Potential Biological Activity Research Articles

The preventive effects of Centaurea maroccana Ball. extract against oxidative stress induced by cisplatin in mice brains: in vitro and in vivo studies

Since antiquity, Centaurea species have been used in folk medicine to treat several diseases owing to their potential biological activities that distinguish this genus such as antioxidant, anticancer, and anti-inflammatory effect. The current study aimed to investigate the possible neuroprotective effects of the n-butanol extract of Centaurea maroccana (BECM) against cisplatin (CP) induced neurotoxicity in mice. BECM’s potential neuroprotective properties were studied in vitro and in vivo models. Male Swiss albino mice were orally received BECM (200 mg/kg) for 10 days before a single intraperitoneal injection of cisplatin (8 mg/kg). Vitamin E (100 mg/kg) was given daily by gavage as a positive control. In vitro results revealed that BECM inhibited lipid peroxidation (LPO) levels and acetylcholinesterase (AChE) activity. In vivo findings showed that BECM pretreatment was able to regulate lactate dehydrogenase (LDH) levels and to improve CP-induced cholinergic dysfunction by inhibiting AChE activity in mice brains. Moreover, BECM attenuated CP-provoked oxidative stress by suppressing LPO levels, increasing total antioxidant capacity (TAC) and enhancing the activities of antioxidant enzymes (catalase (CAT), superoxide dismutase (SOD), reduced glutathione (GSH), glutathione peroxidase (GPx) and glutathione S-transferase (GST)) in both brain cytosolic and mitochondrial fractions. The histological analysis exhibited neurotoprotective effect of BECM by protecting the cerebral cortex and reducing the histomorphological alterations resulted by cisplatin. Interestingly, our extract achieved neuroprotection comparable to vitamin E in most evaluated parameters. It appears that protective potency of BECM against CP-induced neurotoxicity could be related to its richness in polyphenols confirmed by liquid-chromatography tandem mass spectrometry analysis (LC-MS/MS).

Structures, biosynthesis, and bioactivities of prodiginine natural products.

Prodiginines are a large family of microbial secondary metabolites with a core structure of tripyrrole rings. They exhibit not only diverse chemical structures but also rich biological activities, such as anti-cancer, anti-microbial, anti-algae, anti-parasitic, pesticides, and UV radiation resistance. The preferred cytotoxicity to cancer cells rather than normal cells indicates a good biological selectivity and safety, which makes the prodiginines promising candidates for drug development and novel additives for food processing. Until now, 33 prodiginine natural products have been identified in various bacteria, including Serratia, Hahella, Pseudoalteromonas, Vibrio, Zooshikella, Streptomyces, and Actinomadura. However, most efforts are still focused on the star molecule prodigiosin, while little yet is known about other prodiginine members, which retards the research and application of prodiginine compounds. To gain insight into the prodiginine family, we reviewed the recent discoveries on their chemical structures, biosynthesis, biological activities, and mechanisms of action. We believe this article will provide a guideline for new research on prodiginines, such as the discovery of new congeners and drug development. KEY POINTS: • The prodiginines are a large family of natural products with a core structure of tripyrrole rings and exhibit various bioactivities. • The prodiginines have a widespread distribution among many environmental microbes and diverse biosynthetic pathways, indicating important ecological roles and a great potential for new congeners. • The potent biological activities and good selectivity of action make prodiginines good lead compounds for drug development.

Antioxidant, anti-inflammatory, and antibacterial activities of a 70% ethanol-Symphyocladia linearis extract

Research on the potential biological activity of red alga Symphyocladia spp. has been limited to Symphyocladia latiuscula, which is widely used as a food ingredient in Korea. Here, we examined the biological activity of another species, Symphyocladia linearis, which is found in Korea and was reported as a new species in 2013. The aim of this study was to evaluate the antioxidant, anti-inflammatory, and antibacterial properties of a 70% ethanol extract of S. linearis. Antioxidant activity, which was evaluated using radical scavenging assays, revealed half maximal inhibitory concentration values for 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) and 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) of 34.57 and 11.70 μg/mL algal extract, respectively. Anti-inflammatory activity of the S. linearis ethanolic extract was evaluated using RAW 264.7 cells by measuring the inhibition of lipopolysaccharide-induced nitric oxide (NO) and prostaglandin E2 (PGE2) production. The potential cytotoxicity of NO and PGE2 was first examined, confirming no toxicity at concentrations ranging from 10-100 μg/mL. NO production was inhibited 61.1% and 78.0% at 50 and 100 μg/mL S. linearis extract, respectively; and PGE2 production was inhibited 69.1%, 83.2%, and 94.8% at 25, 50, and 100 μg/mL S. linearis extract, respectively. Thus, the S. linearis extract showed very strong efficacy against PGE2 production. The cellular production of reactive oxygen species, measured using 2′,7′-dichlorofluorescin diacetate fluorescence, was inhibited 48.8% by the addition of 100 μg/mL S. linearis extract. Antibacterial activity was evaluated using the disc diffusion method and minimum inhibitory concentration (MIC). S. linearis was effective only against gram-positive bacteria, exhibiting antibacterial activity against Staphylococcus aureus with a MIC of 256 μg/mL extract and against Bacillus cereus with a MIC of 1,024 μg/mL extract. Based on these results, we infer that a 70% ethanolic extract of S. linearis possesses strong anti-inflammatory properties, and therefore has the potential to be used in the prevention and treatment of inflammatory and immune diseases.

Copper- and Visible-Light-Catalyzed Cascade Radical Cyclization of N-Propargylindoles with Cyclic Ethers.

An efficient visible-light-assisted, copper-catalyzed tandem radical cyclization of N-propargylindoles with cyclic ethers is established. A series of 2-oxoalkyl-9H-pyrrolo[1,2-a]indol-9-ones with potential biological activities were synthesized in moderate yields by using a dual catalytic system with copper acetate as a transition metal catalyst and eosin Y as a visible light catalyst. The investigation of reaction mechanism shows that it goes through a cascade oxoalkyl radical addition, cyclization, and oxidation process.

Synthesis, Anticancer and Antitubercular Properties of New Chalcones and Their Nitrogen-Containing Five-Membered Heterocyclic Hybrids Bearing Sulfonamide Moiety.

A new series of sulfonamides, 8a-b, 10, 12, and 14a-b, were synthesized by N-sulfonation reaction with sulfonyl chlorides 6a-b. Five new series of chalcone-sulfonamide hybrids (16-20)a-f were prepared via Claisen–Schmidt condensation of the newly obtained sulfonamides with aromatic aldehydes 15a-f in basic medium. Chalcones substituted with chlorine at position 4 of each series were used as precursors for the generation of their five-membered heterocyclic pyrazoline (22-23)a-d, (24-25)a-b and carbothioamide 27a-f derivatives. The synthesized compounds were evaluated for their anticancer and antituberculosis activities. To determine their anticancer activity, compounds were screened against sixty human cancer cell lines at a single dose (10 μM). Compounds 17a-c were highly active against LOX IMVI (melanoma), with IC50 values of 0.34, 0.73 and 0.54 μM, respectively. Chalcone 18e showed remarkable results against the entire panel of leukemia cell lines with IC50 values between 0.99–2.52 μM. Moreover, compounds 20e and 20f displayed growth inhibition of Mycobacterium tuberculosis H37Rv at concentrations below 10 μM. Although they showed low selectivity in cytotoxicity tests against the Vero cell line, further optimization could advance the potential biological activity of the selected compounds.

Synthesis, Anticancer Evaluation and Pharmacokinetic Studies of Quinoline‐Triazole Hybrid Derivatives

AbstractSynthesis of effective and target‐selective biologically active molecules through conjugation of diversely substituted triazoles and 5‐aminoquinoline was achieved successfully with 1,4‐disubstituted regioisomer products in the 3+2 cycloaddition reaction, as expected. Seven quinoline‐1,2,3‐triazole hybrid compounds which bear different substituent groups were subjected to FTIR, 1HNMR, 13CNMR and MALDI‐MS spectroscopic characterization methods. All quinoline‐1,2,3‐triazole hybrid derivatives (8 a–g) were explored for their anti‐cancer activity towards Human urinary bladder carcinoma (T24) cells through cell viability, fluorescent imaging and colony formation analyses. Some chemical reactivity potentials and the pharmacokinetic properties of the quinoline‐1,2,3‐triazole hybrid compounds were analyzed. The frontier molecular orbital energies gap and chemical behaviour indices based on HOMO and LUMO energy values were analyzed via in‐silico methods. All in vitro and in silico results are in agreement that quinoline‐triazole derivative 8 f has potent anticancer activity and could serve for further investigation to enhance its potential biological activities.

Antibiofilm activity of secondary metabolites of sponge-associated bacterium Alcanivorax sp. from the Red Sea

Sponge-associated bacteria are a well-known source of unique and diverse natural products with potential biological activities. In this study, a rarely occurring sponge-associated bacterium from the genus Alcanivorax was isolated from the sponge Siphonochalina siphonella and subjected to extraction of metabolites. Metabolites were extracted from the culture supernatant and biomass of the bacterium using the solvent extraction method. Extracts were evaluated for antibacterial and antibiofilm activities against five different biofilm-forming bacteria isolated from the microfouling assemblage. The crude extracts were subjected to chemical profiling to identify their composition using gas chromatography-coupled mass spectrometry (GC-MS). The results obtained show mild to strong antibacterial activity of the extracts against the biofilm-forming bacteria with the minimum inhibitory concentration (MIC) of 3.125 mg ml-1. The percentage inhibition of biofilm formation ranged from 46% to 71%. Compounds detected in GC-MS analysis are mostly fatty acids and their derivatives that include compounds with known antibiofilm activity such as tetradecanoic acid, dodecanoic acid, and hexadecanol from the culture supernatant extract. Eicosane; hexadecanoic acid, methyl ester; and hexadecanoic acid, ethyl ester were detected from the biomass extract. Molecular docking analysis of the compounds from the bacterial extracts confirms their potential antibiofilm properties. The result indicated that Alcanivorax sp. associated with the sponge possess relevant antibiofilm activity and may serve as a novel source of secondary metabolites with the application as antibiofilm agents.

Alpha-Phellandrene and Alpha-Phellandrene-Rich Essential Oils: A Systematic Review of Biological Activities, Pharmaceutical and Food Applications.

Alpha-phellandrene is a very common cyclic monoterpene found in several EOs, which shows extensive biological activities. Therefore, the main focus of the present systematic review was to provide a comprehensive and critical analysis of the state of the art regarding its biological activities and pharmaceutical and food applications. In addition, the study identified essential oils rich in alpha-phellandrene and summarized their main biological activities as a preliminary screening to encourage subsequent studies on their single components. With this review, we selected and critically analyzed 99 papers, using the following bibliographic databases: PubMed, SciELO, Wiley and WOS, on 8 July 2022. Data were independently extracted by four authors of this work, selecting those studies which reported the keyword “alpha-phellandrene” in the title and/or the abstract, and avoiding those in which there was not a clear correlation between the molecule and its biological activities and/or a specific concentration from its source. Duplication data were removed in the final article. Many essential oils have significant amounts of alpha-phellandrene, and the species Anethum graveolens and Foeniculum vulgare are frequently cited. Some studies on the above-mentioned species show high alpha-phellandrene amounts up to 82.1%. There were 12 studies on alpha-phellandrene as a pure molecule showed promising biological functions, including antitumoral, antinociceptive, larvicidal and insecticidal activities. There were 87 research works on EOs rich in alpha-phellandrene, which were summarized with a focus on additional data concerning potential biological activities. We believe this data is a useful starting point to start new research on the pure molecule, and, in particular, to distinguish between the synergistic effects of the different components of the OEs and those due to alpha-phellandrene itself. Toxicological data are still lacking, requiring further investigation on the threshold values to distinguish the boundary between beneficial and toxic effects, i.e., mutagenic, carcinogenic and allergenic. All these findings offer inspiration for potential applications of alpha-phellandrene as a new biopesticide, antimicrobial and antitumoral agent. In particular, we believe our work is of interest as a starting point for further studies on the food application of alpha-phellandrene.

Bovine-derived α-lactalbumin exhibits cardiovascular protection against aging by ameliorating the inflammatory process in mice

Cardiovascular aging is the most important factor leading to cardiovascular disease (CVD), and the incidence and severity of cardiovascular events increase with age. Cardiovascular disease is one of the leading causes of death in the aging population. Therefore, it is extremely urgent to develop and explore effective drugs or bioactive molecules to prevent cardiovascular aging and related diseases. In the current work, the effect of bovine α-lactalbumin (α-lactalbumin is one of the major bioactive protein molecules in milk) on cardiovascular aging was investigated in vitro and in vivo. First, a cellular model of cardiovascular aging was established using H2O2-induced in vitro cellular models. It was found that α-lactalbumin could alleviate cardiovascular senescence by assessing Sa-β-gal and senescence-related markers (such as p16/p21/p53) in in vitro cellular models. Bovine α-lactalbumin attenuated aging-related inflammation and oxidative stress. Furthermore, aged mice were used as an in vivo cardiovascular aging model. We explored the effect of α-lactalbumin on cardiovascular aging and found that cardiovascular aging was significantly attenuated by evaluating Sa-β-gal staining and aging-related marker molecules. Mechanistically, we found that α-lactalbumin may alleviate cardiovascular aging by regulating the expression of Sirt1 (Sirtuin 1). In summary, in the current work, we systematically explored the potential biological activity of α-lactalbumin against cardiovascular aging and found that α-lactalbumin has good anti-aging potential in vitro and in vivo, suggesting that α-lactalbumin could be used as an antiaging functional food in the future.

Poisonous Piperidine Plants and the Biodiversity of Norditerpenoid Alkaloids for Leads in Drug Discovery: Experimental Aspects.

There are famous examples of simple (e.g., hemlock, Conium maculatum L.) and complex (e.g., opium poppy, Papaver somniferum L., Papaveraceae) piperidine-alkaloid-containing plants. Many of these are highly poisonous, whilst pepper is well-known gastronomically, and several substituted piperidine alkaloids are therapeutically beneficial as a function of dose and mode of action. This review covers the taxonomy of the genera Aconitum, Delphinium, and the controversial Consolida. As part of studying the biodiversity of norditerpenoid alkaloids (NDAS), the majority of which possess an N-ethyl group, we also quantified the fragment occurrence count in the SciFinder database for NDA skeletons. The wide range of NDA biodiversity is also captured in a review of over 100 recently reported isolated alkaloids. Ring A substitution at position 1 is important to determine the NDA skeleton conformation. In this overview of naturally occurring highly oxygenated NDAs from traditional Aconitum and Delphinium plants, consideration is given to functional effect and to real functional evidence. Their high potential biological activity makes them useful candidate molecules for further investigation as lead compounds in the development of selective drugs.

Role of Phytoconstituents in the Aloe-Mediated Nanoparticles

Currently, green, single-pot biomimetic, and/or biological methods of Nanoparticle (NP) synthesis are preferred over chemical and physical methods because of their rapidity, eco-friendliness, non-pathogenicity, and economic attributes. In addition, these biosynthesis methods exclude the use of high temperature, energy, pressure, and toxic chemicals. Through biosynthetic methods, nanotechnology is related to biotechnology. This has advanced nanobiotechnology which is the development of eco-friendly and biosynthetic nanomaterials/nanoparticles. Therefore, nowadays, biogenic or green synthesis of NPs using plants has emerged as a potential nano-factory, and their applications are based on phytochemicals. The chemical constituents identified in Aloe plants include vitamins, minerals, enzymes, polysaccharides, fatty acids, indoles, hydrocarbons, carboxylic acids, aldehydes, ketones, phenolic compounds, phytosterols, pyrimidines, alkaloids, etc. Each of these chemicals has potential biological activities that make them essential for in nanotechnology. Aloe phytochemicals play a crucial role in the fabrication of Aloe-based NPs by acting as reducing, capping, and stabilizing agents that control the shape and size of the formed NPs. In addition, these phytochemicals play a significant role in the applications of Aloe-based NPs owing to their biological properties. Moreover, it is important to understand the role of phytoconstituents from different Aloe species and in every part of the plants using nanotechnology.

Morphology and Anti-microbial Studies of Zinc Stannate Nanoparticles Constructed via Green Synthesis Approach

In the scientific field, microbial contaminations are growing along with the developments of newer research methodologies. Evaluating anti-microbial activity using newly designed materials has been gaining importance over the years to address this issue. The present work aims to form zinc stannate nanoparticles (ZTO NPs) through bio-synthesis and compare their biological efficiency with the as-synthesized nanoparticles through chemical synthesis. The nanoparticles (Zn2SnO4) were synthesized through a hydrothermal method by developing moderate experimental conditions. Three different combinations were synthesized using 2:1 mole ratio of ZnCl2 and SnCl2 precursors, and leaf extracts such as Aloe barbadensis mill and Terminalia catappa were used in the bio-synthesis method. Sodium hydroxide was used as a mineralizer in the chemical synthesis method. The obtained ZTO NPs were characterized by XRD, SEM-EDS, and UV-Visible spectral techniques. Finally, the antibacterial and anti-fungal activities were evaluated using the Agar-well diffusion method. Competitive biological activity response from the bio-synthesized ZTO NPs against the selected bacterial (Bacillus subtilis, S. Aureus, E. Coli, and P. Aeruginosa) and fungal strains (A. Niger and C. albicans). The synthesized ZTO NPs were highly efficient in exhibiting potential biological activity against the selected microbes.

Mushroom β-Glucan Recovered from Antler-Type Fruiting Body of Ganoderma lucidum by Enzymatic Process and Its Potential Biological Activities for Cosmeceutical Applications.

Mushrooms are incredibly valuable macro fungi that are an important and integral part of the ecosystem. In addition to being used as cuisine, mushrooms have been used for medicinal purposes for many centuries. This research applied a process for recovering β-glucan (BG) from the antler-type fruiting body of Ganoderma lucidum as well as tested the biological activities related to cosmeceutical applications. The characterization of complex structure was performed by fourier-transform infrared (FTIR) and nuclear magnetic resonance (MNR) spectroscopies. The obtained extract contained 40.57% BG and 7.47% protein, with the detectable bioactivities of anti-tyrosinase and antioxidation. Consequently, it showed the activity that can be used to whiten the skin by reducing or inhibiting the process of skin pigmentation. The BG also showed moderate activities of anti-collagenase, anti-elastase, and anti-hyaluronidase. The test by the HET-CAM confirmed no skin irritation of the complex extract. Based on human peripheral blood mononuclear cell (PBMC) test, the BG had no significant inhibiting effect on cell viability. In addition, the obtained BG had functional properties higher than commercially available BG, especially oil-binding capacity. These findings provided new insights into the potential application of G. lucidum BG as a polymeric material in the cosmeceutical industries.

Simple Isolation of Cordycepin from Cordyceps militaris by Dual-Normal Phase Column Chromatography and Its Potential for Making Kombucha Functional Products

Cordycepin (3′-deoxyadenosine) is a potent bioactive metabolite of the medicinal fungus Cordyceps militaris, which has been increasingly exploited to treat various chronic diseases in humans. However, the current synthesis and purification procedures of cordycepin are principally laborious and complicated. This study provides a simple protocol approach to isolate and purify cordycepin from C. militaris by normal phase column chromatography at room temperature. Besides, this is the first to investigate the potential of cordycepin and cordycepin-included extracts from C. militaris for making Kombucha functional products. By a repeated column chromatography, an amount of 1.16 g of cordycepin is isolated from 2.8 kg of fruiting bodies of C. militaris, which obtained an efficiency of 83.26% compared to that estimated by high-performance liquid chromatography (HPLC). The purity of cordycepin is confirmed by thin-layer chromatography (TLC), HPLC, and proton nuclear magnetic resonance (1H NMR). In addition, kombucha-fermented extracts from cordycepin and cordycepin-included fractions show potential biological activities in terms of antioxidant, anti-diabetes via α-glucosidase inhibitory assay, and cytotoxicity via MTT assay on Meg-01 and HL-60 cell lines. Further studies on optimization of extraction protocol and verification of health benefits of kombucha products from cordycepin should be conducted prior to the official mass production.

Novel saccharin analogs as promising antibacterial and anticancer agents: synthesis, DFT, POM analysis, molecular docking, molecular dynamic simulations, and cell-based assay.

Saccharine is a pharmacologically significant active scaffold for various biological activities, including antibacterial and anticancer activities. Herein, saccharinyl hydrazide (1) was synthesized and converted into 2-[(2Z)-2-(1,1-dioxo-1,2-dihydro-3H-1λ6,2- benzothiazole-3-ylidene) hydrazinyl] acetohydrazide (5), which was employed as a key precursor for synthesizing a novel series of small molecules bearing different moieties of monosaccharides, aldehydes, and anhydrides. Potent biological activities were found against Staphylococcus and Escherichia coli , and the results indicated that compounds 6c and 10a were the most active analogs with an inhibition zone diameter of 30–35 mm . In cell-based anticancer assay over Ovcar-3 and M-14 cell lines, compound 10a was the most potent analog with IC50 values of 7.64 ± 0.01 and 8.66 ± 0.01 µM, respectively. The Petra Orisis Molinspiration (POM) theoretical method was used to calculate the drug score of tested compounds and compare them with their experimental screening data. Theoretical DFT calculations were carried out in a gas phase in a set of B3LYP 6-311G (d,p). Molecular docking studies utilizing the MOE indicated the best binding mode with the highest energy interaction within the binding sites. The molecular docking for Ovcar-3 was carried out on the ovarian cancer protein (3W2S), while the molecular docking for M-14 melanoma was carried out on the melanoma cancer protein (2OPZ). The MD performed about 2ns simulations to validate selected compounds’ theoretical studies.

Exploring the protective mechanism of baicalin in treatment of atherosclerosis using endothelial cells deregulation model and network pharmacology

BackgroundBaicalin is a generally available flavonoid with potent biological activity. The present study aimed to assess the underlying mechanism of baicalin in treatment of atherosclerosis (AS) with the help of network pharmacology, molecular docking and experimental validation.MethodsThe target genes of baicalin and AS were identified from public databases, and the overlapping results were considered to be baicalin-AS targets. Core target genes of baicalin were obtained through the PPI network and validated by a clinical microarray dataset (GSE132651). Human aortic endothelial cells (HAECs) were treated with Lipopolysaccharide (LPS) to construct an endothelial injury model. The expression of NOX4 was examined by real-time qPCR and western blot. Flow cytometry was used to detect intracellular levels of reactive oxygen species (ROS). Furthermore, HAECs were transfected with NOX4-specific siRNA and then co-stimulated with baicalin and LPS to investigate whether NOX4 was involved in the anti-oxidative stress effects of baicalin.ResultsIn this study, baicalin had 45 biological targets against AS. Functional enrichment analysis demonstrated that most targets were involved in oxidative stress. Using the CytoHubba plug-in, we obtained the top 10 genes in the PPI network ranked by the EPC algorithm. Molecular docking and microarray dataset validation indicated that NOX4 may be an essential target of baicalin, and its expression was significantly suppressed in AS samples compared to controls. In endothelial injury model, intervention of HAECs with baicalin increased the expression levels of NOX4 and NOS3 (eNOS), and decreased LPS-induced ROS generation. After inhibition of NOX4, the anti-ROS-generating effect of baicalin was abolished.ConclusionCollectively, we combined network pharmacology and endothelial injury models to investigate the anti-AS mechanism of baicalin. The results demonstrate that baicalin may exert anti-oxidative stress effects by targeting NOX4, providing new mechanisms and insights to baicalin for the treatment of AS.

Analysis of Phenolic and Flavonoid Content, α-Amylase Inhibitory and Free Radical Scavenging Activities of Some Medicinal Plants.

In Nepal, about 700 plant species have been reported to be used for the primary care of different diseases. However, many of them have not been studied yet for their scientific evidence. The main aim of this study is the quantitative analysis of flavonoids and phenolic content, antioxidant, and antidiabetic activities of the extracts of four different medicinal plants, namely, Pogostemon benghalensis, Aleuritopteris bicolor, Crateva unilocularis, and Rungia pectinata growing in Nepal. The methanol extracts of plant samples were prepared by the hot percolation method using the Soxhlet apparatus. The phytochemicals of the plant extracts were analysed by colour differentiation methods using different analytical reagents. The phenolic content was estimated by using Folin–Ciocalteu's phenol reagent and the flavonoid was estimated by the aluminium chloride colorimetric method. The 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay was used to evaluate the antioxidant potential. The α-amylase enzyme inhibition activity was performed to evaluate the antidiabetic activity of plant extracts. The amount of total phenolics and flavonoids content was found to be the highest in Pogostemon benghalensis (169.43 ± 3.58 mg GAE/g and 65.2 ± 2.0 mg QE/g), respectively, which also showed the most potent free radical scavenging activity (IC50 35.92 ± 0.65 μg/mL). The extract of Aleuritopteris bicolor showed the highest α-amylase inhibitory activity (IC50 651.58 ± 10.32 μg/mL) whereas Crateva unilocularis and Pogostemon benghalensis exhibited moderate activity. The extract of Rungia pectinata showed the least activity towards α-amylase inhibition. Some of the medicinal plants selected in this study showed high TPC and TFC values with potent biological activities. To the best of our knowledge, these medicinal plants have the least exposure to their biological activities, and the results provide scientific evidence for the traditional uses of these plants against diabetes and infectious diseases. However, a detailed study can be performed in these plants to isolate the active chemical compounds and to evaluate in vivo pharmacological activities to know the active drug candidates for the future drug development process.

In vitro correlation studies of antidiabetic, antioxidant activity and HPLC-ESI-MS/MS analysis of marine seaweeds from Gulf of Mannar

Marine seaweeds are known to exhibit potential biological activity, which possess a variety of biological functions. The important pharmacological aspect of using marine polyphenols as a strong natural antioxidant has been suggested to play a vital role in the alleviation of diabetes mellitus. The present study aims to investigate the antioxidant potential of four green marine seaweeds namely Chaetomorpha crassa, Caulerpa racemosa, Caulerpa verticillata and Caulerpa scalpelliformis in the management of Type 2 diabetes mellitus. In vitro evaluation of the antioxidant activity was assessed by employing ABTS, Phosphomolybdenum, and metal chelation activity methods. The results showed that among four marine seaweeds, the ethanolic extracts of C. verticillata have recorded the highest total flavonoid content (66.19 ± 0.002 mg QE/g) and antioxidant activity in ABTS (96.95 ± 0.411 %), Phosphomolybdenum assay (323.28±0.006μM), and Metal chelation activity (71.92 ± 0.48%). The IC50 values of C verticillata were found to be 0.42 mg/ml for ABTS and 0.78 mg/ml for Metal chelation activity respectively. Also, ethanolic extracts of C verticillata showed highly significant inhibition of α-amylase (70.64 ± 0.39% with IC50 of 0.420 mg/ml) and α-Glucosidase (64.07 ± 0.33% with IC50 of 0.068 mg/ml) in a dose-dependent manner. The resultant principal component analysis had showed the effective association between the antioxidant and antidiabetic potential of the marine seaweeds. It is clear, that C. verticillata could be a good choice to reduce the hyperglycemic condition by inhibiting the carbohydrate hydrolyzing enzymes and maintain tolerable oxidative stress.

Polydatin: Pharmacological Mechanisms, Therapeutic Targets, Biological Activities, and Health Benefits.

Polydatin is a natural potent stilbenoid polyphenol and a resveratrol derivative with improved bioavailability. Polydatin possesses potential biological activities predominantly through the modulation of pivotal signaling pathways involved in inflammation, oxidative stress, and apoptosis. Various imperative biological activities have been suggested for polydatin towards promising therapeutic effects, including anticancer, cardioprotective, anti-diabetic, gastroprotective, hepatoprotective, neuroprotective, anti-microbial, as well as health-promoting roles on the renal system, the respiratory system, rheumatoid diseases, the skeletal system, and women’s health. In the present study, the therapeutic targets, biological activities, pharmacological mechanisms, and health benefits of polydatin are reviewed to provide new insights to researchers. The need to develop further clinical trials and novel delivery systems of polydatin is also considered to reveal new insights to researchers.

Green synthesis of copper oxide nanoparticles using Abutilon indicum leaves extract and their evaluation of antibacterial, anticancer in human A549 lung and MDA-MB-231 breast cancer cells.

In currently, biosynthesis of copper oxide nanoparticles (CuO NPs) are most widely used numerous in biological applications such as biosensor, energy, medicine, agriculture, environmental and industrial wastewater treatment. The hierarchical CuO NPs was synthesized via green chemistry method by using of Abutilon indicum (A. indicum) leaf extract, its nontoxic, facile and low-cost approaches. Biogenic synthesized CuO NPs was characterized by using a UV-visible absorption spectroscopy (UV-Vis), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD) and Field mission scanning electron microscopy (FE-SEM) with Energy-dispersive X-ray spectroscopy (EDX) analysis. The synthesized CuO NPs was performed antibacterial activity against human pathogenic organisms of both Gram negative (Escherichia coli and Salmonella typhi) and Gram positive (Bacillus subtilis and Staphylococcus aureus) bacteria by using agar well diffusion method. Biological synthesized CuO NPs was showed potential bactericidal activity against Gram positive bacteria of B. subtilis than compared to Gram negative bacteria of E. coli. The cytotoxic effect of A. indicum mediated synthesized CuO NPs was evaluated against to human lung A549 and breast MDA-MB-231cancer cell lines by determined using of MTT assay. In furthermore, photocatalytic dye degradation was performed that synthesized CuO NPs have effectively removed 78% of malachite green dye molecule. Our investigation results suggested that the green synthesized CuO NPs potential biological activity of antibacterial activity against Gram positive bacterial, anticancer activity was effectively against MDA-MB-231cancer cell line and good dye degradation was exhibited in malachite green. The A. indicum aqueous leaf extract mediated synthesized CuO NPs has strongly suggested promising nano-biomaterials for fabrication of biomedical applications.