Natural Compound 3β,7β,25-trihydroxycucurbita-5,23(E)-dien-19-al from <i>Momordica charantia</i> Acts as PPARγ Ligand

• Main Authors: Nur Adelina Ahmad Noruddin, Mohamad Faiz Hamzah, Zulfadli Rosman, Nurul Hanim Salin, Alexander Chong Shu-Chien, Tengku Sifzizul Tengku Muhammad
• Format: Article
• Language: English
• Published: MDPI AG 2021-05-01
• Series: Molecules
• Subjects: PPAR gamma; type 2 diabetes; natural product; <i>Momordica charantia</i>
• Online Access: https://www.mdpi.com/1420-3049/26/9/2682

<i>Momordica charantia</i> is a popular vegetable associated with effective complementary and alternative diabetes management in some parts of the world. However, the molecular mechanism is less commonly investigated. In this study, we investigated the association between a major cucurbitane triterpenoid isolated from <i>M. charantia</i>, 3β,7β,25-trihydroxycucurbita-5,23(E)-dien-19-al (THCB) and peroxisome proliferator activated receptor gamma (PPARγ) activation and its related activities using cell culture and molecular biology techniques. In this study, we report on both <i>M. charantia</i> fruit crude extract and THCB in driving the luciferase activity of Peroxisome Proliferator Response Element, associated with PPARγ activation. Other than that, THCB also induced adipocyte differentiation at far less intensity as compared to the full agonist rosiglitazone. In conjunction, THCB treatment on adipocytes also resulted in upregulation of PPAR gamma target genes expression; AP2, adiponectin, LPL and CD34 at a lower magnitude compared to rosiglitazone’s induction. THCB also induced glucose uptake into muscle cells and the mechanism is via Glut4 translocation to the cell membrane. In conclusion, THCB acts as one of the many components in <i>M. charantia</i> to induce hypoglycaemic effect by acting as PPARγ ligand and inducing glucose uptake activity in the muscles by means of Glut4 translocation.