Bhatti Rajbir, Singh J, Saxena A K, Suri Nitasha, Ishar M P S
Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar-143 005, India.
Departments of Pharmacology, Government Medical College, Amritsar-143 001, India.
Indian J Pharm Sci. 2013 Nov;75(6):628-34.
Therapeutic management of cancer is a great clinical challenge and alternative medicines are being extensively explored to have integrated approach to cure cancer. Aegle marmelos (L.) Correa (Rutaceae) is known for its hypoglycaemic, radioprotective, antidiarrhoeal and many other pharmacological activities. The present study is designed to carryout pharmacognostic standardisation and evaluation of antiproliferative activity of the leaf extracts Aegle marmelos (L.) Correa (Rutaceae) and the chromatographic fractions of the most active extract. Hexane, petroleum ether, chloroform and ethanol extracts of the shade dried leaves were prepared by soxhelation and antiproliferative activity was assessed using human cancer cell lines of lung (A-549), colon (CoLo-05), ovary (IGR-OV-1), prostrate (PC3), leukaemia (THP-1) and breast (MCF-7) cancer. Bioactivity-derived fractionation was carried out for most active extract by column chromatography. The phytochemical studies indicated alkaloids, anthraquinones, terpenoids in the alcohol, chloroform extracts and tannins, terpenoids, reducing sugars in the petroleum ether and hexane extracts. Ethanol extract showed maximum inhibition in colon and breast carcinoma cell lines at a dose of 100 μg/ml. Column chromatography of the ethanol extract yielded five fractions. Out of this, fractions 2, 4 and 5 showed significant inhibition in leukaemia cell line with IC50 of 12.5, 86.2 and >100 μg/ml for fractions 2, 4 and 5, respectively. High-performance thin layer chromatography of the fraction 2 revealed imperatorin as one of the major phytoconstituents. Among the different extracts investigated, ethanol extract exhibited significant antiproliferative activity and its fraction 2 containing furanocoumarin imperatorin showed antiproliferative activity against leukaemia cell line with IC50 of 12.5 μg/ml.
癌症的治疗管理是一项重大的临床挑战,人们正在广泛探索替代药物,以寻求治愈癌症的综合方法。印度枳椇(芸香科)因其降血糖、辐射防护、止泻等多种药理活性而闻名。本研究旨在对印度枳椇(芸香科)叶提取物及其最具活性提取物的色谱馏分进行生药学标准化和抗增殖活性评估。通过索氏提取法制备了阴干叶的己烷、石油醚、氯仿和乙醇提取物,并使用肺癌(A-549)、结肠癌(CoLo-05)、卵巢癌(IGR-OV-1)、前列腺癌(PC3)、白血病(THP-1)和乳腺癌(MCF-7)的人类癌细胞系评估抗增殖活性。对最具活性的提取物进行柱色谱法的生物活性导向分级分离。植物化学研究表明,乙醇、氯仿提取物中含有生物碱、蒽醌、萜类化合物,石油醚和己烷提取物中含有单宁、萜类化合物、还原糖。乙醇提取物在100μg/ml剂量下对结肠和乳腺癌细胞系显示出最大抑制作用。乙醇提取物的柱色谱法产生了五个馏分。其中,馏分2、4和5对白血病细胞系显示出显著抑制作用,馏分2、4和5的IC50分别为12.5、86.2和>100μg/ml。馏分2的高效薄层色谱显示欧前胡素是主要植物成分之一。在所研究的不同提取物中,乙醇提取物表现出显著的抗增殖活性,其含有呋喃香豆素欧前胡素的馏分2对白血病细胞系表现出抗增殖活性,IC50为12.5μg/ml。