α-Mangostin is a natural xanthone compound extracted from the peel of Garcinia mangostana and exhibits a wide range of biological activities[1-2]. α-Mangostin exerts anti-inflammatory effects by downregulating the NF-κB pathway, while also displaying antioxidant activity through scavenging free radicals and inhibiting ROS generation. α-Mangostin can be used in research related to cancer, antibacterial, and antiviral studies[3-4].
In vitro, treatment of MCF-7 human breast cancer cells with α-Mangostin (10–30μM) for 12–48 hours, α-Mangostin significantly upregulates MOAP-1 protein expression and promotes its interaction with activated BAX, inducing BAX oligomerization, mitochondrial cytochrome C release, and caspase activation, while downregulating BCL-XL protein levels, ultimately leading to apoptosis[5]. In HUAEC vascular endothelial cells treated with α-Mangostin (10μM) for 24 hours, α-Mangostin inhibits KDR tyrosine kinase and its phosphorylation at the Y1175 site, and suppresses cell proliferation, migration, and tube formation[6].
In vivo, in an angiotensin II-induced hypertensive C57BL/6 mouse model treated with α-Mangostin (4-8mg/kg; administered twice daily via oral gavage for 2 weeks), α-Mangostin significantly reduced systolic blood pressure, improved endothelium-dependent vasodilation, reversed aortic wall thickening and collagen deposition, downregulated aortic ACE/AT1R expression, and upregulated the ACE2/Ang-(1-7)/MasR axis activity [7]. In A375 and B16F10 cell-transplanted nude and C57BL/6 mouse melanoma models treated with α-Mangostin (10mg/kg; intraperitoneal injection every 2 days starting from day 7 after implantation), α-Mangostin significantly inhibited tumor growth and enhanced the chemotherapeutic efficacy of Cisplatin (3mg/kg)[8].
References:
[1] Majdalawieh AF, Khatib BK, Terro TM. α-Mangostin Is a Xanthone Derivative from Mangosteen with Potent Immunomodulatory and Anti-Inflammatory Properties. Biomolecules. 2025 May 7;15(5):681.
[2] Chavan T, Muth A. The diverse bioactivity of α-mangostin and its therapeutic implications. Future Med Chem. 2021 Oct;13(19):1679-1694.
[3] Liu X, Song M, Liu Y, et al. Rational Design of Natural Xanthones Against Gram-negative Bacteria. Adv Sci (Weinh). 2025 Apr;12(14):e2411923.
[4] Majdalawieh AF, Terro TM, Ahari SH, et al. α-Mangostin: A Xanthone Derivative in Mangosteen with Potent Anti-Cancer Properties. Biomolecules. 2024 Oct 30;14(11):1382.
[5] Simon SE, Lim HS, Jayakumar FA, et al. Alpha-Mangostin Activates MOAP-1 Tumor Suppressor and Mitochondrial Signaling in MCF-7 Human Breast Cancer Cells. Evid Based Complement Alternat Med. 2022 Jan 17;2022:7548191.
[6] Shiozaki T, Fukai M, Hermawati E, et al. Anti-angiogenic effect of α-mangostin. J Nat Med. 2013 Jan;67(1):202-6.
[7] Xue QQ, Liu CH, Zhang DY, et al. α-Mangostin Attenuates Blood Pressure and Reverses Vascular Remodeling by Balancing ACE/AT1R and ACE2/Ang-(1-7)/MasR Axes in Ang II-Infused Hypertensive Mice. Phytother Res. 2024 Dec;38(12):5918-5929.
[8] Xie Y, Gong C, Xia Y, et al. α-Mangostin Suppresses Melanoma Growth, Migration, and Invasion and Potentiates the Anti-tumor Effect of Chemotherapy. Int J Med Sci. 2023 Aug 6;20(9):1220-1234.
α-Mangostin是一种在Garcinia mangostana果皮中提取的天然氧杂蒽酮类化合物，具有广泛的生物活性[1-2]。α-Mangostin通过下调NF-κB通路发挥抗炎作用，同时通过清除自由基和抑制ROS生成以发挥抗氧化活性，α-Mangostin可用于癌症和抗菌抗病毒的相关研究[3-4]。
在体外，α-Mangostin（10–30μM）处理MCF-7人乳腺癌细胞12-48小时，α-Mangostin可显著上调MOAP-1蛋白表达并促进其与活化BAX的相互作用，诱导BAX寡聚化、线粒体细胞色素C释放及caspase激活，同时下调BCL-XL蛋白水平，最终导致细胞凋亡[5]。α-Mangostin（10μM）处理HUAEC血管内皮细胞24小时，α-Mangostin能抑制KDR酪氨酸激酶及其Y1175位点的磷酸化，并抑制细胞增殖、迁移及管腔形成[6]。
在体内，α-Mangostin（4-8mg/kg；每日两次灌胃给药，持续2周）处理Ang II诱导的高血压C57BL/6小鼠模型。α-Mangostin显著降低收缩压，改善内皮依赖性血管舒张功能，逆转主动脉壁增厚和胶原沉积，并下调主动脉中ACE/AT1R表达、上调ACE2/Ang-(1-7)/MasR轴活性[7]。α-Mangostin（10mg/kg；每2天腹腔注射一次，从接种后第7天开始）处理A375和B16F10细胞移植的裸鼠和C57BL/6小鼠黑色素瘤模型，α-Mangostin显著抑制肿瘤生长，并增强顺铂（3mg/kg）的化疗效果 [8]。