Nooreen Zulfa, Singh Shilpi, Singh Dhananjay Kumar, Tandon Sudeep, Ahmad Ateeque, Luqman Suaib
Process Chemistry and Technology Department, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow 226015, Uttar Pradesh, India.
Molecular Bioprospection Department, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow 226015, Uttar Pradesh, India.
Biomed Pharmacother. 2017 May;89:366-375. doi: 10.1016/j.biopha.2017.02.040. Epub 2017 Feb 27.
Zanthoxylum armatum or Timoor has been used in different traditional system of medicine due to its aromatic properties and also in the treatment of cancer, diarrhea and cholera. In the present investigation, four chemically distinct compounds namely Tambulin (6), Prudomestin (7), Ombuin (8) and 3, 4, 5, 3', 4', 5'-hexahydroxydiphenyl ether (9) have been isolated and quantified from the fruits. To explore the biological activities, we have further studied the antiproliferative, antimicrobial and antioxidant efficacy. Tambulin which was also found in maximum amount (0.125%) in fruits revealed significant antiproliferative activity (IC 37.96±0.36 to 48.7±0.21μg/mL) against breast, liver, colon and skin cancer cell lines corroborated by resilient binding interaction with SDH (-6.76Kcal/mol) and inhibition constant (Ki: 11.02μM). Hexane and ethyl acetate fraction exhibited moderate antibacterial efficacy (MIC: 250-1000μg/mL) against selected pathogenic microbes while Ombuin displayed broad spectrum antibacterial effect with MIC ranges from 125 to 500μg/mL. Total phenolic content (5.27±0.06 to 46.12±0.40mg/g of gallic acid equivalents), total flavonoids content (6.05±0.24 to 14.46±0.73mg/g of quercetin equivalents), ferric reducing power (42.35±0.85 to 62.52±0.66mg/g of ferrous sulfate equivalents) and percent free radical scavenging activity (59.56±0.38 to 64.85±1.78) were also estimated. Our findings infer that Tambulin exhibited significant antiproliferative activity whereas Ombuin was found to display broad spectrum antibacterial activity which adds one more positive attribute to its traditional usage.
竹叶椒或蒂莫尔因其芳香特性而被用于不同的传统医学体系，还用于治疗癌症、腹泻和霍乱。在本研究中，从果实中分离并定量了四种化学性质不同的化合物，即坦布林（6）、普鲁多斯汀（7）、奥姆宾（8）和3,4,5,3',4',5'-六羟基二苯醚（9）。为了探索其生物活性，我们进一步研究了其抗增殖、抗菌和抗氧化功效。果实中含量最高（0.125%）的坦布林对乳腺癌、肝癌、结肠癌和皮肤癌细胞系显示出显著的抗增殖活性（IC 37.96±0.36至48.7±0.21μg/mL），与琥珀酸脱氢酶的强结合相互作用（-6.76千卡/摩尔）和抑制常数（Ki：11.02μM）证实了这一点。正己烷和乙酸乙酯馏分对选定的致病微生物表现出中等抗菌功效（MIC：250-1000μg/mL），而奥姆宾显示出广谱抗菌作用，MIC范围为125至500μg/mL。还测定了总酚含量（5.27±0.06至46.12±0.40mg/g没食子酸当量）、总黄酮含量（6.05±0.24至14.46±0.73mg/g槲皮素当量）、铁还原能力（42.35±0.85至62.52±0.66mg/g硫酸亚铁当量）和自由基清除活性百分比（59.56±0.38至64.85±1.78）。我们的研究结果表明，坦布林表现出显著的抗增殖活性，而奥姆宾显示出广谱抗菌活性，这为其传统用途增添了又一个积极特性。
