Babu B H, Jayram H N, Nair M G, Ajaikumar K B, Padikkala J
Amala Cancer Research Centre, Amala Nagar, Thrissur, India.
J Exp Clin Cancer Res. 2003 Dec;22(4):581-9.
Antioxidant, antitumor and anticarcinogenic activity of gossypin (3,5,8,3',4'-pentahydroxy-7-O glucosyl flavone) was carried out. The compound needed for 50% inhibition of superoxide, hydroxyl and nitric oxide radicals was 3 microg/ml, 41 microg/ml and 12 microg/ml, respectively. Gossypin also impart 50% inhibition at concentrations 37 microg/ml and 43 microg/ml, respectively for in vitro lipid peroxidation. The compound shows IC50 of 30 microM, 42.5 microM and 45.1 microM concentrations in L 929, HT 29 and K 562 cell lines in 72 hrs MTT assay. The compound shows a zone of inhibition of 8 mm in topo I and topo II inhibition assay in Saccharomyces ceriviseae mutant cultures. It reduces the tumor burden in solid tumor harboring animals (p < 0.001) and effectively inhibits the formation of new blood vessels on tumor mass. 20 mg/kg b.wt of gossypin increase the life span of ascites tumor harboring animals (100%) and (164.7%) respectively by oral and intraperitoneal administration of the drug. Gossypin reduced the incidence of papilloma formation and papilloma/mouse in DMBA/ croton oil induced skin papilloma.
对棉皮素（3,5,8,3',4'-五羟基-7-O-葡萄糖基黄酮）的抗氧化、抗肿瘤和抗癌活性进行了研究。对超氧阴离子、羟基自由基和一氧化氮自由基50%抑制所需的该化合物浓度分别为3微克/毫升、41微克/毫升和12微克/毫升。棉皮素对体外脂质过氧化在浓度分别为37微克/毫升和43微克/毫升时也有50%的抑制作用。在72小时MTT试验中，该化合物在L 929、HT 29和K 562细胞系中的IC50浓度分别为30微摩尔、42.5微摩尔和45.1微摩尔。在酿酒酵母突变体培养物的拓扑异构酶I和拓扑异构酶II抑制试验中，该化合物显示出8毫米的抑制圈。它可减轻荷实体瘤动物的肿瘤负担（p<0.001），并有效抑制肿瘤块上新血管的形成。20毫克/千克体重的棉皮素通过口服和腹腔给药分别使荷腹水瘤动物的寿命延长（100%）和（164.7%）。棉皮素降低了二甲基苯并蒽/巴豆油诱导的皮肤乳头状瘤中乳头状瘤的形成率和每只小鼠的乳头状瘤数量。
