Current Bioactive Compounds - Volume 17, Issue 10, 2021

Background: Many research papers have demonstrated that Nigella has neurotropic properties, and it has also been shown that Nigella seeds have several activities, such as analgesic, antiepileptic, anxiolytic, antidepressant, and psychostimulant activities. Methods: Databases such as PubMed, Science Direct, Scopus, and Google Scholar were used. Results: The orientation towards this type of research has become more accentuated to enhance and detail the pharmacological properties of medicinal, aromatic plants. Conclusion: The present review reveals and combines the experimental research studies carried out to demonstrate the central effects of Nigella.

Background: Literature evidence as well as traditional uses of genus Alphonsea reveal significant antimicrobial and anti-oxidant activitiesencouraging to consider A. madraspatana to have potent antimicrobials, there by offering potential adjuncts to synthesize improved antimicrobial Silver nanoparticles (AgNPs). The objective of the present exposition is to optimize reaction parameters to synthesize antimicrobial Biogenic Silver nanoparticles (BAgNPs) from the extract of A. madraspatana leaves (AML) and to evaluate the effect against bacteria. Methods: BAgNPs were synthesized by the optimized reaction. The Synthesized nanoparticles were characterized by UV, IR, ICP-MS and XRD analysis. The antibacterial potency of optimized BAgNPs was evaluated against E. coli by comparing with positive controls. Results: Results of the optimization process indicate nanoscale BAgNPs were produced at 45°C for 120 min at pH 8 with 1:5 volume ratio of AgNO3 and extract. Optimized BAgNPs exhibits relatively higher antimicrobial activity (31±1mm) compared to Ciprofloxacin (27±1mm) and marketed nanosilver (28± 2 mm). The developed BAgNPs show comparable biofilm inhibition (86.50%) as compared to marketed nanosilver (88.10%) and Ciprofloxacin (83.10%). Conclusion: Experimental evidence suggests methanolic extract of AML under predefined conditions, which successfully generate nano-template of silver with better antibacterial response against E. coli.

Background: The current interest in natural antioxidants from vegetable sources, mainly in bioactive antioxidants, has been increasing in Brazil. The Hibiscus sabdariffa L. is rich in bioactive compounds, besides having antioxidant and antimicrobial properties. Objective: This study aimed to evaluate the antioxidant effect of hibiscus extract on the oxidative stability of soybean oil in an accelerated storage test. Methods: The ethanolic extracts of calyces and hibiscus seeds were evaluated for total phenolic compounds and antioxidant activity using DPPH, FRAP, and β-carotene/linoleic acid. The treatments identified as OS, Tocopherol, Extract, and Mixture, were prepared and submitted to accelerated storage at 60°C. The samples were analyzed on days 0, 6, and 12 for peroxides index, p-anisidine, total oxidation value, oxidative stability, and tocopherols. Results: The extract of calyces of hibiscus presented higher amounts of total phenolic compounds and antioxidant activity. Therefore, it was added to soybean oil. The Extract treatment promoted greater efficiency to inhibit the formation of primary and secondary compounds of lipid oxidation. It provided high oxidative stability to the soybean oil, in addition to greater retention of tocopherols, mainly α- and γ-tocopherol isomers. Conclusion: Among the treatments studied, Extract promoted greater efficiency in the inhibition of the formation of primary and secondary compounds of lipid oxidation, besides providing greater oxidative stability and greater retention of tocopherols during storage.

Aims: Antihyperlipidemic and antiobesity potential of a fixed dose combination of Aquilaria agallocha & Borago officinalis along with its comparative evaluation with Atorvastatin & Orlistat. Background: Hyperlipidemia and obesity are common and challenging health problems throughout the world. These are the conditions in which increased lipids level in blood are the risk factors for atherosclerosis, coronary artery disease, and cerebral vascular diseases. In the present study, the fixed-dose combination of absolute ethanolic extract of Aquilaria agallocha and aqueous extract of Borago officinalis was examined for its antihyperlipidemic effect and antiobesity activity in the Sprague Dawley rats. Objective: A suitable & established experimental model of hyperlipidemia and obesity based on literature survey has been selected. Comparative evaluation of fixed dose combination with selected standard drug against the established model. Compilation of results and statistical analysis. Methods: Drugs and Chemicals: Atorvastatin solution, Orlistat solution, Formalin solution Animals: sprague dawley rats of 150-200 g of either sex were used for the study. Animals were habituated to laboratory conditions for 48 hours prior to experimental protocol to minimize if any of nonspecific stress. All the studies conducted were approve by the Institutional Animal Ethical Committee (IAEC) of Faculty of Pharmacy, Integral University Lucknow (Reg. no. 1213/PO/Re/S/08/CPCSEA, 5th June 2008) having approval no. IU/IAEC/18/32. High fat diet induced Dyslipidemia and obesity: Baseline characteristics of obesity and hyperlipedimia induced by high fat diet in Sprague dawley rats were maintained on normal pellet diet (NPD) for one week before the commencement of experiment. After one week rats were randomly assigned into normal and obese group and fed with NPD and High fat diet and libitum respectively for one week.The food intake, body weight gain ,and lipid profile were carried out on day 8 of dietary manipulation to assess the baseline characteristics of obesity and hyperlipidemia induced by high fat diet in Sprague dawley rats. Results: The result of the study shows that the ethanolic extract of the FDC of aquilaria agallocha & borago officinalis has significant anti-hyperlipidemic and anti-obesity activity against High- fat diet-induced hyperlipidemia and obesity compared to atorvastatin (10 mg/kg) and orlistat (pure drug 10mg/kg). Conclusion: The present study shows that pretreatment with ethanolic extract of FDC of Aquilaria agallocha & Borago officinalis significantly prevented from hyperlipidemia and obesity and decreased the levels of diagnostic marker enzymes significantly. At low dose (Borago officinalis 100 mg/kg + Aquilaria agallocha 250 mg/kg b.w.) ) ethanolic extract of FDC of Aquilaria agallocha & Borago officinalis showed moderate protection against Hyperlipidemia and Obesity. At high dose (Borago officinalis 200 mg/kg + Aquilaria agallocha 500 mg/kg b.w.) ethanolic extract of FDC of Aquilaria agallocha & Borago officinalis showed marked protection against High fat diet induced hyperlipidemia and obesity as well as by biochemical estimations of Lipid profile compare to the standard Atorvastatin(10mg/kg) and Orlistat(10mg/kg). Thus it concludes that ethanolic extract of FDC of Aquilaria agallocha & Borago officinalis possesses potent against high fat diet induced hyperlipidemia and obesity.

Background: Dillenia indica L. (Dilleniaceae) and Anogeissus leiocarpus (DC.) Guill. & Perr. (Combretaceae) are used in traditional Nigerian medicine to treat various forms of cancer. This study investigated the cytotoxic effects of these plant extracts using COV434 granulosa tumor and MCF-7 breast cancer cells. Methods: Samples of D. indica and A. leiocarpus were collected in Ibadan, Nigeria, air-dried, and extracted with methanol. Cell viability and cytotoxicity were determined using CellTiter-Glo® 2.0 assay at concentrations from 1 to 100 μg/mL. Caspase activity and apoptosis were determined using Caspase-Glo® 3/7, Caspase-Glo® 8, and ApoTox-Glo™ triplex assays, and qPCR. Autophagy was measured using a Cyto-ID Autophagy Detection Kit. Results: In COV434, aqueous partitions of A. leiocarpus root (ALR-Aq) and stem bark (ALS-Aq) had IC50s of 23.5 and 26.7 μg/mL, respectively. In MCF-7 cells, the ALR MeOH extract had IC50 of 12.75 μg/mL, while the DIS-Aq had IC50 of 65.28 μg/mL. None of the extracts inhibited the growth of human osteoblasts or rat myoblasts at similar concentrations. Treatment with ALR-Aq and DIS-Aq induced mitochondrial apoptosis in MCF-7 and COV434. Both ALR-Aq and DIS-Aq induced autophagy in COV434 cells, while ALR-Aq induced autophagy in MCF-7 cells. Ellagic acid (IC50 of 3.27μg/mL in COV434 cells) was isolated from ALR-Aq using bioassay-guided fractionation. Conclusion: DIS-Aq and ALR-Aq induced apoptosis in MCF-7 and COV434 cancer cells. Ellagic acid was isolated as the active constituent. Taken together, these data suggest that both plant extracts have strong anti-proliferative effects, and further investigation for their anticancer effects is warranted.

Background: The Ethanolic Extract of Pyrus communis L. fruit (EEPC) was assessed for hepatoprotective and in vitro antiradical activity against carbon tetrachloride-induced hepatotoxicity in rat’s liver. Methods: The degree of hepatoprotection was screened by measuring biochemical parameters, including serum Alanine Transaminase (ALT), Aspartate Transaminase (AST), Alkaline Phosphatase (ALP), Total Albumin (TA), Total Protein (TP) and Total Bilirubin (TB). The antiradical activity was assessed using 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydrogen peroxide and nitric oxide free radical scavenging property. The hepatoprotective effects of the extract were compared with Silymarin used as a standard drug (100 mg/kg, p.o, bodyweight). Results: The ethanolic extract of the fruit has the capabilities to scavenge free radicals, in vitro, respectively. Additionally, the ethanolic extract (200 mg/kg and 400 mg/kg, p.o, bodyweight) exhibited marked hepatoprotective action regarding CCl4 intoxicated rodents in a dose-dependent manner. EEPC at a dose of 400mg/kg could afford significant dose-dependent protection against CCl4 induced hepatocellular injury. Conclusion: Biochemical samples obtained from the animals treated with ethanolic extracts (400mg/kg, body weight) showed a significant decrease in the levels of serum markers indicating hepatic cell protection.

Background: The ethanomedicinal importance of Moringa concanensis Nimmo plant is reflected in the Ayurvedic and traditional system of medicine. It has vast usage in Ayurvedic preparation and diabetes management. Aims of the Study: The research was centered on bringing out the hyperglycemic capabilities of Moringa concanensis Nimmo leaves, and their ethanolic extract (PE) on alloxan monohydrate (AXM) induced diabetic rat model. Materials and Methods: Wistar rats were made diabetic by AXM and treated with PE (200 mg/kg body weight) and glibenclamide as the standard drug. All essential parameters like fasting blood glucose (FBS), post-prandial blood glucose (PPBS), AST, ALT, ALP, ACP, LDH, and oxidative stress markers were measured. Also, to observe β-cells structures, histology of the pancreas was studied. Results: The non-toxicity of PE dose was confirmed by an acute toxicity study. This study model helped determine the anti-hyperglycemic effects of PE by decreasing FBS and PPBS levels in diabetic rats. It also enhanced oxidative stress by decreasing MDA levels and elevating the GSH and SOD. The histopathological analysis helped us study the structural decay of β-cells of pancreatic tissues in diabetic rats. PE potential was confirmed by serum enzymes AST, ALT, ALP, ACP, and LDH as it showed a significant decrease in diabetic rats. Conclusion: It was confirmed from the data that PE is efficient in the governance and control of diabetes. Therefore, there is a need to work at the molecular level to utilize its potential for the benefit of society.

Background: Marine actinobacteria are a potential resource for natural products; their secondary bioactive metabolites have shown several biological activities. Most of the isolated and identified actinobacteria in Algeria were usually explored from caves, Saharan soil or palm groves. The marine ecosystem is poorly explored and documented. Methods: Five Streptomyces strains producing bioactive compounds were isolated from Rachgoun Island located in Western Algeria and characterised phenotypically and genotypically using microbiological and 16S rRNA sequencing methods, respectively. The crude extract of the most representative strain “Streptomyces sp. strain SM2.4” and its seven active fractions were characterised by GC/MS analysis. Results: Streptomyces sp. strain SM2.4 revealed the strongest activity against the Gram-positive bacteria Staphylococcus aureus and Bacillus subtilis, the fungus Aspergillus niger and was inactive against Gram-negative bacteria. GC/MS analysis of the methylated crude extract of Streptomyces sp. strain SM2.4 revealed the presence of 11 major compounds, including fatty acids methyl ester (12-methyltridecanoic acid methyl ester, 9-hexadecenoic acid methyl ester, hexadecanoic acid methyl ester, 14-methylhexadecanoic acid methyl ester and 16-methylheptadecanoic acid methyl ester), 2,4-di-tert-butylphenol, (4S,4aS,8aR)-4,8a-dimethyloctahydro-4a(2H)-naphthalenol (geosmin), 2,4-dimethylbenzaldehyde, 3,4-difluorobenzaldehyde, dimethylfuran-2,4-dicarboxylate and pyrrolo(1,2-a)pyrazine-1,4-dione, hexahydro-3-(2-methylpropyl)-. Partial purification of the crude extract by Thin-layer chromatography provided seven active fractions, which were tested by radial diffusion assay. GC/MS analysis of the active TLC-fractions revealed the presence of a mixture of active compounds from which 2- (bromomethyl)-2-(2-methylphenyl)-1,3-dioxolane was found to be a new 1,3 dioxolane derivative. Furthermore, 3,4-dimethylbenzamide and pyrido[2,3-d] pyridazine-1,4-dione, hexahydro- 3-(2-methylpropyl)-, were extracted for the first time from a natural source. Conclusion: Our study reveals that marine Streptomyces sp. strain SM2.4 has an interesting antimicrobial potential due to its panel of bioactive compounds.

Background: Free radicals can easily damage DNA, proteins and lipids within the tissue. Anti-oxidants from natural sources can diminish the actions of free radicals. The current study deals with the chemical composition and antioxidant activity of the leaves of Zanthoxylum oxyphyllum Edgew. Methods: The antioxidant activities for DPPH, FRAP, ABTS radicals, phosphomolybdate assay, reducing power, and chelating power assay were evaluated of ethanol (ET), methanol (ME), chloroform (CH), ethyl acetate (EA), and petroleum ether (PE) extracts of the leaves. The Density Functional Theory (DFT) study was carried out on major identified phytochemicals to evaluate bioactive molecules responsible for the antioxidant activity. Results: It was observed that the ME extract showed the most potent scavenging activity in DPPH, FRAP, ABTS radicals, phosphomolybdate assay, reducing power, and chelating power assay. The phenolic acids and flavonoids like quercetin, gallic acid, sinapic acid, etc. were identified. The DFT study was done for major phytochemicals of ME extract to evaluate the most responsible bioactive molecule for antioxidant activity. The Gallic acid exhibited the lowest bond dissociation energy (BDE) of 314.9 kcal/mol in gas, 309.2 kcal/mol in methanol, respectively, along with the highest value of radical stabilization energy (RSE), 29.5 kcal/mol. Conclusion: Gallic acid was found to be the most responsible antioxidant among the other compounds, and ME the best solvent system for extraction, followed by CH.