Site-directed PEGylation of trichosanthin retained its anti-HIV activity with reduced potency in vitro

Wang, Jianhua; Tam, Siu-Cheung; Huang, Hai; Ouyang, Dong-Yun; Wang, Yuan‐Yuan; Zheng, Yong‐Tang

doi:10.1016/j.bbrc.2004.03.139

Cited by 100 publications

(59 citation statements)

References 23 publications

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“…Cytotoxicity was measured in parallel with the determination of antiviral activity, using azidothymidine (AZT) as a positive control. 10 The results are shown in Table 2, compounds 1-4 showed therapeutic index (TI) values of 58.65, 26.36, 23.71 and 25.85, respectively. The TI values of all compounds are higher than these of reported 7,8-secolignans, marphenol A, marphenol B and 7,8-secoholostylone B.…”

Section: Resultsmentioning

confidence: 97%

7,8-secolignans from Schisandra neglecta and their anti-HIV-1 activities

Mu¹,

Wang²,

Hu³

et al. 2012

J. Braz. Chem. Soc.

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Quatro novas 7,8-secoligninas (neglectahenols A-D), juntamente com duas 7,8-secolignanas conhecidas, foram isoladas de folhas e caules de Schisandra neglecta. As estruturas foram elucidadas por métodos espectroscópicos, incluindo a técnica de RMN (ressonância magnética nuclear) em uma e duas dimensões. As atividades anti-HIV-1 (vírus da imunodeficiência humana tipo 1) das 7,8-secoligninas e dos neglectahenols também foram testadas, e todos mostraram atividades moderadas. Four new 7,8-secolignans (neglectahenols A-D), together with two known 7,8-secolignans, were isolated from leaves and stems of Schisandra neglecta. The structures were elucidated by spectroscopic methods, including extensive one and two dimension NMR (nuclear magnetic resonance) techniques. 7,8-Secolignans and neglectahenols A-D were also tested for their anti-HIV-1 (human immunodeficiency virus type 1) activities, and all of them showed modest activities.

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Section: Resultsmentioning

confidence: 97%

7,8-secolignans from Schisandra neglecta and their anti-HIV-1 activities

Mu¹,

Wang²,

Hu³

et al. 2012

J. Braz. Chem. Soc.

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“…In Vitro Anti-HIV-1 Assays Compounds 1-20 were evaluated for their anti-HIV-1 activity by microtiter syncytium formation infectivity assay, using the method previously described, with 3Ј-azido-3Ј-deoxythymidine (AZT) as a positive control. 34,35) The assays included cytotoxicity (CC 50 ) in C8166 cell and inhibition (EC 50 ) of syncytium formation in HIV-1 IIIBinfected C8166 cell in vitro. The cytotoxicity was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method.…”

Section: Experimental General Methodsmentioning

confidence: 99%

Anti-human Immunodeficiency Virus-1 Constituents of the Bark of Poncirus trifoliata

Feng

Wang

Cai

et al. 2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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Poncirus trifoliata (L.) RAF., a 1-5 m tree in the family Rutaceae, is widely distributed in P. R. China.1) Its dried immature fruit has been traditionally used for uterine contraction and relaxation, and treating gastrointestinal and cardiovascular diseases.2) The crude extract also has reported for anti-inflammatory, anti-bacterial and anti-mucin releasing activities. [3][4][5] Previous study on the roots and fruits of this plant reported lots of coumarins, [6][7][8][9][10][11][12] flavonoids, 2) and nortriterpenoids. 13,14) However, the chemical constituent of the stem bark of this plant was seldom reported. As part of searching for novel and bioactive compounds, now we report the result of a phytochemical investigation on the stem bark of P. trifoliata. Results and DiscussionsThe chemical investigation on a MeOH extact of the stem bark of P. trfoliata led to the isolation of 36 compounds (1-36) including flavonoids, coumarins, triterpenoids, steroids, and lignans. Compounds 1-3 are new prenylated flavonoids which were elucidated as (Ϫ)-5, 4Ј-dihydroxy-7,8-[(3Љ,4Љ- limonin ( 4, 102.8, 104.7, 121.2, 155.8, 158.7, 160.3, 161.2, 163.8, 181.9) (Table 1). Of them, five carbon signals at d C 21.3 (q), 26.4 (q), 60.5 (d), 71.1 (d), and 79.4 (s) constructed a prenyl group on the basis of heteronuclear multiple bond correlation (HMBC) correlations (Fig. 1). Subsequently, a 2Љ,2Љ-dimethyldihydropyran moiety with hydroxy substitutes at C-3Љ and C-4Љ was established according to the 2D-NMR data and MS analysis (Fig. 1). In the 1 H-NMR spectrum (Table 1)

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“…However, through co-TLC with authentic sample using CHCl 3 -MeOH-H 2 O-HOAC (7 : 3 : 0.8 : 1) as developing system, glucose was detected in the water layer (Rfϭ0.49), which was further concentrated to dryness and subjected to silica gel chromatography eluting with Anti-HIV-1 Assay The anti-HIV activities and cytotoxicities were assessed by microtiter syncytium formation infectivity assay, using the method previously described, with AZT as a positive control. 31) …”

Section: Methodsmentioning

confidence: 99%