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Anticarcinogenic and antioxidant activity of diindolylmethane derivatives

Acta Pharmacologica Sinica 2004年第5期25卷 124-129页

作者： Sakina Hayat BENABADJI Department of Medicinal Chemistry Medical Center of Fudan University

AIM: To investigate the synthesis methods and the bioactivity of diindolylmethane (DIM) derivatives. METHODS:1) A 3D-Quantitative Structure-Active Relationships (QSAR) Comparative Molecular Field Analysis (CoMFA) studyof 14 DIM derivatives was investigated to predict their anticarcinogenic activity. 2) Based on CoMFA model, aseries of new derivatives of DIM were designed and synthesized. 3) Their free radical scavenging and antioxidantpotentials were tested using in-vitro DPPH radical scavenging and b-carotene antioxidant models. 4) Theanticarcinogenic activities of some compounds were tested by using microculture tetrazolium assay (MTT) andsulforhodamine B (SRB) proteochromosomic assays. RESULTS: 1) The CoMFA model derived from DIM ana-logues proved a good predictive ability with q2 value of 0.827. 2) New designed compounds 3c and 4c exhibited3-fold more potent radical scavenging activity than reference substance Vitamin E in DPPH model expressed by IC50values. 3) The primary antitumor screening essay showed that some DIM derivatives designed exhibited theinhibitory activities to some tumor cell growth at relatively high concentration, and DIM was the most effectiveamong them. CONCLUSION: DIMs 3D-QSAR model is reliable. According to it, eleven DIM derivatives weresynthesized, and two derivatives of them possess potent radical scavenging activities and some showed the inhibi-tory activities in primary anticancer assay in vitro.

关键词： indole-3-carbinol diindolylmethane CoMFA analysis antioxidants free radical scavengers 1,1-DPPH carotenoids antitumor drug screening assay

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3D-QSAR Study on diindolylmethane and Its Analogues with Comparative Molecular Field Analysis (CoMFA)

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Chinese Journal of Chemistry 2003年第1期21卷 20-24页

作者： BENABADJI Sakin Hayat 陈海峰袁身刚闻韧 Key Laboratory of Computer Chemistry Shanghai Institute of Organic Chemistry Chinese Academy of Sciences Department of Medicinal Chemistry Medical Center of Fudan University

Comparative molecular field analysis (CoMFA), a three dimensional quantitative structure-activity relationship (3D-QSAR) method was applied to a series of diindolylmethane (DIM) analogs to study the relationship between their structure and their induction of CYP 1A1-associated ethoxyresorufin-O-deethylase (EROD) activity. A DISCO model of pharmacophore was derived to guide the superposition of the compounds. The coefficient of cross-validation (q 2) and non cross-validation (r 2) for the model established by the study are 0.827 and 0.988 respectively, the value of variance ratio (F) is 103.53 and standard error estimate (SEE) is 0.044. These values indicate that the CoMFA model derived is significant and might have a good prediction for the catalytic activity of DIM compounds. As a consequence, the predicted activity values of new designed compounds were all higher than that of the reported value.

关键词： D-QSAR CoMFA diindolylmethane CYP 1A1

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Predicting the physiological relevance of in vitro cancer preventive activities of phytochemicals

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Acta Pharmacologica Sinica 2007年第9期28卷 1274-1304页

作者： Lynne M HOWELLS Elena P MOISEEVA Christopher PNEAL Bethany EFOREMAN Catherine KANDREADI Yi-yang SUN E Ann HUDSON Margaret M MANSON Cancer Biomarkers and Prevention Group University of LeicesterLeicester LE1 7RHUK

There is growing interest in the ability of phytochemicals to prevent chronicdiseases,such as cancer and heart ***,some of these agents havepoor bioavailability and many of the in-depth studies into their mechanisms ofaction have been carried out in vitro using doses which are unachievable *** order to optimize the design of chemopreventive treatment,it is impor-tant to determine which of the many reported mechanisms of action are *** this review we consider the physiologically achievable doses for afew of the best studied agents (indole-3-carbinol,diindolylmethane,curcumin,epigallocatechin-3-gallate and resveratrol) and summarize the data derived fromstudies using these low concentrations in cell *** then cite examples of invitro effects which have been observed in ***,the ability of agentcombinations to act synergistically or antagonistically is *** con-clude that each of the compounds shows an encouraging range of activities invitro at concentrations which are likely to be physiologically *** arealso many examples of in vivo studies which validate in vitro *** consideration is that combinations of agents can result in significantactivity at concentrations where any single agent is ***,for each of thecompounds reviewed here,in vitro studies have provided useful insights intotheir mechanisms of action in ***,data are lacking on the full rangeof activities at low doses in vitro and the benefits or otherwise of combinations invivo.

关键词： bioavailability cancer chemoprevention curcumin diet diindolylmethane epigallo catechin-3-gallate indole-3-carbinolresveratrol

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Development and validation of a rapid UPLC/MS method for the simultaneous determination of I3C, DIM, and related metabolites and its application to pharmacokinetics studies

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Journal of Chinese Pharmaceutical Sciences 2016年第7期25卷 477-488页

作者： Yury Gomez Hu Wang Ah-Ng Tony Kong Graduate Program in Pharmaceutical Science Ernest Mario School of Pharmacy Rutgers The State University of New Jersey Department of Pharmaceutics Ernest Mario School of Pharmacy Rutgers The State University of New Jersey

Indole-3-carbinol(I3C) and diindolylmethane(DIM) are naturally derived dietary phytochemicals with promising anti-cancer properties that have been demonstrated both in vitro and in vivo. Using reversed-phase ultra-performance liquid chromatography(UPLC) coupled with mass spectrometry(MS), a rapid, specific, and high throughput method was developed and validated for the quantification and identification of I3 C, DIM, and other I3 C metabolites in plasma. Samples containing I3 C or DIM and the internal standard 4-methoxy indole(IS) were extracted using a liquid-liquid extraction technique. The mean recovery was 96.21% for I3 C and 108.5% for DIM. Separation was achieved using a Waters Acquity UPLC HSS T3, 1.8 μm, 2.1 mm×150 mm column and acetonitrile–water gradient elution. The flow rate was 0.3 m L/min and the run time was 9 min. The limits of detection and quantification for I3 C and DIM were 15 ng/m L and 25 ng/m L, respectively. Calibration curves for I3 C and DIM were linear(r2>0.99) over a concentration range of 0.025–20 μg/m L. Precision, accuracy, and stability analysis fulfilled the CDER guidelines criteria. The method was successfully applied to the determination of the pharmacokinetic parameters of I3 C or DIM after oral, intravenous, or intraperitoneal administration to Sprague Dawley rats. The method described here is superior over existing analytical methods for I3 C and its metabolites in terms of sensitivity, speed, and separation.

关键词： UPLC/MS Indole-3-Carbinol diindolylmethane Pharmacokinetics Single-dose administration Sprague-Dawley Rats

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