Current Bioactive Compounds - Volume 20, Issue 6, 2024

Background: One of the most crucial heterocycles is piperazine for the creation of novel medication candidates with a variety of medicinal applications. The piperazine moiety is a cyclic compound with four carbon atoms and two nitrogen atoms in positions 1 and 4. Objective: The objective of this studty is the development of 1-((3,4-dimethoxyphenyl) (substitutedphenyl) substituted -piperazine (A1-A10) analogs via the one-pot synthesis method and evaluation for their preliminary antibacterial, antifungal, antimycobacterial, antioxidant, and antimalarial activity. Methods: Desired piperazine derivatives were obtained in a single step reaction using piperazine, aldehydes, and boronic acid derivatives. The structures of all newly synthesized compounds have been established based on analytical and spectral data. An in silico molecular docking study was carried out for the series. Results: The spectral data using IR, ¹H NMR, and ¹³C NMR and mass spectra confirmed the structure of the synthesized compounds. Compounds A6 and A10 were found to be the most promising agents for antimalarial activity. A1-A10 showed a higher IC50 value and found less antioxidant activity. Some of the compounds showed higher potency when compared to the standard drugs in this antimicrobial study. Conclusion: The structure-activity study showed that changes in substituents either on aldehyde, piperazine, or boronic acid derivatives can lead to potential active compounds. These facts make the compounds interesting candidates for further evaluation of their efficacy in the treatment of microbial, tubercular and malarial diseases.

Chalcone is a bioactive flavonoid found in various plants, such as Angelica archangelica, Pueraria lobata, and Glycyrrhiza glabra. It has been studied extensively in the field of pharmaceutical sciences due to its significant role in therapeutic potential including antibacterial, antiinflammatory, analgesic, cytotoxic, and antitumor properties. A plenty of study indicated numerous chalcone derivatives exhibit enhanced potency and reduced toxicity as compared to natural analogues. In this review, we have introduced chalcone and its various derivatives including 1- naphthylacetophenone, 2-benzimidazolyl, 2-furoyloxy, 3-(furan-2-yl)pyrazol-4-yl, 4'-alkoxy, 4- anilinoquinolinyl, 4-aryloxyquinazolines, acridine, benzamide, benzenesulfonamide, bischalcone, cinnamoylthiazoles, D-glucosyl azides, dialkylamino, dihydropyrimidinone, indole, isoquinoline, ligustrazine, morpholinothiazole, naphthalene, quinoline, sulphonamide, thiazoleimidazopyridine, thienyl, thiophene, triazines, triazole-benzimidazole, tri-methoxyphenyl, and α- trifluoromethyl hybrids which display activity against various cancer cell lines, such as breast cancer, prostate cancer, colon cancer, lung cancer, cervical cancer, and liver cancer.

Background: One of the main risk factors for atherosclerosis is hypercholesterolemia. Objective: This study aimed to assess hypercholesterolemia's effect on the liver, heart, and kidney and the impact of Syngonium podophyllum L. leaves methanolic extract as a treating agent in a rat model. Methods: Flavonoid components were isolated and identified from the methanolic extract of Syngonium podophyllum L. leaves. Total serum leptin, total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), triglycerides (TG), aspartate and alanine aminotransferases (AST and ALT), urea, and creatinine levels were all measured as part of the biochemical evaluation. The liver tissue was tested for levels of malondialdehyde (MDA), glutathione (GSH), superoxide dismutase (SOD), and DNA fragmentation. Results: Thirty-nine compounds were identified by GC/MS profiling of the n-hexane fraction of Syngonium podophyllum L leaves. The major volatile constituents were decane, 4-methyl, decane, N-acetyl 3-pentenyl, 1-amine, 2-methyl, 1-hexene, and 3-hydroxy, propanenitrile, while the major phenolic compounds isolated from methanolic extract were luteolin-7- α-L rhamnoside-4'- O-β-glucopyranoside (1), apigenin 6, 8-di-C-β-glucopyranoside (vicenin 2) (2), quercetin-3-O- α-L-rhamnoside (3), quercetin-7-O-β-glucoside compound (4), luteolin-7-O-β-glucoside (5), 5- hydroxy-6,7,8,4'-tetramethoxy flavone (6), gallic acid (7) and quercetin (8). Hypercholesterolemic rats revealed significant alterations (p ≤ 0.05) in the lipid profile, liver and kidney function, DNA fragmentation pattern and antioxidant indices. With oral cholesterol administration of 30 mg/0.3 mL (0.7% tween)/rats fed a high-fat diet for nine weeks, treatment with leaves extract (250 mg/kg body weight) was able to restore all biochemical parameters as well as the architectures of the liver and heart. Conclusion: Due to its abundance in physiologically active phenolic and flavonoid components, the methanolic extract of Syngonium podophyllum L. leaves successfully served as a hypolipidemic, anti-atherosclerotic, and antioxidant therapeutic agent.

Objectives: The study aimed to assess the neuroprotective effect of Boswellia serrata against 3-NP-induced experimental Huntington's disease. Background: Previous studies have shown Boswellia to have sedative, analgesic, and anti-tumour effects. Boswellia serrata yields four pentacyclic triterpene acids and boswellic acid, a bioactive substance that prevents leukotriene biogenesis. Methods: The potential neuroprotective effect of Boswellia serrata against 3-nitro propionic acid (3-NP)-induced Huntington's disease (HD) was examined at oral doses of 45 mg/kg, 90 mg/kg, and 180 mg/kg. In this study, HD was induced by 3-NP at a dose of 10 mg/kg in Wistar rats. The study used 56 Wistar rats (8 per group) for biochemical (inflammatory markers, acetylcholinesterase activity) and behavioural (elevated plus maze, Y-maze, open-field, tail suspension tests, etc.) assessments. Additionally, a histological examination of the brain was carried out. In addition, the analysis of Boswellia serrata extract was performed by different analytical techniques, like UV spectrophotometer, FTIR, and HPLC methods. Results: In the brain, succinate dehydrogenase is a mitochondrial enzyme irreversibly inhibited by 3-NP. Administration of 3-NP resulted in HD with altered behavioural and motor changes in rats. Treatment with Boswellia serrata resulted in remarkable protection of rats against 3-NP-induced behaviour and motor deficits in a dose-dependent manner. Moreover, in rats administered with 3-NP, Boswellia serrata improved memory performance and lowered levels of inflammatory biomarkers. These results have also been supported by histopathological analysis. Acetyl-11-keto-p-boswellic acid was found to be the main active component of Boswellia serrata extract. Conclusion: Boswellia serrata at a dose of 180 mg/kg exhibited better protection compared to the other doses against HD induced by 3-NP. More detailed studies based on molecular targets are needed for the Boswellia serrata to transition from the bench to the bedside for use as an adjuvant in HD patients.

Objective: To study the cytotoxic effect of palmitic acid on myoblasts in vitro and the influence of this toxicant on the expression of myostatin mRNA in myoblast culture. Methods: To research the protective action against these processes of a compound with antioxidant activity, for which 2-ethyl-6-methyl-3-hydroxypyridine malate (ethoxidol) was chosen. Results: Our studies have shown that palmitic acid has a noticeable cytostatic effect on myoblasts in vitro, significantly suppressing their proliferation: the rate of MTT recovery in myoblasts treated with palmitate was only 9.6% of that rate in control myoblasts. In experiments, it was shown that palmitic acid slightly activated the expression of myostatin mRNA. At the same time, the protective effect of 2-ethyl-6-methyl-3-hydroxypyridine malate was not so pronounced. Conclusion: The results of our research indicate that the activation of myostatin synthesis is not one of the main causes of the development of myodystrophy in obese people or people following a high-lipid diet, while the direct cytotoxic effect of palmitic acid on myoblasts is. It is obvious that the use of antioxidants such as ethoxidol has a protective effect on myoblasts in the experiment and may have a certain potential in clinical practice.

Background: Helicobacter Pylori is widely present in human populations, making it one of the most common bacteria found in humans. Due to the drug's side effects, extensive research is being done to find new effective nanoparticles against Helicobacter Pylori in the world. Therefore, this systematic review aims to investigate nanoparticles' antimicrobial activities against Helicobacter Pylori. Methods: All articles published from 2000 to 2023 from Scopus, PubMed, Science Direct, Cochrane, and Ovid databases with keywords Helicobacter Pylori, H.pylori, nanoparticles, solid lipid NPS, and lipid nanocarrier were extracted and transferred to EndNote X9 software by two researchers. Results: During the first stage, 280 articles were chosen. Following the application of the eligibility criteria for inclusion/exclusion, 37 studies were ultimately selected, considering the removal of duplicates, irrelevant articles, and those containing complete text. In the present systematic review study, most nanoparticles used against Helicobacter Pylori were polymericbased nanoparticles. Conclusion: The results indicate the high potential of various nanoparticles against Helicobacter Pylori. Therefore, the results show that these nanoparticles have the potential to prepare anti- Helicobacter Pylori nanoparticles. In addition, these nanoparticles have fewer side effects than chemical drugs.