An International Quarterly Research Journal


                                                               ISSN : 0971 - 9822

                                                             Vol   15,  No   4 ,  October-December,   2011

Asian Chemistry Letters                                                                                    Vol. 15, No. 4 (2011)1-10

Expanded modification of anti-HIV DCK analogues: Bioiosoteres, 8-substitutes change and seco-DCKs


Ying Chen, Qian Zhang and Peng Xia*
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai-201203, China

During the past two decades, many dicamphanoyl-khellactone analogues (DCKs) with angular tricycle scaffold were developed as potent anti-HIV agents by Lee's group. According to bioisosterism, our group further have designed and synthesized a series of novel DCK analogues. Among them, seco-DCKs with only dicycle skeleton not only show good anti-HIV activities, but also seem to get better ADME properties than that of DCKs. This article reviews our research progress on the modification of DCKs by hetero-atom exchange in tricycle core structure, 8-substitutes change and cleavage of core cycles.



Asian Chemistry Letters                                                                                  Vol. 15, No. 4 (2011)11-15

Synthesis and anti-HIV activity of glycyrrhetinic acid derivatives

Ge Jun, Chen Ji-Peng, Chen Ying *, and Xia Peng
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China

Five glycyrrhetinic acid derivatives were synthesized and evaluated for in vitro inhibition of HIV-1 replication  in H9 lymphocytes. Three of them (8, 11, 12) have considerable anti-HIV activity with over 50% inhibitory rate at 10 mg/ml and are worth further study.



Asian Chemistry Letters                                                                                   Vol. 15, No 4 (2011)00-00

Natural products as novel anti-HBV agents


Li-Jun Wang1,2, Chang-An Geng1,2, Rui-Hua Guo1,2, Quan Zhang1, and Ji-Jun Chen1*
1State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany,

Chinese Academy of Sciences, Kunming, 650204, PR China.
2Graduated School of Chinese Academy of Sciences, Beijing, 100039, PR China.

Hepatitis B virus (HBV) infection is a severe health problem all over the world and the present therapeutic strategy for the HBV infection is still unsatisfactory. Therefore, novel classes of non-nucleoside anti-HBV agents with different antiviral targets and mechanisms are still needed. Natural products as the important sources of novel anti-HBV agents with potential anti-HBV activity have been attracted much more interest of scientists. This paper reviews natural products as anti-HBV agents reported so far.
Key words: Hepatitis B virus (HBV); natural products; non-nucleoside; anti-HBV agents


Antiviral agents from the Schisandraceae plants


Wen-Hui Ma and and Dao-Feng Chen*
Department of Pharmacognosy,
School of Pharmacy, Fudan University, Shanghai 201203, People's Republic of China

Schisandraceae family contains two genera, Schisandra and Kadsura. The fruits of Schisandra plants are usually used in Chinese folk medicine to treat hepatitis. Some lignans and triterpenes from the Kadsura and Schisandra plants were found to have significant anti-HIV and anti-HBV effects. In this paper, the antiviral agents from the Schisandraceae plants were summarized.        



Antiviral effect of Yin-Zhi-Ku extract against human and duck
hepatitis B virus replication

Haiyan Zhu1,2, Hai Huang1, Yuanyuan Zhang3, Hongshan Chen4, Bing Wang2, Guan Ye2,

Haolong Zhao2, Pei Zhou1* and Chenggang Huang2*
1Department of Biosynthetic Medicinal Chemistry, School of Pharmacy,

Fudan University, Shanghai 201203, PR China;
2Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences,

Chinese Academy of Sciences, Shanghai 201203, PR China
3Departmen of Microbiology and Microbial Engineering, School of Life Science,
Fudan University, Shanghai 200433, PR China
4Instite of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Beijing 100050, P R China


Yin-Zhi-Ku (YZK) decoction consisting of three extracts from Herba Artemisiae Scopariae, Fructus Gardeniae and Radix Sophorae Flavescentis have been widely used in therapy for liver diseases in China as a common combination remedy. The antiviral activities of YZK and its component extracts on hepatitis B virus (HBV) replication in HBV transfected 2.2.15 cell cultures and duck hepatitis B virus (DHBV) replicaiton in ducklings in vivo were investigated. The intracelluar HBV-DNA copies, hepatitis B s antigen (HBsAg) and hepatitis B e antigen (HBeAg) concentrations in cell culture medium were determined by SyBr green real-time PCR and ELISA methods. Serum DHBV-DNA in ducklings was detected by dot-blot hybridization. YZK complex appeared to down-regulate the secretion of HBsAg and HBeAg as well as the release of HBV DNA replications from HepG2 2.2.15 in a dose-dependent manner, and its in vitro antiviral effect was much stronger than three constituent extracts. The serum DHBV-DNA levels was inhibited significantly in DHBV infected ducklings with the treatment of YZK at dose of 137.6mg/kg bid for 10 days orally. The current investigation provides the scientific evidence for the clinical application of YZK as an antiviral agent.



Natural products with inhibitory effect against hepatitis C virus

Ming-Ming Liu, Yi-Nan Zhang, Lu Zhou* and De-Yong Ye*
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China.

More than 180 million people are infected with hepatitis C virus (HCV) and are at risk of developing liver cirrhosis and/or hepatocellular carcinoma, and the number of such sufferers also increases 3-4 million per year. Dramatic progress has been made in the development of novel antiviral drugs since the discovery of HCV in 1989. Up to date,  about 70 anti-HCV agents are in process of clinical trials. Some of them are natural products or natural product-derived candidates. Natural products could play an important role as sources for searching anti-HCV agents. In this review, 30 small-molecule natural products are summarized and discussed with chemical structure, natural origin, bioactivity and pharmacology.


Anti-HBV compounds from Houttuynia cordata "Thunb."

Yun Jiang, Yan Lu*, Hai Huang, Pei Zhou and Daofeng Chen
School of Pharmacy, Fudan University
826, Zhangheng Road, Shanghai, 201203, P.R.China


Chemical investigation on the EtOAc extract of Houttuynia cordata Thunb. led to the isolation of ten known compounds: aristolactam B (1), cepharadione B (2), vomifoliol (3), vanillin (4), quercetin (5), apigenin (6), p-hydroxybenzoic acid (7), 1,4-dimethoxy benzene (8), 2,5-dimethoxyresorcinol (9) and quercitrin (10). All the isolates were tested for their antiviral effect against hepatitis B virus (HBV) in vitro. Compounds 2, 6 and 8 showed significant anti-HBV activity with inhibitory potency against HBsAg secretion at 35.4%, 55.0% and 63.7%, and that against HBeAg secretion at 23.1%, 30.1% and 39.9%, respectively.


Antiviral effects of flavonoids against influenza virus in vitro

Wei Zhou 1#, Hai Huang 2, #Xunlong Shi2, Pei Zhou2,*and Daofeng Chen2
1Zhejiang Hisun Pharmaceutical Co., Ltd. Zhejiang, 318000, PR China;
 2School of Pharmacy, Fudan University, Shanghai 201203, P R China

Flavonoids are a kind of structurally diverse compounds and show multiple biological activities. In this study, the antiviral activities of different flavonoids against influenza virus in Madin-Daby canine kidney (MDCK) cells were evaluated using cytopathic effect (CPE) method. The results indicated that the investigated flavonoids showed antiviral potency under the maximal nontoxic concentration in the order: Apigenin (1) > hyperoside (2) > rutin (3) > luteolin (4) > puerarin (5), ellagic acid (6), quercetin (7), kaempferol (8), and silymarin (9). However, naringin (10), nobiletin (11), naringenin (12), and tangeretin (13) didn't show any inhibition activity.



A microRaman spectroscopic investigation of a Flemish painting from the late 15th Century

Troels Filtenborga and Ole Faurskov Nielsenb
aNational Gallery of Denmark, Sølvgade 48-50, 1307 Copenhagen, Denmark
bDepartment of Chemistry,
University of Copenhagen, Universitetsparken 5, DK-2100, Copenhagen, Denmark

A painting of the Virgin and Child at the National Gallery of Denmark was recently restored. The painting on panel was obviously executed in the Netherlands in the late 15th century, most probably by Dieric Bouts or a painter closely influenced by him. Infrared recording of the underdrawing with several corrections indicates the authentic nature of this work as opposed to a workshop copy. Two sites of the Virgin’s blue cloak and one site of the cloth in which the child is swept were investigated by Raman microscopy. Samples from the two blue sites showed that the pigment used was ultramarine derived from lapis lazuli. Both samples showed the presence of a band at 549 cm–1 characteristic of the S–3 radical anion. Light microscopy of cross sections from the blue paint showed the presence of two different layers of blue pigments. Only the upper one was present in the samples used for Raman spectroscopy. Judging from the colour and morphology of the lower layer, this consists of the blue pigment azurite. In the 15th century ultramarine was very expensive and was often underpainted by other, less costly pigments. The pigment used for the white scarf was lead white identified by a band at 1050 cm–1. In one of the blue samples a small amount of lead white was found, most likely used by the painter to create slightly different blue tones. The Raman spectra are consistent with the use of linseed oil as the binder, possibly in combination with egg yolk.