OBJECTIVE: High‑density lipoprotein (HDL) cholesterol‑mediated atherosclerotic plaque regression
has gained wide therapeutic attention. The whole plant methanolic extract of the medicinal plant
Desmodium gyrans Methanolic Extract (DGM) has shown to mitigate hyperlipidemia in high
fat‑ and‑cholesterol fed rats and rabbits with significant HDL enhancing property. The study aimed
to assess the functionality and mechanistic basis of HDL promoting effect of DGM.
MATERIALS AND METHODS: Macrophage cholesterol efflux and foam cell formation assays
were performed in THP‑1 macrophages. Male Wistar rats were given DGM extract over 1 month
and assessed the serum HDL, Apolipoprotein A1 (Apo‑A1), and paraoxonase activity. Quantitative
Polymerase chain reaction was carried out to assess the expression level of Apo‑A1, SR‑B1 (Scavenger
receptor B1), and Cholesteryl ester transfer protein (CETP) on cDNA of HepG2 cells exposed to DGM.
RESULTS: Pretreatment of DGM inhibited uptake of oxidized lipids and enhanced the lipid efflux
by THP‑1‑derived macrophages. Oral administration of DGM (100 and 250 mg/kg) progressively
enhanced the serum HDL, Apo‑A1 level, and associated paraoxonase activity in normal male Wistar
rats. In support to this, DGM exposed HepG2 cells documented dose‑dependent increase in the
expression of SR‑B1 and Apo‑A1 mRNA, while reduced the CETP expression.
CONCLUSION: Overall the results indicated that DGM modulates lipid trafficking and possesses
functional HDL enhancing potential through increased Apo‑A1 levels and paraoxonase activity.
Further, reduced CETP expression and increased expression of SR‑B1 suggest the reverse
cholesterol transport promoting role of DGM.