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.