ABSTRACT
Psychotria densinervia hydro-ethanolic leaf extract (PHELE) and bark extract (PHEBE) were evaluated for antioxidant, anti-inflammatory, and inhibition of digestive enzymes activities. The antioxidant activity was characterized by 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), total phenolic content (TPC), and total flavonoid content (TFC) assays. The anti-inflammatory activity was characterized by protein denaturation and antiproteinase tests, while the inhibition of the enzymes was assessed using α-amylase, α-glucosidase, lipase, and cholesterol esterase activities. PHELE presented low (p < 0.001) IC50 (59.09 ± 5.97 µg/ml) for DPPH compared with ascorbic acid (71.78 ± 6.37 µg/ml) and PHEBE (115.40 ± 1.21 µg/ml). The IC50 of PHELE (262.4 ± 4.46 µg/ml) and PHEBE (354.2 ± 1.97 µg/ml) was higher (p < 0.001) than that of catechin (33.48 ± 2.02 µg/ml) for ABTS. PHELE had high (p < 0.001) FRAP (341.73 ± 21.70 mg CE/g) than PHEBE (150.30 ± 0.32 mg CE/g). PHELE presented (p < 0.001) high TPC (270.05 ± 7.53 mg CE/g) and TFC (23.43 ± 0.032 mg CE/g) than PHEBE (TPC: 138.89 ± 0.91 and TFC: 20.06 ± 0.032 mg CE/g). PHELE showed antiprotein denaturation with IC50 (257.0 ± 7.51 µg/ml) (p < 0.001) and antiproteinase activity (74.37 ± 1.10 µg/ml) lower than PHEBE (316.1 ± 6.02 µg/ml and 177.6 ± 0.50 µg/ml), respectively. Orlistat inhibited lipase (p < 0.001) activity with IC50 (37.11 ± 4.39 µg/ml) lower than PHELE and PHEBE (50.57 ± 2.89 µg/ml and 62.88 ± 1.74 µg/ml, respectively). PHELE inhibited cholesterol esterase with IC50 (34.75 ± 3.87 µg/ml) lower than orlistat (54.61 ± 2.56) and PHEBE (80.14 ± 1.71 µg/ml). PHELE inhibited α-amylase IC50 (6.07 ± 4.05 µg/ml) lower than PHEBE (19.69 ± 6.27 µg/ml) and acarbose (20.01 ± 2.84 µg/ml). Acarbose inhibited α-glucosidase (p < 0.001) activity with IC50 (4.11 ± 3.47 µg/ml) lower than PHELE (24.41 ± 2.84 µg/ml) and PHEBE (38.81 ± 2.46 µg/ml). PHELE presented better antioxidant, anti-inflammatory, and enzyme inhibition activity than PHEBE.
ABSTRACT
OBJECTIVE: The present study investigated the effect of the leaves extracts and fractions of Plectranthus glandulosus on the inhibition of pancreatic lipase, cholesterol esterase, adipocytes lipid uptake, and antithrombotic activity which may be important in atherosclerosis development. METHODS: Aqueous, ethanolic, and hydroethanolic extracts of Plactranthus glandulosus were prepared by maceration. The hydroethanolic extract was fractionated into n-hexane, ethylacetate, and n-butanol fractions and their inhibition of pancreatic lipase, cholesterol esterase, adipocytes lipid uptake, and antithrombotic activities measured. Liquid chromatography-high resolution mass spectrometry (LC-HRMS) analysis was carried out to determine phytochemical constituents present in the extracts. RESULTS: The standard orlistat exhibited a higher inhibitory activity on pancreatic lipase and cholesterol esterase (16.31 µg/mL and 15.75 µg/mL, respectively) compared to ethyl acetate fraction (IC50, 17.70 µg/mL and IC50, 24.8 µg/mL, respectively). Among crude extract, hydroethanolic extract showed a better inhibition against pancreatic lipase (IC50, 21.06 µg/mL) and cholesterol esterase (IC50, 25.14 µg/mL) though not comparable to the effect of orlistat. The best lipid uptake inhibition was observed in the hydroethanolic extract (IC50, 45.42 µg/mL) followed by the ethyl acetate fraction (IC50, 47.77 µg/mL). A better antithrombolytic activity was exhibited by the ethyl acetate fraction at all concentrations (50-800 µ/mL), while hydroethanolic extract exhibited the best activity among crude extract. However, these were not comparable to the standard aspirin. The LC-HRMS analysis revealed the presence of 7-O-methyl luteolin 5-O-ß-D-glucopyranoside, chrysoeriol 5-O-ß-D-glucopyranoside, 5,7-dihydroxy-3,2',4'-trimethoxyflavone, and plectranmicin as major compounds in both hydroethanolic extract and ethyl acetate fraction. CONCLUSION: Thus, our finding supports the traditional use of this plant, which might provide a potential source for future antiatherosclerotic drug discovery.
