Current Bioactive Compounds - Volume 19, Issue 9, 2023

Background: Cancer has turned into a health issue that requires the most rapid attention. Because of the disease's global reach and the high number of deaths it causes, research and development of novel anticancer treatments that are both effective and have fewer adverse effects is crucial. According to a 2015 survey by the World Health Organization (WHO), Cancer kills 8.8 million people each year, accounting for 60% of all fatalities. Objective: Because of its wide variety of biological properties and the widespread usage of benzimidazole as a potent anticancer agent, this study emphasizes the importance of this moiety as an anticancer agent. Results: The benzimidazole ring structure has a wide range of pharmacological activity in a number of drugs used to treat diseases such as hypertension, malaria, cancer, microbial diseases, inflammatory disorders, and more. Furthermore, this fused heterocycle benzimidazole core may interact with various anions and cations, as well as biomolecules, in the human body, resulting in a wide range of biological activities such as antineoplastic, antibacterial and antifungal, antiinflammatory and analgesic, antihypertensive, antiviral, and antidepressant. Conclusion: The focus of this review is on recent advances in drug design and development, as well as benzimidazole derivatives and how they work on various sites of action.

Background: An arbovirus called the Zika virus is spread by Aedes mosquitoes. The Zika virus (ZIKV) epidemic that has recently spread over the Western Hemisphere (the Americas and the ongoing outbreak in Brazil) is now recognised as one of the main causes of neurologic disease and other potential neurologic consequences. Methods: There are currently no antivirals available, and vaccines are only available for some. Currently, only symptomatic treatment is available. Various herbal plants, vegetables, fruits, flowers, and microbes have been documented to exhibit antiviral activities possessing good tolerability and minimal side effects. Polyphenols and other phyto-constituents have been extensively studied against arboviruses and have demonstrated promising results. Results: This review article focuses on a potential new herbal formulation with strong antiviral properties against the current zika virus and accompanying symptoms, with intranasal administration as the preferred method for treating neurological symptoms. Conclusion: Natural anti-viral therapy plays an important role in contributing to antiviral drug development and in reducing the global infection burden of arboviruses.

Background: Naregamia alata is an endemic herb of Western Ghats with traditional medicinal uses and pharmacological activities, viz. anti-inflammatory, antioxidant, antipyretic, hepatoprotective and antidiabetic effects. However, no information is available on the phytoconstituents of N. alata responsible for antidiabetic activities. Objective: Isolation and identification of compound/s from the dichloromethane fraction of methanol extract of N. alata and to confirm the antidiabetic activity using streptozotocin-induced diabetic rat models. Methods: The DCM fraction obtained from the methanol extract of N. alata was fractionated using column chromatography. The fractions with in vivo antidiabetic activity were characterised chemically using GCMS, FTIR, and ¹H NMR to identify the phytochemicals responsible for the antidiabetic activities. Results: The study showed the antidiabetic effect of DCM fraction with the regulation of serum biochemical parameters. The chemical characterisation of the fractions responsible for the in vivo antidiabetic effect revealed the presence of hexadecanoic acid methyl ester and 13-docosenamide as two major compounds in one of the fractions (Fraction 1) and citronellol in another fraction (Fraction 2.2.1). Conclusion: The study highlights the role of hexadecanoic acid methyl ester, 13-docosenamide and citronellol in a reversal of serum biochemical parameters along with body weight in streptozotocin- induced diabetic rats to near normal suggesting the potential antidiabetic properties of these compounds.

The liver is an essential organ that aids in the metabolism and elimination of xenobiotics from the body and dysfunction of the liver is a serious health issue that concerns physicians, pharmaceutical companies, and regulatory bodies. The effects of numerous hazardous substances, particularly antibiotics, chemotherapeutics, carbon tetrachloride (CCl4), thioacetamide (TAA), and microorganisms on liver cells have been extensively researched. Synthetic drugs used to treat liver abnormalities in this condition can also harm the liver in other ways. The bioactivation of medicines into chemically reactive metabolites, which can interact with cellular macromolecules like proteins, lipids, and nucleic acids, causing protein malfunction, lipid peroxidation, DNA damage, and oxidative stress, causes liver damage. Natural medications have proven to preserve normal and useful liver stats while causing fewer adverse effects. The use of medicinal plants in the treatment of liver disorders has a long history. This review article aims to gather information about prospective phytochemicals from medicinal plants that have been investigated in modern scientific hepatotoxicity models. During this review process, we concluded that some medicinal plants were showing potent effects against liver damage due to their ability to minimize oxidative stress and modulate the metabolic pathway responsible for liver damage.

Background: Discovery of novel anti-cancer drugs from natural origin has increased tremendously due to the resistance of multiple chemotherapeutic drugs in breast cancer therapy and its high toxicity to undesirable side effects. Objective: The aim of the study was to investigate the bioactivity of secondary metabolites derived from Actinobacteria sp. BACSAS14 isolated from a vegetable farm in Vellore, Tamil Nadu, and India. Methods: Five actinomycetes strains were isolated and screened for antagonistic activity by the agar well diffusion method. Out of which, Actinobacteria sp. BACSAS14 exhibited potency, and its crude extract was tested for anti-inflammatory, anti-microbial, anti-cancer, and antioxidant potential. The Actinobacteria sp. BACSAS14 ethyl acetate extract was analyzed by Gas chromatography- mass spectrometry, Fourier-transform infrared spectroscopy, and Thin Layer Chromatography to determine the bioactive compounds. A drug interaction study with the anti-inflammatory protein COX-2, anti-oxidant protein lipoxygenase, and anti-cancer protein MT1-MMP was done by molecular docking analysis. Results: Maximum activity was found against Pseudomonas aeruginosa (19 mm) at a concentration of 500 μL. Maximum inhibitory activity was 98.8 ± 0.98 % at a concentration of 5 mg/mL with an IC50 value of 417.58 μg/mL. Maximum antioxidant activity was 67.87 ± 0.59% at a concentration of 5 mg/mL. At an extract concentration of 500 μg/mL, cell viability was found to be 31.62 ± 0.79 with an IC50 value of 365.23 μg/mL. The compound with the lowest binding energy was observed to be sulfurous acid, cyclohexylmethyl isohexyl ester. In-silico studies of sulfurous acid, cyclohexylmethyl isohexyl ester revealed promising anti-inflammatory, anti-oxidant and anticancer potential. Conclusion: The current study reported that the bioactive secondary metabolites of Actinobacteria sp. BACSAS14 retains anti-inflammatory, anti-cancer, and antioxidant properties. This is the first report stating the production of the metabolite sulfurous acid, cyclohexylmethyl isohexyl ester from Actinobacteria sp. BACSAS14.

Background: Because of their biological properties, phytochemicals have been essential to nutraceutical treatment for diabetes mellitus. Various phytoconstituents derived from Tinospora are reported to have immunomodulatory, anti-arthritis, antioxidant, anti-allergic cardio, and oxidatively- induced stress protection. Objectives: This study aimed to identify and characterize the key phytoconstituents of Tinospora cordifolia for their anti-inhibitory effects against α-amylase and α-glucosidase enzymes in controlling carbohydrate metabolism and potential drug molecule against Type II Diabetes Mellitus. Methods: Based upon the literature survey, various compounds of T. cardiofolia were deduced from Pubchem and protein structure from the protein data bank. Virtual screening used Pyrx with α-amylase and α-glucosidase. Compounds with the highest binding affinity score and 3-d interaction analysis were used to identify the potential inhibitors among various compounds. Pharmacokinetic studies for drug likeliness and toxicity properties were characterized using SWISS ADME and ADMETSAR webservers. Results: Based on their docking scores and binding affinities,, the biologically active compounds from T. cardifolia viz were observed. Isocolumbin, cordifoliside B, β-sitosterol, ecdysone, palmitoside E, Columbin and cordifoliside C interact with the active site amino acids of both the enzymes. Drug-likeness and pharmacophore studies showed that potential anti α- amylase and α- glucosidase inhibitors. Conclusion: The compounds' efficacy of the screened phytoconstituents from T.cardifolia as prospective therapeutic candidates can be due to their great affinity for the enzymes' catalytic region, which can cause a conformation change and result in a reduction in enzyme activity. This study's findings might indicate a way to create a new class of drugs.

Kaempferol, a natural flavonoid found in numerous fruits, vegetables, and herbs, possesses many pharmacological activities such as antioxidant, anti-inflammatory and anti-cancer. Kaempferol has low aqueous solubility and hence has poor oral bioavailability. Numerous promising techniques were used to enhance its absorption and structural transformation to deliver kaempferol. Novel pharmaceutical technologies, including nanotechnology, carrier complex and cocrystals have been established. However, this review discusses how to deliver kaempferol via topical route in many diseases. This is the earliest review that aims to provide updated information on chemistry, bioavailability, biosynthesis, therapeutic effects and available nanoformulations of kaempferol. It also provides future directions so that the overall bioavailability of kaempferol might be improved, and it may show expansive applications.

Background: The present research aimed to assess the relationship between free radical scavenging activity and oral hypoglycemic potential of methanol extract of the root of Cryptolepis buchanani in Albino Wistar rats. Objective: The following research aimed to study and evaluate the antidiabetic efficacy of the natural plant extracts Cryptolepis buchanani. Methods: Phytochemical screening was done to analyze, and in vitro, the antioxidant activity of plant root extract has been evaluated using DPPH assay and Fe⁺³ Reducing Power Assay. Streptozotocin at a 60 mg/kg dose was used to induce diabetes in albino Wistar rats, which was then treated with methanol extracts (125 and 250 mg/kg, PO) to evaluate antidiabetic activity. Results: The results indicated that methanol extract of the root of Cryptolepis Buchanan had shown its promising antidiabetic potential at a dose of 250 mg/kg in experimental diabetic Wistar rats, which may be linked to its antioxidant property. Conclusion: This experimental study revealed that the extract could potentially alleviate the augmented oxidative state correlated with diabetes. The marked reduction in blood glucose levels proves the hypoglycemic activity of the plant.

Background: In recent years, 2-aminobenzothiazoles were reported as antibacterial, antihelmintic, antitumor, antimalarial, antiviral, analgesic and anti-inflammatory agents. Objectives: The study aimed to explore new potential 2-aminobenzothiazoles as antibacterial and anthelmintic agents. Methods: A favorable two-step method was used for the synthesis of new 2-aminobenzothiazole derivatives (4a-4j) by Schiff base. All synthesized compounds were tested for antibacterial activity using an in vitro cup-plate method and antihelmintic activity by recording in vitro earthworm paralysis and death time. Pharmacokinetics in silico studies were performed to predict the drug performance in the body using the Molinspiration kit. The molecular docking was performed to check the catalytic binding site between the dihydrofolate reductase and synthesized compounds (4a-4j). Results: The compound 4d emerged as the most effective vermifuge and vermicide among all tested compounds. The compounds 4c, 4f, 4g, 4i and 4j were examined as highly potent against grampositive bacteria. The compounds 4b, 4h, and 4i showed maximum inhibition against gramnegative bacteria. In support of antibacterial activity, the compounds 4c and 4j showed good binding orientation in the catalytic binding pocket of the DHFR receptor (PDB ID: 4LAE). These synthesized compounds could have evolved to shape orally active compounds shown in pharmacokinetics in silico studies. Conclusion: The research outcomes showed that explored 2-aminobenzothiazoles have good antibacterial and anthelmintic activity.