Current Topics in Medicinal Chemistry - Volume 22, Issue 18, 2022

Cancer is a fatal disease with a collection of related diseases in various body parts. The conventional therapies cannot show the desired results of treatment due to their imprecise targeting, deprived drug delivery, and side effects. Therefore, it is required to make the drug engineered so that it can target only cancerous cells and inhibit its growth and proliferation. Nanotechnology is a technology that can target and differentiate between cancerous cells and the body's normal cells. Silver itself is a good anticancer and antibacterial agent and employing it with phytochemicals with anticancer properties, and nanotechnology can give the best approach for the treatment. The synthesis of silver nanoparticles using plant extracts is an economical, energy-efficient, low-cost approach, and it doesn’t need any hazardous chemicals. In the present review, we discussed different methods of synthesis of silver nanoparticles using herbal extracts and their role against cancer therapy along with the synergistic role of silver and plant extracts against cancer in the formulation.

Background: Medicinal uses of natural phenolic acids and their synthetic derivatives have been augmented in recent years. Phenolic acids are chemically defined secondary plant metabolites and being moieties or leads are much versatile in nature with a wide scope of biological activities which seek the attention of researchers across the world to synthesize different derivatives of phenolic acids and screen them for their various biological properties. These compounds are of meticulous interest due to the properties they possess and their occurrence. Based on the convincing evidence reported in the literature, it is suggested that phenolic acids and their derivatives are promising molecules as a drug. Objectives: The present review article aims to bring together the information on the biosynthesis, metabolism, and sources of phenolic acids and emphasize the therapeutic potential of phenolic acid and its synthetic derivatives to comprehensively portray the current scenery for researchers interested in designing drugs for furthering this study. Conclusion: Phenolic acids being moieties or lead, are much versatile in nature as they possess a wide range of biological activities like antimicrobial, antioxidant, antiviral, antiulcer, antiinflammatory, antidiabetic, anticancer and many more offers researchers to explore more about these or many untapped benefits in the medicinal field. The information mentioned in this article will be helpful to the forthcoming researchers working in this area. Phenolic acids have massive potential to be investigated for novel medicinal possibilities and for the development of new chemical moieties to treat different diseases of clinical importance.

Influenza viruses (INFV), the Orthomyxoviridae family, are mainly transmitted among humans via aerosols or droplets from the respiratory secretions. However, fomites could be a potential transmission pathway. Annually, seasonal INFV infections account for 290-650 thousand deaths worldwide. Currently, there are two classes of approved drugs to treat INFV infections, being neuraminidase (NA) inhibitors and blockers of matrix-2 (M2) ion channel. However, cases of resistance have been observed for both chemical classes, reducing the efficacy of treatment. The emergence of influenza outbreaks and pandemics calls for new antiviral molecules that are more effective, and that could overcome the current resistance to anti-influenza drugs. In this context, polyphenolic compounds are found in various plants, and these have displayed different multi-target approaches against diverse pathogens. Among these, green tea (Camellia sinensis) catechins, in special epigallocatechin-3-O-gallate (EGCG), have demonstrated significant activities against the two most relevant human INFV, subtypes A and lineages B. In this sense, EGCG has been found to be a promising multi-target agent against INFV since it can act inhibiting NA, hemagglutination (HA), RNA-dependent RNA polymerase (RdRp), and viral entry/adsorption. In general, the lack of knowledge about potential multi-target natural products prevents an adequate exploration of them, increasing the time for developing multi-target drugs. Then, this review aimed to compile most relevant studies showing the anti-INFV effects of EGCG and its derivatives, which could become antiviral drug prototypes in the future.

Caralluma edulis is a well-known species of the genus Caralluma from Apocynaceae, commonly known as chunga. Caralluma species are mostly succulent perennial herbs, several of which are edible species. The plant has an outstanding therapeutic background in the traditional system of treatment. It has been recommended for the treatment of a number medical disorders such as hypertension, Alzheimer’s disease, rheumatism, gastric problems and leprosy. Traditionally the stem was boiled in water and this extract was then used to cure diabetes. The pharmacological effects of C. edulis have also been explored in various in vitro and in vivo experiments. In this regard, the extract of the plant exhibited strong antioxidant, and analgesic activity against inflammation as well as xylene-mediated ear edema as topical effects. The significant anti-hyperlipidemic effect of the plant extract is also reported. However, the extract was found insignificant in the reversal of alloxan-induced diabetes in the rabbit model at test doses. These pharmacological effects are strongly supported by the presence of different bioactive phytochemicals in the plant. These groups of compounds include sterols, terpenoids, flavonoids, and pregnane glycosides. C. edulis is a very potential member of the genus Caralluma with strong traditional history, phytochemistry and phytopharmacology, and needs further exploration for clinically used lead compounds. In this review, we have focused on combining different reported data on the traditional uses of the plant, its phytochemical profile and pharmacological effects in different experimental assay along with subsequent future prospects.

P-coumaric acid is a common dietary polyphenol present in fruits, vegetables, and cereals in conjugated and free form. The toxicity profile of the drug is very low, and it exhibits many pharmacological actions (antihypertensive, anti-inflammatory, anticancer, antimicrobial activity, antidiabetic, anticancer, and antioxidant effect). P-coumaric acid also acts as a free radical scavenger and inhibits various enzymes, which generate free radicals. It is also used as the raw material for the preparation of preservatives, vanillin, sports foods, skin defense agents, and as a cross-linker for the formation of edible films and food gels. The current study is based upon biological effectiveness, molecular docking, SAR, sources of p-coumaric acid, and related derivatives.

Introduction: Although drugs currently available for the treatment of anxiety and depression act through modulation of the neurotransmission systems involved in the neurobiology of the disorder, yet they often present side effects, which can impair patient adherence to treatment. Methods: This has driven the search for new molecules with anxiolytic and antidepressant potential. Aromatic plants are rich in essential oils, and their chemical constituents, such as monoterpenes, are being studied for these disorders. This study aims to evaluate the anxiolytic and antidepressant-like potential of the monoterpene tetrahydrolinalool in in vivo animal models and review pharmacological targets with validation through molecular docking. Male Swiss mice (Mus musculus) were treated with THL (37.5-600 mg kg^-1 p.o.) and submitted to the elevated plus maze, open field, rotarod, and forced swim tests. In the elevated plus-maze, THL at doses of 37.5 and 75 mg kg^-1 induced a significant increase in the percentage of entries (72.7 and 64.3% respectively), and lengths of stay (80.3 and 76.8% respectively) in the open arms tests. Results: These doses did not compromise locomotor activity or motor coordination in the animals. In the open field, rotarod tests, and the forced swimming model, treatment with THL significantly reduced immobility times at doses of 150, 300, and 600 mg kg^-1, and by respective percentages of 69.3, 60.9 and 68.7%. Conclusion: In molecular docking assay, which investigated potential targets, THL presented satisfactory energy values for: nNOs, SGC, IL-6, 5-HT1A, NMDAr, and D1. These demonstrate the potential of THL (a derivative of natural origin) in in vivo and in silico models, making it a drug candidate.