Current Bioactive Compounds - Volume 18, Issue 10, 2022

Background: Diabetes has become a considerably more frequent condition and has increased alarmingly in recent years, possibly due to the adoption of modern lifestyle and food habits. The two prominent features of diabetes mellitus are high blood glucose and insulin deficiency, leading to severe consequences. Developing next-generation anti-diabetic medicines with fewer side effects has been a major focus in this situation. Objective: This research aimed to investigate the total phenolic and flavonoid content, antioxidant, antibacterial, α-amylase, and α-glucosidase inhibition activity, as well as in silico analysis of Mimosa pudica L. Methods: The inhibitory activity against α-amylase and α-glucosidase was performed using CNPG3 and PNPG, respectively. Antioxidant activity was estimated using DPPH free radical scavenging assay. The well diffusion method was used for the antibacterial. Using folin- ciocalteu’s reagent, the total phenolic content was determined. The total flavonoid content was determined using the aluminium trichloride method. In addition, molecular docking was performed using autodock vina. Results: Inhibition of α-glucosidase (IC50 = 1.059±0.14μg/mL) was found to be more significant than α-amylase (IC50 = 164.9±0.95μg/mL). The plant was also found to have antioxidant activity (IC50 = 8.207 ±0.23μg/mL), as well as antibacterial activity against Staphylococcus aureus (ZOI = 13mm) and Bacillus subtilis (ZOI = 10mm). Similarly, the total phenolic and flavonoid content was found to be 177.93±1.8 mg GAE/g, and 19.747±6.11 mg QE/g, respectively. In addition, compounds (stigmasterol, quercetin, and avicularin) isolated from M. pudica showed perfect binding to the enzyme’s active site. Conclusion: Mimosa pudica of Nepalese origin possess potent inhibition against digestive enzymes. Therefore, M. pudica can be used as an alternative therapeutic source to combat the global threat of diabetes.

Background: Traditional medicine has used Mimosa pudica Linn. for diabetes treatment. This study evaluates the antidiabetic and renoprotective effects of the ethyl acetate fraction of M. pudica leaves on streptozotocin-induced diabetes in mice. Methods: The cold maceration method was used to extract M. pudica leaves with 80% ethanol at room temperature. Ethyl acetate (EtOAc) fraction was obtained from the M. pudica leaves extract by successively partitioning with different solvents. Mice were induced diabetes type 2 by streptozotocin (STZ) at a low dose and treated with EtOAc fraction of M. pudica leaves at 50 mg/kg and 100 mg/kg b.w for 60 days. After 24 hours of the final dose of therapy, the mice were sacrificed to extract blood and kidney tissues for biochemical and histopathological analysis. Results: The EtOAc fraction of M. pudica leaves showed strong activity in improving glucose concentration in the oral glucose tolerance test. Our results showed that EtOAc fraction significantly decreased levels of glucose, total cholesterol (TC), low-density lipoprotein (LDL), and triglyceride (TG) and increased the level of high-density lipoprotein (HDL), and protected kidneys against damage in mice. EtOAc fraction also increased the levels of antioxidant enzymes, including catalase (CAT), glutathione peroxidase (GPx), and superoxide dismutase (SOD), and decreased malondialdehyde (MDA) formation and pro-inflammatory cytokines (IL-1β and TNF-α) in kidney tissues. Moreover, the renoprotective effect was also observed in the histopathological analysis. Conclusion: Our findings support the fact that the EtOAc fraction of M. pudica leaves has potent anti-diabetic nephropathy activity by decreasing pro-inflammatory cytokines and improving antioxidant levels.

Background: Heterocyclic compounds possess a wide variety of roles in most fields of science, such as biochemistry, medicinal chemistry, veterinary products, agrochemicals, etc. Triazole, a heterocycle compound, serves as a building block for various compounds having multiple applications, mostly in medicine. Triazole is a five-membered ring containing compounds that occur in nature, found in several microorganisms, fungi, and marine organisms. The triazole nucleus is a boon for researchers with significant scope in the long-term. Triazole derivatives possess various pharmacological properties due to their ability to exert several non-covalent interactions, which can improve the solubility and the ability to bind to bimolecular targets. Objective: We focused on the structure-activity relationship of triazole derivatives possessing various biological activities such as antibacterial, antifungal, anticonvulsant, antidiabetic, antimalarial, analgesic, anti-inflammatory, antioxidant, antidepressant, antitubercular, anticancer, etc. Results: This study revealed the significance of certain substituents on triazole nuclei for different biological activities. Conclusion: From this, we conclude that the triazole nucleus will be a lead for further research on drug discovery.

Background: This study aimed to isolate and analyse the essential oils of Eugenia caryophyllus flower buds and Citrus reticulata peels for antioxidant and antibacterial properties. Methods: By using the DPPH (2,2-diphenyl-1-picryl-hydrazyl-hydrate) free radical method and the ferric reducing antioxidant power (FRAP) method, the antioxidant activities of total volatile oil components of both oils were assessed. Agar well diffusion and dilution were used to test antibacterial activity. Results: Optical rotation (0.95 and 1.01), weight per mL (1.03 and 1.06), and refractive index (1.52 and 1.53) were all tested for both oils. The existence of a total of 26 and 28 most important volatile chemical components in oils produced from Eugenia caryophyllus and Citrus reticulata, respectively, was determined by GC-MS chemical analysis of the total volatile component. Retention time in a Gas Chromatography (GC) technique was used to identify the components. The mass spectral database was used to identify the values of oil components. The predominant components were eugenol (77.08%) in Eugenia caryophyllus oil and limonene (78.46%) in Citrus reticulate oil. Eugenia caryophyllus oil has strong antibacterial action against microorganisms like S. pyrogenes, with a ZOI of 15.90–26.84 mm, followed by oil from Citrus reticulata peels with a ZOI of 14.60– 22.82 mm. Conclusion: The presence of terpenes and phenolics in both essential oils resulted in substantial antioxidant activity. Agar well diffusion and dilution were used to test antibacterial activity. In the concentration range of 5–100 mg/mL, both essential oils demonstrated good bacteriostatic and bactericidal activity against microbial strains.

Background: Aristolochia longa L. (Aristolochiaceae), known as Berreztam, is frequently used in traditional medicine to manage several diseases and has been the subject of several studies. However, its inhibitory effect on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) has not yet been reported. Thus, the present work aimed to study the anticholinesterase and antioxidant activities of extracts from different parts of A. longa from the Mila region (Algeria). Methods: Phytochemical screening and quantitative determination of total phenolic, flavonoids, and flavonols were performed by colorimetric methods. The antioxidant activity was evaluated using four complementary tests (ABTS, FRAP, CUPRAC, and β-carotene-linoleic acid), and the inhibitory effect of the extracts on AChE and BChE was carried out by Elman’s method. Results: Polyphenols, flavonoids, tannins, carbohydrates, and terpenes were revealed in the extracts, while saponins, alkaloids, anthraquinones, anthocyanins, and mucilages were absent. The plant was found to have high levels of phenolic compounds (values between 46.33 ± 8.39 176.56 ± 4.00 mg/g), with the leaves being found to be the richest part. Methanolic extract of leaves and stems showed the highest antioxidant activity evaluated. The extracts showed negligible inhibitory effect on AChE but showed a potential effect on BChE, especially the methanolic extract of roots was the most potent (IC50=23.09 ± 1.81 μg/mL). Conclusion: These results suggest a possible use of the different parts of Aristolochia longa as a source of bioactive compounds endowed with antioxidant and anti-butyrylcholinesterase properties.

Background: Peganum harmala L. is a medicinal herbal plant widely used in traditional medicine in various countries, especially in Algeria. This study aimed to carry out the extraction of P. harmala seeds and to evaluate the antioxidant and antihemolytic potentials of 100 mg/kg methanol extract in plasma, blood, and liver of Swiss albino mice. Methods: The antioxidant capacity of the plasma samples was performed using free radical scavenging (DPPH assay) and reducing power activities. However, the antihemolytic effect of methanol extract was measured in the blood induced by tBH. The biomarkers of oxidative stress were evaluated in liver tissues by measuring the activity of catalase enzyme (CAT), and the level of GSH and MDA products. Results: The results showed that 100 mg/kg of MOHE did not show any significant changes in plasma antioxidant capacity by DPPH assay when we compared with a control group (32.70 ± 4,45 %), however, the reducing power capacity of plasma is remarkable in methanolic extract and VitC groups. Fifty percent of red blood cell lysis was calculated (HT50) for measuring the antihemolytic effect, the results showed that MOHEhad a protective effect against RBC hemolysis with HT50 = 78,51 ± 11,32 min. In addition, MOHE increases the activity of CAT, GSH levels whereas it decreases the MDA levels in the homogenate liver, which demonstrates that MOHE inhibits the lipid peroxidation in the liver. Conclusion: This plant has a strong pharmacological power due to its secondary metabolite. However, its uses for therapeutic purposes is not without danger and exposes the risk of intoxication.

Background: Aquatic organisms are considered to be an important source of bioactive peptides with a high antioxidant and antihypertensive capacity. Therefore, the objective of this study was to hydrolyse peptide fractions from white shrimp (Litopenaeus vannamei) muscle by Alcalase and Protamex and to evaluate the angiotensin I-converting enzyme (ACE) inhibitory and the antioxidant activities. Methods: Protein hydrolysates of White shrimp were obtained by enzymatic hydrolysis using Alcalase and Protamex until the degree of hydrolysis reached 10% and 20%. Peptide fractions were obtained from White shrimp protein hydrolysates by ultrafiltration using membranes with sizes of 10 and 3 kDa. The antioxidant activity was evaluated for the three peptide fractions (F1: >10 kDa, F2: 3-10 kDa and F3: <3 kDa). To measure the antihypertensive activity, fractions with molecular sizes of less than 3 kDa were used. Results: The fractions obtained with Alcalase showed greater inhibitory effects on the ACE. In general, the molecular weight of the fractions influenced the antioxidant activity, with fractions smaller than 3 kDa having a high capacity for sequestering the DPPH radical, while peptide fractions with a size greater than 10 kDa presented higher reducing power. However, in capturing the ABTS radical, a high antioxidant capacity was observed for both fractions. Conclusion: The results suggest white shrimp would be an attractive raw material for the manufacture of antioxidant and anti-hypertensive nutraceutical ingredients.

Background: Schiff bases are organic compounds and play a vital role in making biologically active compounds in various fields of chemistry. It shows antioxidant, antidepressant, antimalarial, anti-inflammatory, antiglycation, and antimicrobial activity. Objective: Our current study is focused on synthesizing thirty-four 2-mercaptobenzimidazole (MBI) based novel hydrazone derivatives (9-42) which were examined for antioxidant free radical scavenging activity via both 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydrogen peroxide (H2O2) assay and explored their alpha-glucosidase inhibitory potential at various concentrations. Methods: Multistep reactions were involved in the synthesis of 2-mercaptobenzimidazole-based hydrazone derivatives. All steps of the reaction were carried out under different conditions through a reflux condenser to get the final target products, and the reaction was monitored regularly in each step through thin layer chromatography (TLC). The antioxidant and α-glucosidase inhibition assay was performed. Results: Obtained results of antioxidants confirmed that compounds 42 (IC50 = 27.21μg/mL), 36 (IC50 = 27.90μg/mL), 23 (IC50 = 28.10μg/mL) and 35 (IC50 = 45.60μg/mL) possess excellent potential activity compared to standard ascorbic acid having (IC50 = 60.15 μg/mL) in DPPH assay. While in the case of H2O2 three compounds 38 (IC50 = 51.45 μg/mL), 15 (IC50 = 53.50 μg/mL), and 42 (IC50 = 60.42 μg/mL) showed excellent activity as compared to standard Gallic acid having (IC50= 60.67 μg/mL). In the screened compounds against alpha-glucosidase, compound 14 (IC50 = 162 μg/mL) was found to be the most active in the whole series. Another active compound 42 (IC50 = 237μg/mL) possessed moderate inhibitory potency against α-glucosidase enzyme. Conclusion: The different biological activities of these novel compounds may be due to different groups in the main skeleton of 2-mercaptobenzimidazole. Further experimental analysis and assessment of these compounds are important because they may lead to better antioxidants used in foods, cosmetics, and health-related products and act as antidiabetic drug development.

Background: Chalcone and flavone moieties play an important role in medicinal chemistry for the development of potential therapeutic agents. These two derivatives serve a wide range of applications in recent studies and are promising lead molecules for the synthesis of compounds with vast therapeutic utility for many diseases, particularly for cancer therapy. Objective: The present review focused on the fact that chalcone and flavone derivatives possess an interesting spectrum of anticancer activities and their representative mechanisms of action for antitumor therapy. Chalcone and flavones have potential in vitro and in vivo anticancer activity on multiple targets with different mechanisms, including topoisomerase inhibition, MDR channel inhibition Targeting NF-kB pathway, Serine/threonine protein kinase inhibition, PRAP1 inhibition, tubulin polymerase inhibition, Aromatase inhibition, cell cycle disruption, apoptosis inducing, immunomodulatory and inflammation mediatory mechanism. The advantage of chalcone and flavone scaffolds is their convenient synthetic methods and wide clinical potential. Methods: We have scrutinized and reviewed 60 research articles published in different databases in recent years highlighting chalcones and flavones with different anticancer activities and evaluated their binding interactions in docking studies and potency in in vitro studies. Substituted chalcones and flavones with various heterocyclic nuclei and aliphatic and aromatic side chains are discussed. A thorough investigation on the mechanism by which each flavone and chalcone exerted its specific anticancer activity was done and is reviewed. Results: It was seen that research conducted on chalcones and flavones proved it as a privileged structure with multifunctional anticancer activity. More exploration of these molecules will provide newer cancer therapeutic agents with less toxicity. Conclusion: The review will be helpful for the wide variety of scientific community doing research on these versatile molecules.