Human phospholipase A2 group IIa (sPLA2IIa) is an inflammatory enzyme that plays a significant role in tumorigenesis. Inhibiting the sPLA2IIa enzyme with an effective molecule can reduce the inflammatory response and halt cancer progression. The present study evaluates quercitrin, a biflavonoid, for sPLA2IIa inhibition and anticancer activity. Quercitrin inhibited sPLA2IIa activity to a greater extent—at 86.24% ± 1.41 with an IC50 value of 8.77 μM ± 0.9. The nature of sPLA2IIa inhibition was evaluated by increasing calcium concentration from 2.5 to 15 µM and substrate from 20 to 120 nM, which did not alter the level of inhibition. Intrinsic fluorescence and far UV-CD studies confirmed the direct interaction of quercitrin with the sPLA2IIa enzyme. This significantly reduced the sPLA2IIa-induced hemolytic activity and mouse paw edema from 97.32% ± 1.23–16.91% ± 2.03 and 172.87% ± 1.9–118.41% ± 2.53, respectively. As an anticancer activity, quercitrin reduced PC-3 cell viability from 98.66% ± 2.51–18.3% ± 1.52 and significantly decreased the IL-6 level in a dose-dependent manner from 98.35% ± 2.2–37.12% ± 2.4. It increased the mean survival time (MST) of EAC-bearing Swiss albino mice from 30 to 35 days. It obeyed Lipinski’s rule of five, suggesting a druggable property. Thus, all the above experimental results were promising and encouraged further investigation into developing quercitrin as a therapeutic drug for both inflammatory diseases and cancers.

Introduction and Aim: Garcinia indica is a wild edible fruit plant distributed in tropical regions of India. Fruits of G. indica were traditionally used to treat chronic inflammatory diseases like rheumatoid arthritis, gastrointestinal disorders, etc., But the basis of anti-inflammatory function of the fruit is not understood. Therefore, this study aims to evaluate the anti-inflammatory function of G. indica. Initially phytochemical screening of G. indica was carried out, tested antioxidant potency of G. indica fruit and evaluated its anti-inflammatory function by inhibition of secretory phospholipase A2 IIA (sPLA2IIA) enzyme. Methodology: The Soxhlet extraction method was used for the preparation of extracts of G. indica fruit. DPPH and phosphomolybdenum assays were carried out to estimate the antioxidant activities of G. indica fruit. The inhibition of sPLA2IIA, modulating indirect hemolytic and edema inducing activity and protein denaturation assays were done to evaluate the anti-inflammatory function. Results: Aqueous and solvent extracts of G. indica fruit showed a wide variety of phytochemicals. The ethanol extract of G. indica fruit showed greater antioxidant activity (79.12 % ±1.2) and reduction power (68.14% ± 4.4). The extract showed sPLA2IIA inhibition to a greater extent (50%), neutralized sPLA2IIA induced indirect hemolysis (IC50 45.518 µg/mL) and mouse paw edema (119.35% ± 2.74) with the IC50 value of 45.12 ±1.36µg. Conclusion: The extracts of G. indica contain a wide variety of phytochemicals. The ethanol extract of G. indica fruit exhibited a greater antioxidant activity and anti-inflammatory activity. Thus, the results defended the traditional usage of the G. indica fruit in the indigenous system of medicine.

Melastoma malabathricum is a medicinal plant found throughout Southeast Asian countries. Traditionally M. malabathricum was used for treating diseases such as hemorrhoids, cuts and wounds, toothache, and stomachache. Scientific findings also revealed the wide pharmacological actions of various parts of M. malabathricum such as anti-nociceptive, anti-inflammatory, wound healing, anti-diarrheal, cytotoxic, and antioxidant activities. The present study evaluated the mechanism of action of the anti-inflammatory activity of M. malabathricum. Initially different solvent extracts of M. malabathricum were evaluated for total phenolics, total flavonoids, anti-oxidant activity, antiinflammatory activity (protein denaturation), anti-cancer activity (prostate cancer cell line), and for sPLA2 inhibition. Results showed that ethanolic extract of Melastoma. malabathricum leaves showed higher phenolic and flavonoid concentrations, i.e. 36.77mg GAE/g dry wt. and 245.5 mg QE/gm of dry weight, respectively. Ethanol extract also exhibited the highest free radical scavenging activity in the DPPH method and phosphomolybdenum assay of which the IC50 values were 77.424 mu g/ml and 95.159 mu g/ml respectively. The anti-inflammatory assay (protein denaturation assay) of leaf extract showed the IC50 value of 45.518 mu g/ml. Further, the extract exhibited greater sPLA2 inhibition (143.9 mu g/ml) in the ELISA method against standard inhibitor thioetheramide-PC (6.73 mu g/ml). Finally, the MTT assay for anti-cancer activity showed the IC50 value of 630.57 mu g/ml against the standard cisplatin on the prostate cancer (PC-3) cell line.

Objective: Macrotyloma uniflorum (Horse gram) is an important legume widely consumed in the tropical south Asian countries including India. The present investigation is the elucidation of anti-inflammatory activity of M. uniflorum as it has several medicinal properties. The M. uniflorum was evaluated for inhibition of human secretory phospholipase A 2 (sPLA 2 ) as a function of anti-inflammatory activity. Methods: The total phenols, antioxidant (DPPH scavenging), Anti-lipid peroxidation, PLA 2 inhibition and lipoxygenase (5 & 15-LOX) inhibition activity of aqueous extracts of M. uniflorum coat and pulp were assayed by in vitro method. The aqueous extract of M. uniflorum seed coat was subjected to inhibit PLA 2 enzymes from human inflammatory fluids (Human Synovial Fluid and Human Pleural Fluid) and snake venoms ( Naja naja and Vipera russllii ) using [14]C labeled E. coli by in vivo method. A further effect of substrate and calcium concentration on inhibition of VRV-PLA 2 in presence and absence of M. uniflorum coat extract were assayed. Results: Aqueous coat extract of M. uniflorum shows higher phenolics and biological activity and inhibited all sPLA 2 enzymes in concentration dependent manner. The IC 50 values are found to be in the range of 11.42-20.88μg and IC 50 values for 5-LOX and 15-LOX is 25.92μg and 32.47μg respectively. The extract effectively neutralized indirect hemolytic activity and showed similar potency in neutralizing the in vivo sPLA 2 induced mouse paw edema. Conclusion: These findings suggest that, the active compound/s in extracts of M. uniflorum individually or synergistically responsible for observed sPLA 2 inhibition.