Mini Reviews in Medicinal Chemistry - Volume 20, Issue 13, 2020

Curcumin is a poly phenolic compound extracted from turmeric. Over the past years, it has acquired significant interest among researchers due to its numerous pharmacological activities like anti- cancer, anti-alzheimer, anti-diabetic, anti-bacterial, anti-inflammatory and so on. However, the clinical use of curcumin is still obstructed due to tremendously poor bioavailability, rapid metabolism, lower gastrointestinal absorption, and low permeability through cell that makes its pharmacology thrilling. These issues have led to enormous surge of investigation to develop curcumin nano formulations which can overcome these restrictive causes. The scientists all across the universe are working on designing several drug delivery systems viz. liposomes, micelles, magnetic nano carriers, etc. for curcumin and its composites which not only improve its physiochemical properties but also enhanced its therapeutic applications. The review aims to systematically examine the treasure of information about the medicinal use of curcumin. This article delivers a general idea of the current study piloted to overwhelm the complications with the bioavailability of curcumin which have exhibited an enhanced biological activity than curcumin. This article explains the latest and detailed study of curcumin and its conjugates, its phytochemistry and biological perspectives and also proved curcumin as an efficient drug candidate for the treatment of numerous diseases. Recent advancements and futuristic viewpoints are also deliberated, which shall help researchers and foster commercial translations of improved nanosized curcumin combination for the treatment of various diseases.

Inspired by nature, humankind has been able to attain significant achievements in the drug and food industries. Particularly, medicinal plants are a rich source of medicinal, cosmetic, sanitary, and aromatic substances. Genus Ferula from the Apiaceae family is a plant genus that possesses over 170 species, which have been carefully documented with regard to their medicinal properties. Ferula spp. affects many body organs, and their respective functions, in humans, such as the immune system, gastrointestinal tract, genitourinary, endocrine, respiratory, cardiovascular, nervous system, bone (skeleton), and teeth. In spite of the benefits, ferulosis (Ferula toxicity) is an important aspect of Ferula consumption in humans and animals. Hemorrhagic problems and infertility are important signs of ferulosis. In this review, we have described all of the effects of the active ingredients of Ferula spp. and their mechanisms of actions, when known, based on an extensive literature review. Thus, our review opens a window of the benefits of Ferula as a phyto-pharmaceutical and its therapeutic applications in pharmacy, dentistry, and medicine.

Pulmonary pharmaceutical formulations are targeted for the treatment of respiratory diseases. However, their application is limited due to the physiological characteristics of the lungs, such as branching structure, mucociliary and macrophages, as well as certain properties of the drugs like particle size and solubility. Nano-formulations can ameliorate particle sizes and improve drug solubility to enhance bioavailability in the lungs. The nano-formulations for lungs reviewed in this article can be classified into nanocarriers, no-carrier-added nanosuspensions and polymer-drug conjugates. Compared with conventional inhalation preparations, these novel pulmonary pharmaceutical formulations have their own advantages, such as increasing drug solubility for better absorption and less inflammatory reaction caused by the aggregation of insoluble drugs; prolonging pulmonary retention time and reducing drug clearance; improving the patient compliance by avoiding multiple repeated administrations. This review will provide the reader with some background information for pulmonary drug delivery and give an overview of the existing literature about nano-formulations for pulmonary application to explore nano-strategies for improving the bioavailability of pulmonary pharmaceutical formulations.

Electrospun nanofibers regarding their special features, including high drug loading capacity, high surface to volume area, flexibility, and ease of production and operation, are of great interest for being used in tissue engineering, and drug delivery approaches. In this context, several studies have been done for the production of biodegradable and biocompatible scaffolds containing different anticancer agents for fighting with solid tumors. Surprisingly, these scaffolds are able to deliver different combinations of drugs and agents, such as nanoparticles and release them in a time dependent manner. Here in this review, we summarize the principles of electrospinning and their uses in entrapment of drugs and anti-proliferative agents suitable for cancer therapy. The latest studies performed on treating cancer using electrospinning are mentioned and their advantages and disadvantages over conventional treatment methods are discussed.

It is expected that in 2050, there will be more than 20% of senior citizens aged over 60 years worldwide. Such alarming statistics require immediate attention to improve the health of the aging population. Since aging is closely related to the loss of antioxidant defense mechanisms, this situation eventually leads to numerous health problems, including fertility reduction. Furthermore, plant extracts have been used in traditional medicine as potent antioxidant sources. Although many experiments had reported the impact of various bioactive compounds on aging or fertility, there is a lack of review papers that combine both subjects. In this review, we have collected and discussed various bioactive compounds from 26 different plant species known to affect both longevity and fertility. These compounds, including phenolics and terpenes, are mostly involved in the antioxidant defense mechanisms of diverse organisms such as rats, mites, fruit flies, roundworms, and even roosters. A human clinical trial should be considered in the future to measure the effects of these bioactive compounds on human health and longevity. Ultimately, these plant-derived compounds could be developed into health supplements or potential medical drugs to ensure a healthy aging population.

This review explains the effects of naproxen and the naproxen moiety in important biological activities. Naproxen, 2-(6-methoxynaphthalen-2-yl)propionic acid, is one of the most utilized propionic acid derivatives to the cure of many injuries or pains. Naproxen is a non-steroidal antiinflammatory drug (NSAID), which is generally used among the NSAIDs. Even though it has gastrointestinal side effects, naproxen has been safely used for many years because of the good cardiovascular sight. In the past years, except for anti-inflammatory effects, other pharmacological activities of naproxen, especially anticancer and antimicrobial activities, gain the attention of researchers. Naproxen shows its activity by inhibiting the COX-2 enzyme. There is significant interest in the possibility that COX-2 inhibitors might retard or prevent the development of various cancer types, which is often characterized by COX-2 expression. The activities of both naproxen and new molecules derived from naproxen were frequently investigated.

Background: Being derived from primary amine and aromatic aldehyde, Schiff base and their complexes have an imperative role in the improvement of inorganic chemistry, which are broadly studied as coordination compounds and are gradually becoming more important in biochemical and analytical applications. Methods: They have also been used for antibacterial, antifungal, anticancer, antitubercular activities. Novel synthesised Schiff’s base 2-methoxy-4-((3-methylpyridin-2-ylimino)methyl)phenol (SB) and its metal complexes (Zn[II], Cu[II], Co[II] and Ni[II]) were characterised by UV, IR and NMR spectroscopy. Formation of the Schiff base and the metal (Zn[II], Cu[II], Co[II] and Ni[II]) chelates was supported by spectral and analytical data. The ligand and metal complexes have been screened for their antibacterial activity against Staphylococcus aureus, Salmonella typhi, Escherichia coli, Klebsiella pneumoniae and antifungal activity against the fungi Candida albicans and Aspergillus niger. Further, the synthesised compounds were also screened for antiproliferative activity against the human colorectal carcinoma (HCT116) cell line using the Sulforhodamine B assay. Result: Metal complexes formed were found to enhance the potency of the Schiff base due to coordination with a copper complex, showing better activity than others. Conclusion: Copper complex was observed to be more potent than other complexes against all the pathogenic microbes and cancer cell line (HCT116).