A comprehensive review of ethnomedicinal approaches, phytochemical analysis, and pharmacological potential of Vitex trifolia L.

Plants, renowned for their rich reservoir of metabolites, play a pivotal role in addressing health-related issues. The Verbenaceae family stands out, showcasing immense potential in preventing and treating chronic diseases. Vitex trifolia L. (V. trifolia), a shrub with a rich history in traditional medicine, particularly in Eastern Asia, has garnered attention for its diverse therapeutic applications. This comprehensive review aims to bridge traditional knowledge and contemporary insights by investigating ethnopharmacology, phytochemistry, and pharmacological effects of V. trifolia. The keyword "V. trifolia" and its synonyms were searched within the main scientific databases including PubMed, Web of Science, ScienceDirect, Google Scholar, and Baidu Scholar (from 1974 to 2022, last search: 21.10.2023). Phytochemical analyses reveal a spectrum of secondary metabolites in V. trifolia, including terpenoids, flavonoids, lignans, phytosterols, anthraquinones, and fatty acids. Notably, terpenoids and flavonoids emerge as the main bioactive metabolites. Pharmacological studies validate its therapeutic potential, demonstrating significant antioxidant, anti-inflammatory, hepatoprotective, anticancer, anti-amnesic, antimicrobial, antiviral, anti-malaria, antispasmodic activities, and reported insecticidal effects. Despite existing literature exploring pharmacological attributes and secondary metabolites of related species, a conspicuous gap exists, specifically focusing on the pharmacological activities and novel methods of purification of pure metabolites from V. trifolia. This review aimed to fill this gap by delving into traditional medicinal applications, exploring secondary metabolites comprehensively, and providing an in-depth analysis of pharmacological effects of pure metabolites. Combining traditional uses with contemporary pharmacological insights, this article sought to serve as a crucial reference for future research and practical application of V. trifolia. This approach contributes substantially to understanding the plant, fostering scientific inquiry, and facilitating its broader application in healthcare.

Design, synthesis, in vitro, and in silico evaluations of kojic acid derivatives linked to amino pyridine moiety as potent tyrosinase inhibitors.

In the present study, novel series of kojic acid derivatives conjugated to amino pyridine moiety were designed and synthesized to explore their inhibitory activity against tyrosinase. To this end, the structure of all derivatives was characterized by 1H NMR, 13C NMR, FT-IR, and elemental analysis. Next, all derivatives were evaluated against tyrosinase compared to the kojic acid as positive control and exhibited different inhibitory potencies. Furthermore, the antioxidant potential of all derivatives was determined. The kinetic analysis of the most active agent revealed that 3-hydroxy-6-(hydroxymethyl)-2-((3-nitrophenyl)(pyridin-2-ylamino)methyl)-4H-pyran-4-one (4h) binds to the enzyme in the uncompetitive mode of action. The docking analysis and molecular dynamic simulations showed considerable binding affinity and significant interactions with tyrosinase enzyme to target the melanogenesis pathway, proposing them as potent candidates to control hyperpigmentation in the future.

Thioquinoline derivatives conjugated to thiosemicarbazide as potent tyrosinase inhibitors with anti-melanogenesis properties.

In the present study, a series of aryl-substituted thioqunoline conjugated to thiosemicarbazide were rationally designed and synthesized. The formation of target compounds was confirmed by spectral characterization techniques such as IR, 1H-NMR, 13C-NMR, ESI-MS, and elemental analysis. Among the synthesized derivatives, compound 10g bearing para-chlorophenyl moiety was proved to be the most potent tyrosinase inhibitor with an IC50 value of 25.75 ± 0.19 µM. Compound 10g as the most potent derivative exhibited a noncompetitive inhibition pattern against tyrosinase in the kinetic study. Furthermore, the in silico cavity detection, as well as the molecular docking assessments, were performed to follow the behavior of 10g within the proposed binding site. Besides, the toxicity of 10g and its potency to reduce the melanin content on A375 cell lines were also measured. Consequently, aryl-substituted thioqunolines conjugated to thiosemicarbazide might be a promising candidate in the cosmetics, medicine, and food industry as tyrosinase inhibitors.

Synthesis and bioactivities evaluation of quinazolin-4(3H)-one derivatives as α-glucosidase inhibitors.

The development of new antidiabetes agents is necessary to obtain optimal glycemic control and overcome its complications. Different quinazolin-4(3H)-one bearing phenoxy-acetamide derivatives (7a-r) were designed and synthesized to develop α-glucosidase inhibitors. All the synthesized derivatives were evaluated against α-glucosidase in vitro and among them, compound 7b showed the highest α-glucosidase inhibition with an IC50 of 14.4 µM, which was ∼53 times stronger than that of acarbose. The inhibition kinetic studies showed that the inhibitory mechanism of compound 7b was a competitive type towards α-glucosidase. Also, molecular docking studies analyzed the interaction between the most potent derivative and α-glucosidase. Current findings indicate the new potential of quinazolin-4(3H)-ones that could be used for the development of novel agents against diabetes mellitus.

Comparison of the effects of alcoholic extract of aerial parts of Anvillea garcinii and atorvastatin on the lipid profile and thyroid hormones in hypercholesterolemic rats.

Objective: Decreased thyroid hormones along with increased blood fats and overweight, lead to atherosclerosis and eventually cardiovascular disease. The aim of this study was to compare the effects of alcoholic extract of aerial parts of Anvilea garcinii and atorvastatin on the lipid profile and thyroid hormones in hypercholesterolemic rats. Materials and Methods: In this study, 40 male Wistar rats were divided into 5 groups (n=8): control, hypercholesterolemic vehicle and three experimental groups. The control group, received water and normal food daily, the hypercholesterolemic vehicle group received drug solvent (atorvastatin dissolved in distilled water) and three experimental groups received alcoholic extract of A. garcinii (100 and 300 mg/kg) and atorvastatin (10 mg/kg) as gavage. At the end of the 45- day period, blood samples were prepared from all groups and the amount of desired factors was measured and analyzed. Results: The amount of lipid profiles (cholesterol, HDL, LDL, VLDL,TG) and thyroid stimulating hormone in the vehicle group were increased compared to the control group, while the amount of these factors were decreased in the experimental groups compared to the vehicle group. Furthermore, the level of thyroid hormones in the hypercholesterolemic vehicle group was decreased compared to the control group, while the level of these hormones was increased in the experimental groups receiving the extract compared to the vehicle group. Conclusion: Alcoholic extract of A. garcinii aerial parts, may increase thyroid hormones, and sequentially reduce blood lipids; thus, it could be a good candidate for the treatment of hypercholesterolemia and hypothyroidism.

The physiological and pharmacological effects of Ziziphoratenuior L.: A review study.

OBJECTIVE: Many reports have revealed preventive and therapeutic effects of Ziziphoratenuior; however, few systematic reviews have evaluated such effects. The present study reviews the physiological and pharmacological effects of Z. tenuior extract and its components. MATERIALS AND METHODS: English articles were searched in international databases, such as Embase, Scopus, and PubMed; Persian studies were also searched in national databases such as SID and Magiran. RESULTS: Pulegone is one of the most important effective compounds of Z. tenuior, which has analgesic, anti-inflammatory, and anti-stress properties as it affects serotonergic and opioidergic systems and decreases the gastric acid secretion. Moreover, this compound inhibits cholesterol absorption and synthesis, resulting in hyperlipidemic effects and weight loss. In addition to its antioxidant, antitumor, and antibacterial properties, this herb contains an antidiabetic effect mediated by increasing the number of pancreatic beta cells and insulin secretion, and inhibiting alpha-amylase. Although its effective dosage has no side effects, the overuse of its effective compounds, such as pulegone, may raise some liver and pulmonary disorders. CONCLUSION: Z. tenuior and its extract can have preventive and therapeutic effects on diabetes and hyperlipidemia-associated diseases. Since most studies on this herb were in vivo, it is necessary to design clinical trials to evaluate its effects.