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Dive into the research topics where Jian-Dong Jiang is active.

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Featured researches published by Jian-Dong Jiang.


Metabolism-clinical and Experimental | 2008

Combination of simvastatin with berberine improves the lipid-lowering efficacy

Wei-Jia Kong; Jin Wei; Zeng-Yan Zuo; Yue-Ming Wang; Dan-Qing Song; Xue-Fu You; Li-Xun Zhao; Huai-Ning Pan; Jian-Dong Jiang

We have identified berberine (BBR) as a novel cholesterol-lowering drug acting through stabilization of the low-density lipoprotein receptor (LDLR) messenger RNA. Because the mechanism differs from that of statins, it is of great interest to examine the lipid-lowering activity of BBR in combination with statins. Our results showed that combination of BBR with simvastatin (SIMVA) increased the LDLR gene expression to a level significantly higher than that in monotherapies. In the treatment of food-induced hyperlipidemic rats, combination of BBR (90 mg/[kg d], oral) with SIMVA (6 mg/[kg d], oral) reduced serum LDL cholesterol by 46.2%, which was more effective than that of the SIMVA (28.3%) or BBR (26.8%) monotherapy (P < .01 for both) and similar to that of SIMVA at 12 mg/(kg d) (43.4%). More effective reduction of serum triglyceride was also achieved with the combination as compared with either monotherapy. Combination of BBR with SIMVA up-regulated the LDLR messenger RNA in rat livers to a level about 1.6-fold higher than the monotherapies did. Significant reduction of liver fat storage and improved liver histology were found after the combination therapy. The therapeutic efficacy of the combination was then evaluated in 63 hypercholesterolemic patients. As compared with monotherapies, the combination showed an improved lipid-lowering effect with 31.8% reduction of serum LDL cholesterol (P < .05 vs BBR alone, P < .01 vs SIMVA alone). Similar efficacies were observed in the reduction of total cholesterol as well as triglyceride in the patients. Our results display the rationale, effectiveness, and safety of the combination therapy for hyperlipidemia using BBR and SIMVA. It could be a new regimen for hypercholesterolemia.


Bioorganic & Medicinal Chemistry Letters | 2008

Synthesis and structure–activity relationships of berberine analogues as a novel class of low-density-lipoprotein receptor up-regulators

Peng Yang; Dan-Qing Song; Ying-Hong Li; Wei-Jia Kong; Yan-Xiang Wang; Li-Mei Gao; Shu-Yu Liu; Rui-Qiang Cao; Jian-Dong Jiang

Berberine (BBR, 1) is a novel cholesterol-lowering agent that up-regulates low-density-lipoprotein receptor (LDLR) expression through a mechanism different from that of statins. Because of the unique mode of action and good safety record, BBR provoked our interest to do structure modification at different domains for its cholesterol-lowering activity. Nineteen BBR analogues with substituents on the benzene ring D were synthesized in the present study. The analysis of structure-activity relationship (SAR) indicated that the two methoxyl groups in an ortho-distribution on this benzene ring afforded a good activity. Among the 19 analogues, compound 8j bearing a methoxyl at both 10- and 11-position showed an increased LDLR up-regulatory activity in respect to BBR, and therefore has been selected as a promising cholesterol-lowering drug candidate for further evaluation.


Bioorganic & Medicinal Chemistry Letters | 2009

Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines)

Zongying Liu; Yue-ming Wang; Zhuorong Li; Jian-Dong Jiang; David W. Boykin

A series of 3,4-diarylthiazol-2(3H)-ones and three 3,4-diarylthiazol-2(3H)-imines were synthesized and evaluated for their cytotoxicity in a panel of human cancer cell lines. Compounds 21 and 22 showed potential anticancer activity against human CEM cells with IC50 values of 0.12 and 0.24microM, respectively.


Bioorganic & Medicinal Chemistry Letters | 2009

Synthesis and biological evaluation of berberine analogues as novel up-regulators for both low-density-lipoprotein receptor and insulin receptor

Yan-Xiang Wang; Yu-Ping Wang; Hao Zhang; Wei-Jia Kong; Ying-Hong Li; Fei Liu; Rong-Mei Gao; Ting Liu; Jian-Dong Jiang; Dan-Qing Song

Berberine (BBR) is a natural compound with up-regulating activity on both low-density-lipoprotein receptor (LDLR) and insulin receptor (InsR). This one-drug-multiple-target characteristic might be suitable for the treatment of metabolic syndrome. In searching for up-regulators effective for both LDLR and InsR expression, the structure-activity relationship (SAR) analysis for BBR analogues was done. Fourteen BBR analogues were designed, synthesized and biologically evaluated. SAR analysis revealed that appropriate modifications on the phenyl ring A or D of BBR might retain the up-regulatory activities on the expression of both LDLR and InsR. Among these compounds, compound 13a bearing 9-methoxy and 10-hydroxyl on the ring D showed promising activities on either LDLR or InsR gene expression. The 10-hydroxyl of 13a could be an arm to connect proper chemical groups for optimizing drug-bioavailability in vivo. Thus, 13a could be considered to be a parent compound to make pro-drugs for either blood lipids or glucose.


Organic Letters | 2013

Myriberine A, a New Alkaloid with an Unprecedented Heteropentacyclic Skeleton from Myrioneuron faberi

Sheng-Dian Huang; Yu Zhang; Ming-Ming Cao; Ying-Tong Di; Gui-Hua Tang; Zong-Gen Peng; Jian-Dong Jiang; Hongping He; Xiao-Jiang Hao

Myriberine A (1) possessing an unprecedented carbon skeleton was isolated from Myrioneuron faberi. The structure and absolute configuration of 1 were elucidated by a combination of spectroscopic data, X-ray crystallographic, and computational methods. Myriberine A (1) demonstrated inhibition against the hepatitis C virus (HCV) life cycle in vitro.


Journal of Organic Chemistry | 2014

Cyclohexane-Fused Octahydroquinolizine Alkaloids from Myrioneuron faberi with Activity against Hepatitis C Virus

Ming-Ming Cao; Yu Zhang; Xiao-Hui Li; Zong-Gen Peng; Jian-Dong Jiang; Yu-Cheng Gu; Ying-Tong Di; Xiao-Nian Li; Duo-Zhi Chen; Cheng-Feng Xia; Hongping He; Shun-Lin Li; Xiao-Jiang Hao

Investigation of the alkaloids from Myrioneuron faberi, a plant unique to China, gave four pairs of enantiomers (1-4). (±)-β-Myrifabral A (1) and (±)-α-myrifabral A (2) formed an inseparable mixture of anomers (cluster A), as did (±)-β-myrifabral B (3) and (±)-α-myrifabral B (4) (cluster B). Their structures were determined by X-ray diffraction and NMR analysis. Compounds 1-4 possessed novel cyclohexane-fused octahydroquinolizine skeletons and represent the first quinolizidine alkaloids from the genus Myrioneuron. The epimers of cluster A (1 and 2) were modified and separated. In vitro, clusters A and B and their derivatives inhibited replication of hepatitis C virus (HCV, IC50 0.9 to 4.7 μM) with cytotoxicity lower than that of telaprevir.


Bioorganic & Medicinal Chemistry Letters | 2013

Evaluation of anti-HCV activity and SAR study of (+)-lycoricidine through targeting of host heat-stress cognate 70 (Hsc70)

Duo-Zhi Chen; Jian-Dong Jiang; Ke-Qing Zhang; Hong-Ping He; Ying-Tong Di; Yu Zhang; Jie-Yun Cai; Lei Wang; Shun-Lin Li; Ping Yi; Zong-Gen Peng; Xiao-Jiang Hao

The anti hepatitis C virus (HCV) activity of (+)-lycoricidine (1) was evaluated for the first time in this letter, yielding an EC50 value of 0.55 nmol/mL and an selection index (SI) value of 12.72. Further studies indicated that 1 induced this effect by down-regulating host heat-stress cognate 70 (Hsc70) expression. In addition, 20 derivatives were designed and synthesised to investigate the basic structure-activity relationship (SAR) of the title compound. Several of these derivatives exhibit a good inhibition of HCV, such as compound 3 (EC50=0.68 nmol/mL, SI=33.86), compound 2d (EC50=15 nmol/mL, SI=12) and compound 5 (EC50=33 nmol/mL, SI >10.91). Meanwhile, the experimental data suggest that the modification of certain groups of (+)-lycoricidine can reduce the cytotoxicity of the compounds.


Journal of Natural Products | 2016

Myritonines A–C, Alkaloids from Myrioneuron tonkinensis Based on a Novel Hexacyclic Skeleton

Xiao-Hui Li; Yu Zhang; Jia-Hui Zhang; Xiao-Nian Li; Ming-Ming Cao; Ying-Tong Di; Zong-Gen Peng; Jian-Dong Jiang; Xiao-Jiang Hao

Myritonines A-C (1-3), three new alkaloids bearing an unprecedented heterohexacyclic skeleton, were isolated from Myrioneuron tonkinensis. Their structures were determined by a combination of spectroscopic data and single-crystal X-ray diffraction analysis. Compound 3 represents the first Myrioneuron alkaloid featuring a unique trans-decahydroquinoline motif and was also found to possess a rare cyano functionality. Compounds 1 and 2 showed inhibition against the hepatitis C virus in vitro.


Journal of Natural Products | 2015

Alkaloids with Different Carbon Units from Myrioneuron faberi

Ming-Ming Cao; Yu Zhang; Sheng-Dian Huang; Ying-Tong Di; Zong-Gen Peng; Jian-Dong Jiang; Chun-Mao Yuan; Duo-Zhi Chen; Shun-Lin Li; Hongping He; Xiao-Jiang Hao

Three new Myrioneuron alkaloids, myrifamines A-C (1-3), with unique skeletons were isolated from Myrioneuron faberi. The absolute configuration of 1 was confirmed by single-crystal X-ray diffraction analysis, and the stereochemistry of the other two alkaloids was determined using a combination of ROESY experiments and calculated and experimental electronic circular dichroism spectra. Myrifamine C (3) is the first example of a symmetric dimer among the Myrioneuron alkaloids. Known alkaloids myrionamide (4) and schoberine (5) were also isolated, and experimental NMR and X-ray diffraction data suggest their structural revision. Compound 2 showed significant inhibitory activity toward the hepatitis C virus in vitro, with a therapeutic index (CC50/EC50) greater than 108.7.


Journal of Asian Natural Products Research | 2008

A potent anti-HIV polyphenol from Salvia yunnanensis

Zheng-Fu Zhang; Hong-Shan Chen; Zong-Gen Peng; Zhuorong Li; Jian-Dong Jiang

A new polyphenol, designated as salvianolic acid N, was isolated from the aqueous extracts of the roots of Salvia yunnanensis. Its chemical structure was elucidated as 3-(3,4-dihydroxylphenyl)-2-{(E)-3-(1,8,9-trihydroxyl-dibenzo[b,f]oxpin-3-yl)acryloxloxy}propanoic acid (1) on the basis of NMR and MS spectral analyses. The new polyphenol inhibited both HIV-1 IN in vitro and also reduced HIV-1 p24 antigen in MT-4 cell lines.

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Zong-Gen Peng

Peking Union Medical College

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Xiao-Jiang Hao

Chinese Academy of Sciences

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Yu Zhang

Chinese Academy of Sciences

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Ming-Ming Cao

Chinese Academy of Sciences

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Dan-Qing Song

Peking Union Medical College

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Ying-Tong Di

Chinese Academy of Sciences

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Zhuorong Li

Peking Union Medical College

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Duo-Zhi Chen

Chinese Academy of Sciences

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Shun-Lin Li

Chinese Academy of Sciences

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Ying-Hong Li

Peking Union Medical College

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