Molecular Insights into the In Vivo Analgesic and Anti-Inflammatory Activity of Indomethacin Analogues.

The primary objective of this research was to identify and explore the most potent and efficacious cyclooxygenase inhibitors, utilizing indole acetic acid drugs as a lead molecule. To achieve this objective, various derivatives (2a-2c and 2e-2g) of the selected lead molecule, indomethacin, were synthesized using a reflux condensation process, targeting the hydroxyl group. The synthesized analogues were subjected to different spectroscopic procedures to determine their structure and confirm their analogues. These derivatives were further screened for acute toxicity and anti-nociceptive and anti-inflammatory activity using established protocols. Docking analysis was performed to evaluate the possible protein-ligand interaction. The test compounds were found to be safe at doses of 50, 75, 100, and 200 mg/kg, i.p. The pharmacological screening revealed that test compounds 2a-2f had a superior peripheral analgesic effect at a dose of 10 mg/kg, in comparison to the parent drug indomethacin, while compound 2g exhibited slightly lower activity at the same dose. The hot plate results showed lower central analgesic activity of the test compounds compared to the standard Tramal, but it was still significant. Anti-inflammatory results were significant, comparable to Diclofenac sodium and indomethacin, except for compounds 2b, 2c, and 2e at a dose of 10 mg/kg body weight. Molecular docking analysis demonstrated that the derived compounds had augmented negative binding energies (-149.39, -146.72, -160.85, -159.34, -140.03, and -150.91 KJ/mol) compared to the parent drugs (-141.07), which supported the research's theme of producing stronger derivatives of standard drugs with significant anti-nociceptive and anti-inflammatory potential. The derived compounds exhibited significant analgesic and anti-inflammatory activities and, therefore, have the potential to be studied further as new drug candidates for pain and inflammation.

A comprehensive review of summer savory (Satureja hortensis L.): promising ingredient for production of functional foods.

This review aims to measure the different aspects of summer savory including biological activity, medicinal properties, nutritional value, food application, prospective health benefits, and its use as an additive in broiler feed. Furthermore, toxicity related to this is also overviewed. Summer savory leaves are abundant in total phenolic compounds (rosmarinic acid and flavonoids) that have a powerful antioxidant impact. Rosmarinic (α-O-caffeoyl-3,4-dihydroxy-phenyl lactic) acid has been identified in summer savory as a main component. According to phytochemical investigations, tannins, volatile oils, sterols, acids, gums, pyrocatechol, phenolic compounds, mucilage, and pyrocatechol are the primary compounds of Satureja species. Summer savory extract shows considerable biological potential in antioxidant, cytotoxic, and antibacterial assays. Regarding antioxidant activity, summer savory extract displays an inhibitory effect on lipid peroxidation. Summer savory also has Fe (III) reductive and free radical scavenging properties and contains minerals and vitamins. Summer savory has important biological properties, including antimicrobial activity and antioxidant activity, and protective effects against Jurkat T Cells, Alzheimer's disease, cancer, infection, cardiovascular diseases, diabetes, and cholesterol. The leaves and stems of this plant are employed in the food, feed, and pharmacological industries due to their antioxidant properties and substantial nutritional content. Conclusively, summer savory is widely considered beneficial for human health due to its versatile properties and medicinal use.

Plant-food-derived Bioactives in Managing Hypertension: From Current Findings to Upcoming Effective Pharmacotherapies.

A sedentary lifestyle has evoked a high risk of cardiovascular (CV) disease, diabetes, and obesity, all of them with high morbimortality rates and with a common denominator, hypertension. Numerous pharmacological drugs have been used for the treatment of hypertension. However, the side effects associated with the use of existing pharmacological therapies have triggered a demand for plant-based medications. In this connection, the aim of this review was to provide an in-depth analysis of the use of plant-derived bioactives for the effective management of hypertension. Phytoconstituents from leaves, bark, stem, roots, seeds, and fruits of medicinal plants grown in our different regions of the globe have been highly searched. Among them, polyphenols (e.g., flavonoids as quercetin, anthocyanins as cyanidin, tannins as ellagic acid, stilbenes as resveratrol, lignans as honokiol and others as hydroxytyrosol or curcumin), organosulfur compounds (e.g. s-allyl cysteine and allicin), fatty acids (e.g. α-lipoic acid, DHA and oleic acid), alkaloids (e.g. berberine or tetrandrine) and some terpenes have been intensively investigated for the management of hypertension, with effective ability being stated in controlling high blood pressure and related health problems both in vivo and in vitro studies. Some of the activities presented by these bioactive compounds are reducing oxidative stress, renin-angiotensin system control, SIRT1 activation, regulating platelet aggregation and COX activity, anti-atherogenic effects, anti-inflammatory properties, vasorelaxation and other results that translate into the prevention or control of hypertension. The knowledge of these bioactive compounds is important in developing countries where traditional medicine is the majority, but it can also give rise to new approaches in hypertension therapy.

Nigella Plants - Traditional Uses, Bioactive Phytoconstituents, Preclinical and Clinical Studies.

Nigella is a small genus of the family Ranunculaceae, which includes some popular species due to their culinary and medicinal properties, especially in Eastern Europe, Middle East, Western, and Central Asia. Therefore, this review covers the traditional uses and phytochemical composition of Nigella and, in particular, Nigella sativa. The pharmacological studies reported in vitro, in vivo, and in humans have also been reviewed. One of the main strength of the use of Nigella is that the seeds are rich in the omega-6 fatty acid linoleic acid and provide an extra-source of dietary phytochemicals, including the bioactive thymoquinone, and characteristics saponins, alkaloids, and flavonoids. Among Nigella species, N. sativa L. is the most studied plant from the genus. Due to the phytochemical composition and pharmacological properties, the seed and seed oil from this plant can be considered as good candidates to formulate functional ingredients on the basis of folklore and scientific knowledge. Nonetheless, the main limations are that more studies, especially, clinical trials are required to standardize the results, e.g. to establish active molecules, dosage, chemical profile, long-term effects and impact of cooking/incorporation into foods.

Proanthocyanidins: A comprehensive review.

Proanthocyanidins are condensed tannins with various pharmacological properties. These phytochemicals are considered as 'offense and defense molecules because of their human health benefits. The validation of their diverse health aspects, namely, antioxidant, anticancer, antidiabetic, neuroprotective, and antimicrobial has earned them repute in thermochemistry. Proanthocyanidins are oligo- or polymers of monomeric flavan-3-ols produced as an end product of flavonoid biosynthetic pathway. Agricultural wastes and food processing wastes contain immense amount of proanthocyanidins, exploitation of which can be a sustainable source of dietary supplements and functional ingredients. The current review article discusses recent developments in the health promoting properties of proanthocyanidins and the associated hurdles.

Aqueous garlic extract and its phytochemical profile; special reference to antioxidant status.

Garlic (Allium sativum L) has distinct nutritional profile with special reference to its bioactive components and is used in different diet-based therapies to cure various lifestyle-related disorders. For this purpose, characterization and extraction of garlic were carried out followed by antioxidant assays. Different solvents (50% aqueous ethanol, 50% aqueous methanol and water) at different time intervals (4, 5 and 6 h) at 60°C were used to optimize aqueous extraction efficiency of garlic. Among the solvents, water extract resulted in better extraction yield (31.85 ± 2.09 g/25 g) at 5 h. The antioxidant potential of all these solvents was estimated through in vitro studies. In this context, it was observed that higher amount of total phenolic contents was present in aqueous methanol 71.87 ± 1.69% at 45 min. Antiradical (1,1-diphenyl-2-picrylhydrazyl assay) and antioxidant activity showed that the maximum value was 73.80 ± 3.69 and 83.83 ± 0.16%, respectively, in methanolic extract at 45 min while glucose diffusion and ferric reducing antioxidant power were 97.00 ± 0.20 and 32.66 ± 0.72% at p < 0.05, respectively. Aqueous garlic extract was selected as the best treatment on the basis of percentage yield and safety modulation in human body absorption. Aqueous garlic extract was subjected to pH, acidity, total soluble solids (TSS) and colour. It was observed that the pH of aqueous garlic extract decreased with the passage of time while acidity increased. It was also concluded that storage affected the value of TSS and colour significantly. L* values for colour on 0 day were 34.18 ± 0.08, whereas those on 28th day were 38.84 ± 0.03. It was predicted that 28 days storage resulted in significant increase in L* value, while a* value decreased from 4.31 ± 0.01 to 0.32 ± 0.01 at the end of storage study.