Therapeutic effects of purified polyphenols from Coccinia grandis: correlation between hypertension and diabetes mellitus

Inhibition of key enzymes is a good strategy to effectively control diabetes mellitus (DM), hypertension (HT) and cardiovascular diseases (CVDs). Very restricted reports are available for the enzyme inhibitory property of Coccinia grandis (Cg) immature fruits. In the above background, the present study aims to explore the α-amylase, invertase, cholesterol esterase (CEase) and angiotensin converting enzyme (ACE) inhibitory properties of Cg. Two dimensional preparative thin layer chromatography (2D PTLC) coupled high resolution liquid chromatography–mass spectrometry (HRLC–MS2) purified polyphenolic eluate was investigated for the enzyme inhibitory properties. Hot water extracts of Coccinia grandis (HWE-Cg) has showed strong inhibitory effect against α- amylase (97.17 ± 0.01%), invertase (97 ± 0.02%) and cholesterol esterase (83.6 ± 0.001%), and moderate activity against ACE (73.62 ± 0.001%) than organic solvent extracts (OSE-Cg). Microwave assisted process optimization has revealed a drastic reduction in time duration and material ratio, but no improvement in ACE inhibitory activity. Eight different polyphenols that includes hydroxyl ferulic acid (m/z 205), apigenin (m/z 277), isorhamnetin-O-sophoroside (m/z 640) and isoscutellarein-O-pentoside (m/z 415) were purified and predicted using 2D PTLC and HRLC-MS2 techniques, respectively. The eluate has established significant inhibitory effect against CEase (81.12 ± 0.10%) and amylase (62.28 ± 0.12%), than invertase (34.43 ± 0.11%) and ACE (20.12 ± 0.14%). Moreover, controlled drug release profile was recorded by HWE-Cg loaded calcium alginate beads and filled SS316L stainless steel bioimplant. Hence, Coccinia grandis can be used as traditional medicine to regulate DM, HT and CVDs.