Proanthocyanidins isolated from the leaves of Ficus glomerata evaluated on the activities of rumen enzymes: in vitro and in silico studies.

Two new proanthocyanidins (2S:3S)-(-)-epicatechin-(4α→8)4-(2R:3R)-(+)-catechin (Compound 1) and (2R, 3R)-3-O-galloyl-(+)-catechin (4ß→8)3-(2R, 3R)-3-O-galloyl-(+)-catechin (Compound 2) were isolated from Ficus glomerata and characterized by ultraviolet spectroscopy (UV), proton nuclear magnetic resonance (1H NMR), 13C NMR, and heteronuclear multiple bond correlation . The bioactivity and drug scores of isolated compounds were predicted using OSIRIS property explorer applications with drug scores of 0.03 (compound 1) and 0.05 (compound 2). Predictive drug scores provided an indication of the compounds' potential to demonstrate desired biological effects. Furthermore, the newly discovered proanthocyanidins tended to interact with protein due to their chemical structure and molecular conformation. With the aim of maintaining this focus, compounds 1 and 2 were subjected to in vitro testing against ruminal enzymes to further explore their potential impact. Both compounds showed significant inhibition activities (p < 0.01) against glutamic oxaloacetic transaminase in both protozoa and bacterial fractions, with an effective concentration (EC50) of 12.30-18.20 mg/mL. The compounds also exhibited significant inhibition (p < 0.01) of ruminal glutamic pyruvic transaminase activity, with EC50 values ranging from 9.77 to 17.38 mg/mL. Furthermore, the inhibition was recorded in R-cellulase between EC50 values of 15.85 and 23.99 mg/mL by both compounds. Additionally, both compounds led to a decrease in protease activity with increasing incubation time and concentration. In conclusion, the results indicate that these novel proanthocyanidins hold the potential to significantly impact rumen enzyme biology. Furthermore, their promising effects suggest that they could be further explored for drug development and other important applications.

Analgesic activity of Eugenia jambolana leave constituent: a dikaempferol rhamnopyranoside from ethyl acetate soluble fraction.

CONTEXT: Eugenia jambolana Lam. (Myrtaceae) is a medicinal plant used in folk medicine for the treatment of diabetes, inflammation, and pain. OBJECTIVE: We investigated the antinociceptive effect of kaempferol-7-O-α-l-rhamnopyranoside]- 4'-O-4'-[kaempferol-7-O-α-l-rhamnopyranoside (EJ-01), isolated from the E. jambolana leaves. MATERIALS AND METHODS: EJ-01 (3, 10, and 30 mg kg(-1), orally) was assessed for peripheral (formalin-nociception and acetic acid-writhing) and central (hot plate and tail flick test) analgesic activity in mice and the in vitro anti-inflammatory activity (25, 50, and 100 µg mL(-1)) in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. RESULTS AND DISCUSSION: EJ-01 (10 and 30 mg kg(-1)) significantly inhibited mean writhing counts (37.74 and 36.83) in acetic acid writhing and paw licking time (55.16 and 45.66 s) in the late phase of the formalin test as compared with the respective control (60.66 and 104.33 s). EJ-01 did not show analgesic activity in central pain models. Significant reduction in the tumor necrosis factor (TNF)-α (295.48, 51.20, and 49.47 pg mL(-1)) and interleukin (IL)-1ß (59.38, 20.08, and 15.46 pg mL(-1)) levels were observed in EJ-01-treated medium (25, 50, and 100 µg mL(-1)) as compared with vehicle-treated control values (788.67 and 161.77 pg mL(-1)), respectively. Significant reduction in total nitrite plus nitrate (NOx) levels (70.80 nmol) was observed in the EJ-01-treated medium (100 µg mL(-1)) as compared with the vehicle-treated value (110.41 nmol). CONCLUSION: EJ-01 is a valuable analgesic constituent of E. jambolana leaves and this study supports the pharmacological basis for the use of this plant in traditional medicine for curing inflammatory pain.