Kamal Yousaf, Fatima Nighat, Mumtaz Amara, Shahzadi Irum, Mannan Abdul, Anaya-Eugenio Gerardo D, Arellano Eric Daniel Salinas, Ahmed Madiha, Hussain Zahid, de Blanco Esperanza J Carcache
Department of Pharmacy, COMSATS University Islamabad, Abbottabad 22060, Pakistan.
Faculty of Pharmacy, Hamdard University, Islamabad 45550, Pakistan.
Curr Pharm Des. 2025;31(15):1239-1246. doi: 10.2174/0113816128299481240223054918.
This study aims to isolate and characterize potential cytotoxic compounds from the roots of Linn. (Caesalpiniaceae) and evaluate their activity against human cancer cell lines. Five compounds, namely β-sitosterol (1), piperine (2), piperolein B (3), retrofractamide A (4), and dehydropipernonaline (5), were isolated from roots using various chromatographic procedures.
The root extracts were prepared using aqueous and organic solvents, including n-hexane, ethyl acetate, and methanol. The isolated compounds were subjected to a sulforhodamine B cytotoxicity assay against DU-145 and PC-3 (prostate), HT-29 (colon), and MCF-7 (breast) human cancer cell lines. Among the isolates, compound 5 exhibited significant bioactivity against all tested cell lines. Compound 4 demonstrated activity, specifically against MCF-7 cancer cell lines.
Importantly, these compounds were identified for the first time from roots. In conclusion, this study highlights the enhanced spectrum of cytotoxic activity exhibited by the isolated compounds. These findings encourage further investigation to elucidate the mechanism of action of these compounds against the respective cell lines.
The identification and characterization of these bioactive compounds contribute to the understanding of the potential therapeutic applications of B. variegata in cancer treatment.
本研究旨在从(豆科)的根中分离并鉴定潜在的细胞毒性化合物,并评估它们对人癌细胞系的活性。使用各种色谱方法从根中分离出了五种化合物,即β-谷甾醇(1)、胡椒碱(2)、胡椒脂碱B(3)、反式断裂酰胺A(4)和脱氢胡椒碱(5)。
使用水和有机溶剂(包括正己烷、乙酸乙酯和甲醇)制备根提取物。对分离出的化合物进行了针对DU-145和PC-3(前列腺)、HT-29(结肠)和MCF-7(乳腺)人癌细胞系的磺酰罗丹明B细胞毒性测定。在这些分离物中,化合物5对所有测试的细胞系均表现出显著的生物活性。化合物4显示出活性,特别是对MCF-7癌细胞系。
重要的是,这些化合物首次从根中被鉴定出来。总之,本研究突出了分离出的化合物所表现出的增强的细胞毒性活性谱。这些发现鼓励进一步研究以阐明这些化合物对各自细胞系的作用机制。
这些生物活性化合物的鉴定和表征有助于理解变色豆梨在癌症治疗中的潜在治疗应用。