Mini Reviews in Medicinal Chemistry - Volume 21, Issue 3, 2021

Coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndromerelated coronavirus-2 (SARS-CoV-2), has become an ongoing pandemic worldwide. However, there are no vaccines or antiviral drugs with proven clinical efficacy. Therefore, a remedial measure is urgently needed to combat the devastating COVID-19. The pharmacological activities of Nacetylcysteine (NAC) and its potential functions in inhibiting the progression of COVID-19 make it a promising therapeutic agent for the infection. In this mini-review, we discussed the therapeutic potential of NAC in COVID-19 from the perspective of its multisite pharmacological actions.

Background: Centipeda minima (the family Asteraceae) is an annual herbaceous plant native to the tropical regions, especially in eastern tropical Asia. C. minima is well-known in the list of medicinal plants with capacities in treatment of whooping cough, nasal allergy, malaria, and asthma. More than sixty reports on phytochemical and pharmacological aspects of this plant are now available, but a supportive review is insufficient. Objective: The current review aims to make a compilation of almost all of the isolated compounds from the title plant, together with their pharmacological activities. Methodology: Centipeda minima is a meaningful keyword to search for previous references, while the reliable databases, such as Sci-Finder, Google Scholar, Pub Med, Science Direct, the Web of Science, Scopus, Bentham science, Taylor Francis, Springer, IOP Science were utilized at most. Conclusion: More than one hundred secondary metabolites, classifying as terpenoids, flavonoids, mono-phenols, fatty acids, amides, and other types, were isolated from this plant. Among them, sesquiterpene lactones are dominant in either C. minima species or numerous plants of genus Centipeda. These phytochemical groups also possessed various biological results like anti-cancer, anti-bacteria, anti-allergy, anti-virus, anti-inflammation, and hepatoprotective activities. With many kinds of bioactive results such as anti-cancer and anti-inflammation, the use of C. minima plant extracts and isolated compounds for drug development seems to be a futuristic strategy.

Background: AKT/PKB is an important enzyme with numerous biological functions, and its overexpression is related to carcinogenesis. AKT stimulates different signaling pathways that are downstream of activated tyrosine kinases and phosphatidylinositol 3-kinase, hence functions as an important target for anti-cancer drugs. Objective: In this review article, we have interpreted the role of AKT signaling pathway in cancer and the natural inhibitory effect of Thymoquinone (TQ) in AKT and its possible mechanisms. Method: We have collected the updated information and data on AKT, its role in cancer and the inhibitory effect of TQ in AKT signaling pathway from Google Scholar, PubMed, Web of Science, Elsevier, Scopus, and many more. Results: Many drugs are already developed, which can target AKT, but very few among them have passed clinical trials. TQ is a natural compound, mainly found in black cumin, which has been found to have potential anti-cancer activities. TQ targets numerous signaling pathways, including AKT, in different cancers. In fact, many studies revealed that AKT is one of the major targets of TQ. The preclinical success of TQ suggests its clinical studies on cancer. Conclusion: This review article summarizes the role of AKT in carcinogenesis, its potent inhibitors in clinical trials, and how TQ acts as an inhibitor of AKT and TQ’s future as a cancer therapeutic drug.

Natural products and medicinal plants have played a vital role in providing healthcare and ensuring well-being for many civilizations since antiquity. It is estimated that around 50% of drugs in the market have a natural product origin especially medicinal plants and herbal drugs, animals, fungi, and marine organisms. Some of these biologically active constituents of extracts have low absorption and distribution which, as a result, lead to loss of bioavailability and efficacy and might hamper their applications in the clinic. To overcome these impediments for the formulation of herbal drugs, food supplements, and essential oils, several nanomedical approaches such as liposomes, microemulsions, polymeric nanoparticles, solid lipid nanoparticles (SLNs), liquid crystal systems (LC), and precursor systems for liquid crystals (PSLCs) have been proposed. Nanoparticles have been used to modify and ameliorate the pharmacokinetic and pharmacodynamic properties of different drugs, thus incorporating biotechnological systems may be useful to enhance the bioavailability and bioactivity of herbal drug formulations. Consequently, essential for any natural compounds is the extent of its absorption after being ingested and its ability to be distributed in various tissues or organs of the body. The present review article aims to give an overview of the recent advancements in developing herbal drug formulations based on nanoparticle technologies.

Benzothiazole is a heterocyclic aromatic and bicyclic compound in which, benzene ring is attached with thiazole ring. This nucleus is established in marine as well as terrestrial natural compounds. The benzothiazole skeleton is established in a broad variety of bioactive heterocycles and natural products. The benzothiazole nucleus is considered as the principle moiety in several biologically active compounds. Over the decade, chemists are paying more attention towards the revision of the biological and therapeutic activities such as antimicrobial, analgesic, antiinflammatory, antitubercular, antiviral and antioxidant of benzothiazole containing compounds. The molecular structures of a number of potent drugs including Frentizole, Pramipexole, Thioflavin T and Riluzole etc., are based on benzothiazole skeleton. The present work is the compilation and presentation of all available information in a systematic manner with an aim to present the findings in a way, which may be beneficial for future research.

Many plants in the genus Zanthoxylum, belonging to the Rutaceae family, are used as folk medicines for the treatment of various diseases, which have gained much attention for their phytochemical and pharmacological activity investigations. Alkaloids are the largest secondary metabolites with structurally diverse types found in this genus and they demonstrate a wide range of biological activities. The aim of this review is to provide a summary on the isolation, classification, and biological properties of alkaloids from Zanthoxylum species, which also will bring more attention to other researchers for further biological study on alkaloids for the new drug development.

Schizophrenia is a chronic neuropsychiatric disorder that affects nearly 1% of the global population. There are various anti-psychotic drugs available for the treatment of schizophrenia, but they have certain side effects; therefore, there is a need to explore and develop novel potential lead compounds against schizophrenia. The currently available drugs e.g. typical and atypical antipsychotics act on different dopamine and serotonin receptors and as per literature reports, various piperidine and piperazine derivatives have shown promising activity against these receptors. When different heterocyclic groups are attached to basic piperidine and piperazine rings, the antipsychotic activity is greatly potentiated. In this direction, various antipsychotic drugs have been synthesized at the laboratory level, and few are under clinical trial studies, such as Lu AE58054, PF-04802540, ORG25935, DMXB-A, Bitopertin, and ABT-126. In the present review, we include the studies related to the effect of different substituents on piperidine/piperazine derivatives and their anti-psychotic activity. Various series of synthesized compounds by other researchers with piperidine/piperazine nucleus have been reviewed and diagrammatically represented in the form of SAR (structure-activity relationships), which will help the scientists for the development of potential lead compounds.

Oxidative/nitrosative stress can be caused by excessive production of ROS and RNS with metabolic reactions that change the balance in favor of oxidants in cases where oxidants increase and antioxidants decrease in organisms using oxygen. ROS and RNS react with several biological macromolecules in cells, such as carbohydrates, nucleic acids, lipids, and proteins, and alter their functions. Some natural antioxidants are constantly being researched for their benefits in terms of human health, which can strengthen the body's antioxidant defense system and have the potential to scavenger free radicals. It is a well-known and practical strategy to prevent and / or treat diseases due to the consumption of more suitable fruits, herbs, spices and vegetables, and the presence of bioactive antioxidant compounds. Moringa oleifera, a new and important one of these plants, has a wide range of bioactive compounds that can be obtained in different herbal structures such as leaves, seeds, stems and shells. It consists of bioactive molecules, such as phenolic compounds, fats, fatty acids, carbohydrates, proteins, functional peptides, vitamins, minerals and essential amino acids as well as a number of glycosides and has great potential for use in various formulations in various health and food products. This review highlights the formation of MO, its importance in natural medicine, its pharmacological value, and its role as a possible anti-proliferative agent against cancer and its use in some diseases.