Drug intelligence / Profile preview

glaucocalyxin B

Development stage
Preclinical
Modality
Small Molecules
Administration
Experimental (in Vitro, Animal Models: Oral, Intraperitoneal, Injection In Preclinical Studies)
01

Overview

**Glaucocalyxin B** is a naturally occurring ent-kaurane diterpenoid isolated primarily from the plant *Rabdosia japonica*. It exhibits significant bioactivity in a range of preclinical models, notably as an anti-inflammatory, anti-oxidative, and antitumor agent. Mechanistically, glaucocalyxin B acts as a small molecule modulator of multiple cellular pathways: - Inhibits activation of the NF-κB signaling pathway by targeting its p65 subunit, thus reducing pro-inflammatory cytokine expression and the M1 polarization of macrophages[3][1]. - In models of diabetic cardiomyopathy and rheumatoid arthritis, it ameliorates inflammation and oxidative stress through modulation of the NF-κB/NLRP3 and Nrf2/heme oxygenase-1 (HO-1) pathways[1][7]. - In cancer cells, it induces apoptosis and autophagy—mediated via increased reactive oxygen species (ROS), inhibition of the PI3K/Akt pathway, and increased PTEN activity[4][5][6]. - It also enhances sensitivity to chemotherapy agents such as cisplatin in ovarian cancer cells[6]. There is no evidence that glaucocalyxin B is approved for pharmaceutical use; current reports reflect preclinical research or experimental applications.

Other names
80508-81-2[(1R,2R,4S,9R,10S,13S,16R)-2-hydroxy-5,5,9-trimethyl-14-methylidene-6,15-dioxo-16-tetracyclo[11.2.1.01,10.04,9]hexadecanyl] acetatekaur-16-ene-3,15-dione 14-(acetyloxy)-7-hydroxy- (7alpha,14R)ent-kaurane diterpenoidGLB
02

Targets

RELA (Nuclear Factor Kappa B Subunit p65)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)AKT (RAC-alpha serine/threonine-protein kinase)

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