Isogarcinol

Isogarcinol is a polyprenylated benzophenone natural compound extracted from plants of the Garciniagenus. Isogarcinol is also an effective inhibitor of acetylcholinesterase (AChE; IC₅₀=1.13μM) and butyrylcholinesterase (BChE; IC₅₀=8.30μM)^[1-2]. Isogarcinol exhibits not only antileishmanial activity but also anticancer and immunomodulatory activities^[3-4].

In vitro, breast cancer cell lines MDA-MB-231, MCF-7, T47D, and BT-549 were treated with Isogarcinol (1-17μM). Isogarcinol significantly inhibited cell viability, proliferation, invasion, and migration, while promoting apoptosis^[5]. Human promyelocytic leukemia cells (HL-60 cells) were treated with Isogarcinol (5–20μg/mL) for 24–48 hours. Isogarcinol significantly inhibited cell proliferation and induced apoptosis, accompanied by G2/M phase cell cycle arrest^[6].

In vivo, BALB/c mice were orally administered Isogarcinol (40–100mg/kg) daily for 6 days. Isogarcinol significantly suppressed 2,4-dinitrofluorobenzene (DNFB)-induced delayed-type hypersensitivity (DTH), alleviated ear swelling, and reduced the thymic index^[7]. Chronic graft-versus-host disease (cGVHD) model BDF1 mice were orally administered Isogarcinol (30–60mg/kg) daily for 10 weeks. Isogarcinol significantly reduced proteinuria levels, improved renal histopathological damage, and corrected abnormal serum levels of blood urea nitrogen, creatinine, triglycerides, and cholesterol^[8].

References:
[1] Schobert R, Biersack B. Chemical and Biological Aspects of Garcinol and Isogarcinol: Recent Developments. Chem Biodivers. 2019 Sep;16(9):e1900366.
[2] Lenta BN, Vonthron-Sénécheau C, Weniger B, et al. Leishmanicidal and cholinesterase inhibiting activities of phenolic compounds from Allanblackia monticola and Symphonia globulifera. Molecules. 2007 Jul 20;12(8):1548-57.
[3] Chen S, Han K, Li H, et al. Isogarcinol Extracted from Garcinia mangostana L. Ameliorates Imiquimod-Induced Psoriasis-like Skin Lesions in Mice. J Agric Food Chem. 2017 Feb 1;65(4):846-857.
[4] Matsumoto K, Akao Y, Kobayashi E, et al. Cytotoxic benzophenone derivatives from Garcinia species display a strong apoptosis-inducing effect against human leukemia cell lines. Biol Pharm Bull. 2003 Apr;26(4):569-71.
[5] Zhang D, Chu Y, Li M, et al. Isogarcinol Reduces MARS Levels and Deactivates the PI3K/AKT Pathway to Suppress the Malignant Properties of Breast Cancer Cells. Cell Biochem Biophys. 2025 Sep;83(3):3437-3449.
[6] Pieme CA, Ambassa P, Yankep E, et al. Epigarcinol and isogarcinol isolated from the root of Garcinia ovalifolia induce apoptosis of human promyelocytic leukemia (HL-60 cells). BMC Res Notes. 2015 Nov 23;8:700.
[7] Cen J, Shi M, Yang Y, et al. Isogarcinol is a new immunosuppressant. PLoS One. 2013 Jun 13;8(6):e66503.
[8] Li W, Li H, Zhang M, et al. Isogarcinol Extracted from Garcinia mangostana L. Ameliorates Systemic Lupus Erythematosus-like Disease in a Murine Model. J Agric Food Chem. 2015 Sep 30;63(38):8452-9.

Isogarcinol是一种从藤黄属植物中提取的多异戊烯基取代的苯甲酮类天然化合物，Isogarcinol还是有效的乙酰胆碱酯酶（AChE；IC₅₀=1.13μM）和丁酰胆碱酯酶（BChE；IC₅₀=8.30μM）抑制剂^[1-2]。Isogarcinol不仅具有抑制利什曼原虫活性，还具有抑制癌症、调节免疫反应的活性^[3-4]。

在体外，Isogarcinol (1-17μM) 处理乳腺癌细胞系 MDA-MB-231、MCF-7、T47D和BT-549。Isogarcinol显著抑制细胞的活力、增殖、侵袭和迁移能力，同时促进细胞凋亡^[5]。Isogarcinol（5–20μg/mL）处理人早幼粒白血病细胞（HL-60细胞）24–48小时。Isogarcinol显著抑制细胞增殖并诱导细胞凋亡，同时引起G2/M期细胞周期阻滞^[6]。

在体内，Isogarcinol（40–100mg/kg）每日口服给药BALB/c小鼠6天。Isogarcinol显著抑制2,4-二硝基氟苯（DNFB）诱导的迟发型超敏反应（DTH），减轻耳肿胀并降低胸腺指数^[7]。Isogarcinol（30–60mg/kg）每日口服给药慢性移植物抗宿主病（cGVHD）模型BDF1小鼠10周。Isogarcinol显著降低蛋白尿水平并改善肾脏组织病理学损伤，同时纠正血清尿素氮、肌酐、甘油三酯和胆固醇的异常升高^[8]。