor activity with optimal IC50 value of 0.89 ± 0.07 μM in MCF-7 cells. Investigation of structure-activity relationship (SAR) indicates that electron-withdraw substituents on the ring contribute to the enhancement of the antitumor activities. The simplified vinca alkaloids are confirmed as antimitotic agents, which inhibit the polymerization of tubulin just like vinblastine. © 2013 Elsevier Masson SAS. All rights reserved.


Wang R.,Jiangxi University of Traditional Chinese Medicine | Zhao T.,Puyang Maternaity and Child Care Hospital | Sun Y.,Jiangxi University of Traditional Chinese Medicine | Chen H.,Jinan University | Chen H.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research
Zhongshan Daxue Xuebao/Acta Scientiarum Natralium Universitatis Sunyatseni | Year: 2015

In order to investigate the protective effects of Momordica charantia extract (MCE) on obesity and insulin resistance, C57BL/6j mice fed in a high-fat diet (HFD) were used as animal model. Obese mouse model was successfully made after 2-week HFD induction. The mice were then randomly divided into normal control, model control, MCE dose of 13.5, 27.0, and 54.0 g/kg treated groups. Mice in normal and model control groups were treated with 0.5% CMC-Na, and other groups were treated with MCE (i. g.), respectively, with the same volume twice a day for ten weeks. It was shown that the body weight, epididymal and total visceral white adipose tissue weight were decreased by treatment of MCE 54.0 g/kg without the change of food intake. The increased serum TG, CHO, LDL-C, glucose, insulin concentration and insulin resistance index were significantly inhibited. The concentration of TG was also decreased by the treatment of MCE 27.0 g/kg; while the concentration of HDL-C was increased by the treatment of MCE 13.5, 27.0 and 54.0 g/kg, respectively. The adipocyte hypertrophy induced by HFD was mitigated by MCE dose-dependently. © 2015, Journal of Zhongshan University. All right reserved.


Feng W.,Jinan University | Feng W.,Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research | Mei S.,Jinan University | Wenjie Y.,Jinan University | Luyuan H.,CAS Guangzhou Institute of Biomedicine and Health
Protein Expression and Purification | Year: 2011

Manganese superoxide dismutase (Mn-SOD) is one of the major enzymes responsible for the defense against oxidative damage due to reactive oxygen species (ROS) in the mitochondria. The present study aimed to produce and evaluate the genetically engineered manganese superoxide dismutase protein. A recombinant plasmid containing DNA segment coding Mn-SOD protein was transformed into Escherichia coli (E. coli) Rosetta-gami strain, for expression. After induction with IPTG, an expected molecular mass of 25 kDa was detected by SDS-PAGE. After Ni-NTA affinity chromatography purification, the purity rate came up to 95%. UV spectroscopy data for our preparations indicated that a peak at 275 nm existed in the spectrum. SOD activity assay showed that the activity of the rhMn-SOD was 1890.9 U/mg. The ORAC level of rhMn-SOD was 151492.2 uM Trolox equiv/mg. Furthermore, in vitro bioacitivity assay indicated that the rhMn-SOD protein can inhibit the proliferation of the leukemia K562 cells. © 2010 Elsevier Inc. All rights reserved.


Lu D.,Jinan University | Zhang J.,Beijing University of Chinese Medicine | Yang Z.,Jinan University | Liu H.,Jinan University | And 6 more authors.
Journal of Separation Science | Year: 2013

We aim to determine the chemical constituents of three species of Cistanches Herba using HPLC coupled with diode array detection and high-resolution MS. Ten phenylethanoid glycosides were identified and further quantified as marker substances by HPLC coupled with diode array detection method. The separation was conducted using an Agilent TC-C18 column with 0.1% formic acid and methanol as the mobile phases under gradient elution. The analytical method was fully validated in terms of linearity, sensitivity, precision, repeatability as well as recovery, and subsequently applied to evaluate the quality of 36 batches of Cistanche plants. The chemometric procedures (i.e., hierarchical clustering analysis and principal component analysis) were used to compare different species of Cistanches Herba, leading to successful classification of the Cistanche samples in accordance with their origins. In conclusion, this study provides a chemical basis for quality control of Cistanches Herba. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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