Drug intelligence / Profile preview

kuguacin J

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Kuguacin J is a **triterpenoid compound** isolated from the leaves of *Momordica charantia* (bitter melon). It exhibits potent antineoplastic (anticancer) activity, most notably by **inhibiting growth of androgen-dependent prostate cancer cells via G1 cell cycle arrest and induction of apoptosis**. Mechanistically, it reduces cyclins D1 and E, CDKs, increases p21 and p27, modulates Bcl-2 family proteins, enhances cleavage of caspase-3 and PARP, downregulates the androgen receptor, and induces p53. Furthermore, kuguacin J is a **direct inhibitor of P-glycoprotein (P-gp/ABCB1) function at the drug-substrate binding site**, effectively reversing multidrug resistance in cancer cell lines by increasing intracellular accumulation of chemotherapeutic agents like vinblastine and paclitaxel. It does not affect P-gp expression. Kuguacin J is researched primarily in vitro and has not been approved as a pharmaceutical agent[4][7].

Other names
1141453-65-7(3S,7S,8S,9R,10R,13R,14S,17R)-3,7-dihydroxy-4,4,13,14-tetramethyl-17-[(2R,4E)-6-methylhepta-4,6-dien-2-yl]-2,3,7,8,10,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthrene-9-carbaldehyde
02

Targets

BCL-2 (BCL-2 family)CDK4 (Cyclin-dependent kinase 4)CDK2 (Cyclin-dependent kinase 2)ABCB1 (P-glycoprotein)AR (Adrenergic receptors)CDKN1A (Cyclin-dependent kinase inhibitor 1A)TP53 (Cellular Tumor Antigen p53 R175H)

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