Alanazi Abdullah I R, Abdallah Hossam M, Mohamed Hagar M, Ibrahim Sabrin R M, Alfaifi Mohammad Y, Elbehairi Serag Eldin I, Mohamed Gamal A
Department of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.
Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
J Pharm Bioallied Sci. 2025 Apr-Jun;17(2):56-60. doi: 10.4103/jpbs.jpbs_991_25. Epub 2025 Jul 23.
The pericarp of (mangosteen) has been used as a medicinal agent by Southeast Asians for centuries in the treatment of skin infections and wounds. Its main active constituents were xanthones and phenolic compounds. The plant and its metabolites possessed diverse bioactivities.
A methanolic extract of pericarp was subjected to solvent partitioning and chromatographic purification to isolate α-mangostin (1), β-mangostin (2), gartanin (3), garcinone C (4), garcinone D (5), and (+)-2R,3R-taxifolin-3-O-α-L-rhamnoside (astilbin) (6) that were identified by NMR spectral data, as well as comparing with literature data. These compounds were assessed for their cytotoxic effect against (SKOV-3), hepatic cell line (HepG-2), and colorectal cancer (HCT-116) cell lines using sulforhdamine B (SRB) assay. Doxorubicin was used as a positive control.
All compounds exhibited varying degrees of cytotoxic activity. Garcinone D demonstrated significant cytotoxic potential (IC 27.27 ± 2.41 µM) against SKOV-3 cells. While α-mangostin and β-mangostin exhibited cytotoxic activity (IC values of 28.1 ± 1.1 µM and 31.9 ± 10.7 µM, respectively) towards HepG-2 cells. Also, β-mangostin and garcinone D demonstrated cytotoxic effects with IC values of 56.1 ± 2.5 µM and 44.3 ± 2.5 µM, respectively against HCT-116.
The study highlights the cytotoxic potential of xanthones derived from pericarp. Among the isolated metabolites, garcinone D and α-mangostin emerged as promising lead compounds for further anticancer drug development due to their significant in vitro cytotoxic effects.
几个世纪以来，东南亚人一直将山竹果皮用作治疗皮肤感染和伤口的药物。其主要活性成分是氧杂蒽酮和酚类化合物。该植物及其代谢产物具有多种生物活性。
对山竹果皮的甲醇提取物进行溶剂分配和色谱纯化，以分离出通过核磁共振光谱数据鉴定并与文献数据比较的α-倒捻子素（1）、β-倒捻子素（2）、藤黄宁（3）、藤黄酮C（4）、藤黄酮D（5）和（+）-2R，3R-紫杉叶素-3-O-α-L-鼠李糖苷（落新妇苷）（6）。使用磺酰罗丹明B（SRB）测定法评估这些化合物对卵巢癌细胞系（SKOV-3）、肝癌细胞系（HepG-2）和结肠癌细胞系（HCT-116）的细胞毒性作用。阿霉素用作阳性对照。
所有化合物均表现出不同程度的细胞毒性活性。藤黄酮D对SKOV-3细胞显示出显著的细胞毒性潜力（IC 27.27±2.41μM）。而α-倒捻子素和β-倒捻子素对HepG-2细胞表现出细胞毒性活性（IC值分别为28.1±1.1μM和31.9±10.7μM）。此外，β-倒捻子素和藤黄酮D对HCT-116表现出细胞毒性作用，IC值分别为56.1±2.5μM和44.3±2.5μM。
该研究突出了山竹果皮中氧杂蒽酮的细胞毒性潜力。在分离出的代谢产物中，藤黄酮D和α-倒捻子素因其显著的体外细胞毒性作用而成为进一步抗癌药物开发的有前景的先导化合物。
