In Silico PASS Predictions and Exploration of Antioxidant and Anti-inflammatory Activity of Citrus Karna Raf. Fruit.

Objective: Inflammation and oxidative stress are major factors in the development of many disorders. Natural antioxidants present in plants can interrupt, decrease, or reduce the oxidation of components sensitive to oxidative processes by scavenging free radicals and lowering oxidative stress. Most anti-inflammatory agents used in the management of inflammatory disorders diminish oxidative damage. The biological potential of Citrus karna Raf. remains undisclosed, despite its richness in several bioactive compounds. Methods: The methanolic extract was evaluated for quantitative phytochemical analysis and antioxidative efficacy using 1,1-diphenyl-2-picrylhydrazyl radical and hydrogen peroxide scavenging activity. A carrageenan-induced paw edema model was employed to evaluate the anti-inflammatory potential as antioxidants exert anti-inflammatory effects. In silico prediction of activity spectra for substance predictions were performed to understand the possible mechanism of action of phytochemicals. Results: Citrus karna methanolic extract (CKME) showed dose-dependent radical scavenging effects. The powerful scavenging activity of CKME could be due to the diverse polyphenolic compounds such as ascorbic acid, beta-carotene, and naringin. In addition, the percentage inhibition of paw edema and swelling was observed in CKME-treated rats and mice, which is the same as that of standard drug-treated groups. The Pa value of ascorbic acid, beta-bisabolene, linalool, and naringin is more than 0.7 which shows that these phytoconstituents might contribute to the anti-inflammatory action of extract samples such as CKME. Conclusions: Our findings shows that CKME possess strong antioxidant and anti-inflammatory effects. The richness of plants in polyphenolics such as flavonoids might be a contributing factor for these potential effects.

Isolation and Characterization of Anti-Inflammatory Compounds from Ficus microcarpa L.f. Stem Bark.

The anti-inflammatory effect of the ethyl acetate extract of F. microcarpa bark (EAFMB) was investigated in acute and chronic (21 days) inflammation induced in Wistar albino rats. EAFMB (200 mg/kg b.w.) exhibited comparable anti-inflammatory effects to the reference drug, with a reduction of 59.48% at 4 h in acute inflammation and 83.96% on day 21 in chronic inflammation. Bioassay-guided fractionation using DPPH radical scavenging activity led to isolating and identifying three compounds from EAFMB: oleanolic acid, catechin, and p-hydroxycinnamic acid. All these compounds demonstrated the concentration-dependent inhibition of COX enzymes and the protection of egg albumin from heat-induced denaturation. Catechin exhibited the highest COX inhibition (COX-1 and COX-2 IC50 = 9.02 and 50.38 µM, respectively) and anti-denaturation effect (IC50 = 27.13 µg/mL) compared to oleanolic acid and p-hydroxycinnamic acid. These isolated compounds are likely responsible for the anti-inflammatory activities of F. microcarpa bark.

Role of Pentacyclic Triterpenoids in Chemoprevention and Anticancer Treatment: An Overview on Targets and Underling Mechanisms.

The incidences of cancer are continuously increasing worldwide, affecting life of millions of people. Several factors associated with the internal and external environment are responsible for this deadly disease. The key internal determinants like abnormal hormonal regulation, genetic mutations and external determinants such as lifestyle and occupational factors enhances onset of cancer. From the ancient time, plants were remained as the most trusted source of medicine for the treatment of diverse disease conditions. Extensive studies have been performed for the discovery of effective anticancer agent from the plant and still it is going on. Pentacyclic triterpenoids are biologically active phytochemicals having a different range of activities such as anti-inflammatory, hepatoprotective, anti-hypertensive, antiulcerogenic and anti-tumor. These compounds generally contain ursane, oleanane, lupane and friedelane as a chief skeleton of pentacyclic triterpenoids which are generally present in higher plants. Isoprene unit, phytochemical, with good antitumor/anticancer activity is required for the biosynthesis of pentacyclic triterpenoids. Mechanisms such as cytotoxicity, DNA polymerase inhibition, regulation of apoptosis, change in signal transductions, interfere with angiogenesis and dedifferentiation, antiproliferative activity and metastasis inhibition are might be responsible for their anticancer effect. Present review spotlights diverse targets, mechanisms and pathways of pentacyclic triterpenoids responsible for anticancer effect.

Pharmacological evaluation for anti-asthmatic and anti-inflammatory potential of Woodfordia fruticosa flower extracts.

CONTEXT: Woodfordia fruticosa Kurz. (Lythraceae) flowers are ethnopharmacologically acclaimed in the Indian medicinal system to treat asthma. OBJECTIVE: To evaluate W. fruticosa flower extracts for anti-asthmatic effect. MATERIALS AND METHODS: Ethyl acetate, acetone, methanol, and hydro-alcohol extracts of W. fruticosa flowers were obtained successively and standardized. Ability of extracts to stabilize free radicals and compound-48/80-induced mast cell degranulation was evaluated. In vitro anti-inflammatory potential of extracts at 100 and 200 µg/ml by membrane stabilization and in vivo inhibition of rat paw edema up to 5 h (100 and 200 mg/ml; p.o.) was evaluated. In vitro bronchorelaxant effect was examined against histamine- and acetylcholine (1 µg/ml; independently)-induced guinea pig tracheal contraction. Extracts were evaluated for bronchoprotection (in vivo) ability against 0.1% histamine- and 2% acetylcholine-induced bronchospasm in guinea pigs at 100 and 200 mg/ml; p.o. RESULTS: Standardization studies revealed that the methanol extract exhibited highest polyphenolic (62.66 GAE), and flavonoid (6.32 RE) content and HPLC fingerprinting confirmed the presence of gallic acid (Rt 1.383). IC50 values for DPPH scavenging and metal chelation by the methanol extract were 40.42 and 31.50 µg/ml. Methanol and ethyl acetate extracts at 100 µg/ml exhibited 06.52 and 07.12% of histamine release. Methanol, ethyl acetate, and hydro alcohol extracts at 200 mg/kg demonstrated 32.73, 29.83, 26.75% and 32.46, 9.38, 26.75% inhibition of egg albumin and carrageenan-induced inflammation, respectively. Methanol extract exhibited 100% bronchorelaxation and 48.83% bronchoprotection. CONCLUSION: Woodfordia fruticosa flower (WFF) extracts exhibited anti-asthmatic effect by demonstrating bronchoprotection, bronchorelaxation, anti-inflammatory, antioxidant, and mast cell stabilization ability.

Bronchorelaxant, mast cell stabilizing, anti-inflammatory and antioxidant activity of Randia dumetorum (Retz.) Lamk. extracts.

Randia dumetorum (RD) fruits in different form have been ethnopharmacologically reported to possess antiasthmatic property. Therefore, present study was undertaken to evaluate two different extracts of RD i.e., ethyl acetate (RD-EA) and methanol (RD-ME) for bronchorelaxant, anti-inflammatory, mast cell stabilizing and antioxidant effect along with safety margin, according to OECD guidelines for toxicity. RD-ME and RD-EA (1 mg/mL) exhibited 68.75 and 57.39% inhibition of contraction against acetylcholine, while against histamine induced contraction, inhibition observed was 100 and 78.13%, respectively. Moreover, extracts attenuated the experimentally induced inflammation at 200 mg/kg with % inhibition of 41.62 by RD-ME and 30.36 by RD-EA in carrageenan model, while in egg albumin model RD-ME and RD-EA exhibited % inhibition of 48.31 and 33.75, respectively. In addition, RD-ME and RD-EA at 100 microg/mL demonstrated significant decrease in histamine release of 08.31 and 16.71 in C-48/80 induced mast cell degradation. RD extracts also exhibited antioxidant activity in DPPH, reducing power and metal chelation method, along with safe margin for oral administration as observed in acute toxicity evaluation.