Tahir Farooq

Acetyl and butyryl cholinesterase inhibitory sesquiterpene lactones from Amberboa ramosa

BackgroundAlzheimer’s disease (AD) is characterized by a progressive memory loss that leads to a profound emotional disturbance in later stages. As no safe and effective drug is yet available for the treatment of AD, secondary metabolites from plants may be instrumental in meeting this challenge. Keeping in view this point we evaluated sesquiterpenes of medicinal plant Amberboa ramosa for their cholinesterase inhibitory activity.ResultsFour sesquiterpene lactones have been isolated from the ethyl acetate soluble fraction of Amberboa ramosa. In which one compound Amberbin C (1) was found to be new while other three Amberin (2), Amberbin A (3), and Amberbin B (4) were previously reported ones. The structures of the isolated compounds were elucidated using different spectroscopic techniques. Isolated compounds were tested for their inhibitory potential against acetyl cholinesterase and butyryl cholinesterase enzymes. All compounds showed excellent inhibitory activities against acetyl cholinesterase and butyryl cholinesterase.ConclusionsA new sesquiterpene lactone has been isolated and fully characterized, the sesquiterpene lactones from Amberboa ramosa showed good inhibitory activities against acetyl cholinesterase and butyryl cholinesterase enzymes, this study indicated that sesquiterpene lactone can become interesting lead molecules in drug development against Alzheimer’s disease (AD).

Facile and Green Synthesis of Saturated Cyclic Amines

Single-nitrogen containing saturated cyclic amines are an important part of both natural and synthetic bioactive compounds. A number of methodologies have been developed for the synthesis of aziridines, azetidines, pyrrolidines, piperidines, azepanes and azocanes. This review highlights some facile and green synthetic routes for the synthesis of unsubstituted, multisubstituted and highly functionalized saturated cyclic amines including one-pot, microwave assisted, metal-free, solvent-free and in aqueous media.

Stem Cell Therapy and Type 1 Diabetes Mellitus: Treatment Strategies and Future Perspectives

Type 1 diabetes mellitus (T1DM) is classified as an autoimmune disease which progressively results in the depletion of insulin-secreting β-cells. Consequently, the insulin secretion stops leading to hyperglycemic situations within the body. Under severe conditions, it also causes multi-organ diabetes-associated dysfunctionalities notably hypercoagulability, neuropathy, nephropathy, retinopathy, and sometimes organ failures. The prevalence of this disease has been noticed about 3% that has highlighted the serious concerns for healthcare professionals around the globe. For the treatment of this disease, the cell therapy is considered as an important therapeutic approach for the replacement of damaged β-cells. However, the development of autoantibodies unfortunately reduces their effectiveness with the passage of time and finally with the recurrence of diabetes mellitus. The development of new techniques for extraction and transplantation of islets failed to support this approach due to the issues related to major surgery and lifelong dependence on immunosuppression. For T1DM, such cells are supposed to produce, store, and supply insulin to maintain glucose homeostasis. The urgent need of much-anticipated substitute for insulin-secreting β-cells directed the researchers to focus on stem cells (SCs) to produce insulin-secreting β-cells. For being more specific and targeted therapeutic approaches, SC-based strategies opened up the new horizons to cure T1DM. This cell-based therapy aimed to produce functional insulin-secreting β-cells to cure diabetes on forever basis. The intrinsic regenerative potential along with immunomodulatory abilities of SCs highlights the therapeutic potential of SC-based strategies. In this article, we have comprehensively highlighted the role of SCs to treat diabetes mellitus.

Synthesis of antibacterial poly( o -chloroaniline)/chromium hybrid composites with enhanced electrical conductivity

Electrically conductive polyorthochloroaniline/chromium nanocomposites (POC/Cr NCs) were prepared by in situ chemical oxidative polymerization of orthochloroaniline in the presence of Cr nanoparticles (Cr NPs). The load percentage of Cr nanofiller was varied in POC matrix to investigate the effect of Cr nanoparticles on the properties of the nanocomposites. The composition, structure, and morphology of POC and its composites were examined by Scanning electron microscopy, Fourier transform infrared spectroscopy, and UV–visible spectroscopic analysis. The antibacterial potential of POC and its composites was evaluated by the disc diffusion method against Escherichia coli and Bacillus subtilis. The results showed the improved antibacterial potential with the increase in the load percentage of nanofiller. The electrical conductivity of polymer and its composites was measured and correlated with the load percentage. The results showed that electrical conductivity of the composites was enhanced with the increase in load percentage of Cr nanoparticles.

Ethnopharmacological Investigations of Phytochemical Constituents Isolated from the Genus Cuscuta

The genus Cuscuta, of the family Cuscutaceae, is present in plants and has been traditionally used medicinally against many diseases and conditions, notably depression, mental illness, headache, spleen disease, jaundice, diabetes mellitus, and hypertension. Large numbers of phytochemical constituents such as alkaloids, flavonoids, lignins, oxygen heterocyclic compounds, steroids, fatty acids, phenolic acids, resin glycosides, and polysaccharides have been isolated from different species of Cuscuta. Ethnopharmacological studies conducted on such constituents have also been shown Cuscuta to possess anticancer, antiviral, antispasmodic, antihypertensive, anticonvulsant, antibacterial, antioxidant, diuretic, and hair-growth activity. Many tribes and traditional communities have long used the different forms of Cuscuta for treatment and prevention of many diseases. In this article, we comprehensively summarize relevant data regarding the phytochemical, ethnopharmacological, and traditional therapeutic uses of Cuscuta. In addition, we review the parts of the plants that are used as traditional therapeutic agents, their regions of existence, and their possible modes of action. To conclude, we provide evidence and new insights for further discovery and development of natural drugs from Cuscuta. We show that further studies are needed to investigate the mechanism of action and safety profile of phytochemical constituents isolated from Cuscuta.

Emerging Trends in Non-Interferon-Based Genotype-Specific Antiviral Agents: Pharmaceutical Perspectives

Hepatitis C virus (HCV) presents a serious global health threat. Initially, the health-care community mainly focused on interferon (IFN)-based therapeutic options to eradicate HCV, but with the passage of time, these applications became unsuitable due to some serious side effects related to the use of IFN. In recent years, research conducted on different phases of HCVs life cycle has opened a new gateway for the use of a direct-acting new generation of anti-HCV agents. Their safer and ultrarapid response has made possible the introduction of triple therapy and use of IFN-free therapeutic treatment strategies. However, the high cost of these successful therapies has raised serious concerns, particularly in low-income countries, and this has forced pharmaceutical scientists to explore more cost-effective IFN-free alternatives for the treatment of HCV. In this article, we have briefly summarized the latest data regarding the research and development of non-IFN-based antiviral agents. The studies mentioned in this article highlight the significance of non-IFN-based direct-acting antiviral (DAA) agents. Economical alternative anti-HCV agents are expected to become available in the near future for better and more cost-effective treatments of HCV.

Amberinone, a new guaianolide from Amberboa ramosa

The Amberboa is a medicinally important genus present in the family Asteraceae; members of this genus are mainly distributed in Pakistan and India. It has been used in different systems of traditional medicines for different diseases. Amberinone (1), a new sesquiterpene lactone, has been isolated from the ethyl acetate (EtOAc) soluble fraction of Amberboa ramosa together with chrysin (2), quercitine (3), eriodictyol (4) and keamferol (5). This is the first report of these compounds from this species. The structures of the isolated compounds have been elucidated by 1D and 2D 1H 13C NMR spectroscopy.