Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance inHepG2/Dox cells.

Abstract

Tenacissimoside A (1) and 11alpha-O-benzoyl-12beta- O-acetyltenacigenin B (2), two derivatives of tenacigenin B (3) from the plant Marsdenia tenacissima, reversed multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells. The sensitivity of HepG2/Dox cells to the antitumor drugs doxorubicin, vinblastine, puromycin, and paclitexel was increased by 18-, 10-, 11-, and 6-fold by 20 microg/mL (or 25 microM) of 1 and 16-, 53-, 16-, and 326-fold by 20 microg/mL (or 39 microM) of 2, respectively. A preliminary mechanistic study has suggested that 1 might modulate Pgp-mediated multidrug resistance through directly interacting with the Pgp substrate site.

• Authors: Ying-Jie Hu, Xiao-Ling Shen, Hong-Long Lu, Yu-Hu Zhang, Xin-An Huang, Lin-Chun Fu, Wang-Fun Fong
• Journal: Journal of natural products (J Nat Prod) Vol. 71 Issue 6 Pg. 1049-51 (Jun 2008) ISSN: 1520-6025 [Electronic] United States
• PMID: 18512984 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 11alpha-O-benzoyl-12beta-O-acetyltenacigenin B
• ATP Binding Cassette Transporter, Subfamily B, Member 1
• Antineoplastic Agents, Phytogenic
• Drugs, Chinese Herbal
• Multidrug Resistance-Associated Proteins
• Steroids
• tenacigenin B
• tenacissimoside A
• Puromycin
• Vinblastine
• Doxorubicin
• Paclitaxel

Topics

• ATP Binding Cassette Transporter, Subfamily B, Member 1 (metabolism)
• Antineoplastic Agents, Phytogenic (chemistry, isolation & purification, pharmacology)
• Cell Cycle (drug effects)
• Doxorubicin (pharmacology)
• Drug Resistance, Neoplasm (drug effects)
• Drug Screening Assays, Antitumor
• Drugs, Chinese Herbal (chemistry, isolation & purification, pharmacology)
• Humans
• Marsdenia (chemistry)
• Multidrug Resistance-Associated Proteins (metabolism)
• Paclitaxel (pharmacology)
• Plants, Medicinal (chemistry)
• Puromycin (pharmacology)
• Steroids (chemistry, isolation & purification, pharmacology)
• Vinblastine (pharmacology)