Antiproliferative activity of Rhinacanthus nasutus (L.) kurz extracts and the active moiety, rhinacanthin C
Antiproliferative activity of Rhinacanthus nasutus (L.) kurz extracts and the active moiety, rhinacanthin C
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DOI：
10.1248/bpb.27.1070
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发表时间：
2004-07-01
影响因子：
2
通讯作者：
Okumura, K
中科院分区：
文献类型：
--
作者：
Gotoh, A;Sakaeda, T;Okumura, K
鼻刺花Rhinacanthus nasutus（L.）苦豆属（菊科）灌木，广泛分布于中国南方和印度。本研究采用体外抗肿瘤实验方法，对毛茛根乙醇提取物和毛茛叶水提取物的抗肿瘤活性进行了研究。使用人宫颈癌细胞系HeLa、其MDR 1过表达亚系Hvr 100 - 6、人前列腺癌PC-3细胞和人膀胱癌T24细胞在体外评估了推测的活性部分紫藤素C。采用化学方法合成了菊红素C，并测定了其在红毛菊中的含量。采用高效液相色谱法，以光电二极管阵列检测器测定鼻屎提取物的含量。R.还使用携带肉瘤180的小鼠在体内评估了鼻疽提取物。结果表明：1）紫茎泽兰素C的体外抗增殖活性与5-FU相当或略弱于5-FU; 2）紫茎泽兰素C对MDR1过表达的Hvr 100 - 6细胞具有与亲本HeLa细胞相似的抗增殖活性; nasutus是由于紫茎泽兰素C，而R. nasutus是由非紫茎泽兰素C的成分引起的;口服给药14 d后，鼻屎提取物显示出体内抗增殖活性。
Rhinacanthus nasutus (L.) KURZ (Acanthaceae) is a shrub widely distributed in South China and India. In this study, the antiproliferative activity of the ethanol extract of root and aqueous extract of leaves of R. nasutus, and the supposed active moiety rhinacanthin C was assessed in vitro using the human cervical carcinoma cell line HeLa, its MDR1-overexpressing subline Hvr100-6, human prostate carcinoma PC-3 cells and human bladder carcinoma T24 cells. Rhinacanthin C was chemically synthesized and its content in the R. nasutus extracts was determined by HPLC with a photodiode array detector. The antiproliferative activity of the R. nasutus extracts was also assessed in vivo using sarcoma 180-bearing mice. It was suggested that 1) the in vitro antiproliferative activity of rhinacanthin C was comparable with or slightly weaker than that of 5-FU, 2) rhinacanthin C showed antiproliferative activity for MDR1-overexpressing Hvr100-6 cells, similarly to parent HeLa cells, 3) the in vitro antiproliferative activity of the ethanol extract of root R. nasutus was due to rhinacanthin C, whereas that of the aqueous extract of leaves of R. nasutus was due to constituents other than rhinacanthin C, and 4) both of the R. nasutus extracts showed in vivo antiproliferative activity after oral administration once daily for 14 d.