Flavonoids and Phenols,the Potential Anti-Diabetic Compounds from Bauhinia strychnifolia Craib. Stem.

Bioactive compounds from medicinal plants are good alternative treatments for T2DM. They are also sources of lead molecules that could lead to new drug discoveries. In this study, Bauhinia strychnifolia Craib. stem, a traditional Thai medicinal plant for detoxification, was extracted into five fractions, including crude extract, BsH, BsD, BsE, and BsW, by ethanolic maceration and sequential partition with hexane, dichloromethane, ethyl acetate, and water, respectively. Among these fractions, BsE contained the highest amounts of phenolics (620.67 mg GAE/g extract) and flavonoids (131.35 mg QE/g extract). BsE exhibited the maximum inhibitory activity against α-glucosidase (IC₅₀ 1.51 ± 0.01 µg/mL) and DPP-IV (IC₅₀ 2.62 ± 0.03 µg/mL), as well as dominantly promoting glucose uptake on 3T3-L1 adipocytes. Furthermore, the four compounds isolated from the BsE fraction, namely resveratrol, epicatechin, quercetin, and gallic acid, were identified. Quercetin demonstrated the highest inhibitory capacity against α-glucosidase (IC₅₀ 6.26 ± 0.36 µM) and DPP-IV (IC₅₀ 8.25 µM). In addition, quercetin prominently enhanced the glucose uptake stimulation effect on 3T3-L1 adipocytes. Altogether, we concluded that quercetin was probably the principal bioactive compound of the B. strychnifolia stem for anti-diabetic, and the flavonoid-rich fraction may be sufficiently potent to be an alternative treatment for blood sugar control.     

Phenolics Profiling of Carpobrotus edulis (L.) N.E.Br. and Insights into Molecular Dynamics of Their Significance in Type 2 Diabetes Therapy and Its Retinopathy Complication

Adverse effects associated with synthetic drugs in diabetes therapy has prompted the search for novel natural lead compounds with little or no side effects. Effects of phenolic compounds from Carpobrotus edulis on carbohydrate-metabolizing enzymes through in vitro and in silico methods were assessed. Based on the half-maximal inhibitory concentrations (IC₅₀), the phenolic extract of the plant had significant (p < 0.05) in vitro inhibitory effect on the specific activity of alpha-amylase (0.51 mg/mL), alpha-glucosidase (0.062 mg/mL) and aldose reductase (0.75 mg/mL), compared with the reference standards (0.55, 0.72 and 7.05 mg/mL, respectively). Molecular interactions established between the 11 phenolic compounds identifiable from the HPLC chromatogram of the extract and active site residues of the enzymes revealed higher binding affinity and more structural compactness with procyanidin (−69.834 ± 6.574 kcal/mol) and 1,3-dicaffeoxyl quinic acid (−42.630 ± 4.076 kcal/mol) as potential inhibitors of alpha-amylase and alpha-glucosidase, respectively, while isorhamnetin-3-O-rutinoside (−45.398 ± 4.568 kcal/mol) and luteolin-7-O-beta-d-glucoside (−45.102 ± 4.024 kcal/mol) for aldose reductase relative to respective reference standards. Put together, the findings are suggestive of the compounds as potential constituents of C. edulis phenolic extract responsible for the significant hypoglycemic effect in vitro; hence, they could be exploited in the development of novel therapeutic agents for type-2 diabetes and its retinopathy complication.     

Antidiabetic,Antiglycation, and Antioxidant Activities of Ethanolic Seed Extract of Passiflora edulis and Piceatannol In Vitro

The objective of this work was to investigate the antidiabetic, antiglycation, and antioxidant potentials of ethanolic extract of seeds of Brazilian Passiflora edulis fruits (PESE), a major by-product of the juice industry, and piceatannol (PIC), one of the main phytochemicals of PESE. PESE, PIC, and acarbose (ACB) exhibited IC₅₀ for alpha-amylase, 32.1 ± 2.7, 85.4 ± 0.7, and 0.4 ± 0.1 µg/mL, respectively, and IC₅₀ for alpha-glucosidase, 76.2 ± 1.9, 20.4 ± 7.6, and 252 ± 4.5 µg/mL, respectively. The IC₅₀ of PESE, PIC, and sitagliptin (STG) for dipeptidyl-peptidase-4 (DPP-4) was 71.1 ± 2.6, 1137 ± 120, and 0.005 ± 0.001 µg/mL, respectively. PESE and PIC inhibited the formation of advanced glycation end-products (AGE) with IC₅₀ of 366 ± 1.9 and 360 ± 9.1 µg/mL for the initial stage and 51.5 ± 1.4 and 67.4 ± 4.6 µg/mL for the intermediate stage of glycation, respectively. Additionally, PESE and PIC inhibited the formation of β-amyloid fibrils in vitro up to 100%. IC₅₀ values for 1,1-diphenyl-2-picrylhydrazyl radical (DPPH^•) scavenging activity of PESE and PIC were 20.4 ± 2.1, and 6.3 ± 1.3 µg/mL, respectively. IC₅₀ values for scavenging hypochlorous acid (HOCl) were similar in PESE, PIC, and quercetin (QCT) with values of 1.7 ± 0.3, 1.2 ± 0.5, and 1.9 ± 0.3 µg/mL, respectively. PESE had no cytotoxicity to the human normal bronchial epithelial (BEAS-2B), and alpha mouse liver (AML-12) cells up to 100 and 50 µg/mL, respectively. However, 10 µg/mL of the extract was cytotoxic to non-malignant breast epithelial cells (MCF-10A). PESE and PIC were found to be capable of protecting cultured human cells from the oxidative stress caused by the carcinogen NNKOAc at 100 µM. The in vitro evidence of the inhibition of alpha-amylase, alpha-glucosidase, and DPP-4 enzymes as well as antioxidant and antiglycation activities, warrants further investigation of the antidiabetic potential of P. edulis seeds and PIC.     

Molecular Docking and Dynamics Simulation of Natural Compounds from Betel Leaves (Piper betle L.) for Investigating the Potential Inhibition of Alpha-Amylase and Alpha-Glucosidase of Type 2 Diabetes

Piper betle L. is widely distributed and commonly used medicinally important herb. It can also be used as a medication for type 2 diabetes patients. In this study, compounds of P. betle were screened to investigate the inhibitory action of alpha-amylase and alpha-glucosidase against type 2 diabetes through molecular docking, molecular dynamics simulation, and ADMET (absorption, distribution, metabolism, excretion, and toxicity) analysis. The molecule apigenin-7-O-glucoside showed the highest binding affinity among 123 (one hundred twenty-three) tested compounds. This compound simultaneously bound with the two-target proteins alpha-amylase and alpha-glucosidase, with high molecular mechanics-generalized born surface area (MM/GBSA) values (ΔG Bind = −45.02 kcal mol⁻¹ for alpha-amylase and −38.288 for alpha-glucosidase) compared with control inhibitor acarbose, which had binding affinities of −36.796 kcal mol⁻¹ for alpha-amylase and −29.622 kcal mol⁻¹ for alpha-glucosidase. The apigenin-7-O-glucoside was revealed to be the most stable molecule with the highest binding free energy through molecular dynamics simulation, indicating that it could compete with the inhibitors’ native ligand. Based on ADMET analysis, this phytochemical exhibited a wide range of physicochemical, pharmacokinetic, and drug-like qualities and had no significant side effects, making them prospective drug candidates for type 2 diabetes. Additional in vitro, in vivo, and clinical investigations are needed to determine the precise efficacy of drugs.     

Development of Immunonutrient from Pumpkin (Cucurbita Moschata Duchense Ex. Lamk.) Seed

Pumpkin seeds has long been used as a source of nutrition. Based on its content, it is possible that part of this plant used as immunonutrient. The purpose of this research is to study the immunomodulatory activity of pumpkin seeds. It effects on the non-specific immune response was determined through carbon clearance test, organ indexes (liver, spleen and thymic gland) and mice peritoneal exudate activity (PEA). The effects on specific immune response were determined through total antibody titre, delayed type of hypersensitivity (DTH) reaction and number of lymphocytes. On non specific immune response test, pumpkin seed at a low dose (PLD-3.8 g/kg bw) and at a high dose (PHD-7.6 g/kg bw) showed immunostimulanting effect with phagocytic index of 1.219 and 1.347, respectively. PHD increased PEA activity (p<0.01) in lysing microbes. On specific immune response test, PLD and PHD showed immunostimulation effect indicated through 50% haemaglutination activity (HA titre) i.e., 1:512 and 1:2048, respectively compared to than that of control (1:256) for secondary antibody titre. Through cellular immunity test, 48 hours after challenged, PHD showed significant (p<0.05) increased in footpad thickness. After 7 days administration, both doses of pumpkin increased lymphocytes number significantly (p<0.05). Based on the data it can be concluded that, pumpkin seeds have immunomodulatory effects, and can therefore be used as immunonutrient     

Molecular docking of phenolic compounds and screening of antioxidant and antidiabetic potential of Olea europaea L. Ethanolic leaves extract

Oxidative stress has a crucial role in diabetic pathophysiology, therefore consuming naturally derived antioxidants as a remedial target. This study examines the naturally occurring antioxidant and antidiabetic of Olea europaea L. ethanolic leaves extract. Olea europaea L. leaves were macerated (OLE) by using absolute ethanol. Phytochemical and physiochemical analysis of OLE was screened using standard methods. The antioxidant effects were examined by DPPH (1, 1-diphenyl-2-picrylhydrazil) radical scavenging assay. In vitro antidiabetic was assayed by α-amylase enzyme inhibition study. Ethanolic extraction of OLE by maceration technique, 10% yield. Loss on drying, foreign organic matters and total ash value of OLE showed 2%, 0.2% and 16.5%, respectively. Phytochemical test on OLE confirmed saponin, flavonoid, glycoside, tannin, phenol and carbohydrate presences. The total phenolic and flavonoid contents of OLE is 490 mg GAE/g and 855 mg RUE/g of extract, respectively. OLE (IC₅₀ 38.37 ± 0.26 µg/ml) showed functional DPPH scavenging assay comparable to ascorbic acid (IC₅₀ 30.37 ± 0.17 µg/ml). In the alpha-amylase inhibitory activity, Acarbose showed an IC₅₀ value of 20.06 ± 0.19 µg/ml, while OLE portrayed an IC₅₀ value of 37.99 ± 0.15 µg/ml. The kinetic studies revealed that all samples at high concentrations reacted within a very short time, and a steady state was reached almost immediately. The lowest concentration showed slow kinetic behaviour implied longer periods before the constant state was reached. Molecular docking studies evidenced that most of the phenolic compounds of OLE interact with the active site of Human pancreatic α-amylase through the hydrogen bonding and hydrophobic interaction confirming the alpha-amylase inhibitory effect. The results suggest that Olea europaea L. has been a conceivable natural bioactive source as an antioxidant and an antidiabetic agent.     

Exploration of carbonic anhydrase inhibition of bioactive metabolites from Pistacia integerrima by molecular docking and first-principles investigations

Bioassay guided fractionation of Pistacia integerrima crude methanolic extract gave Pistacide-A (1) and Pistacide-B (2), along with ten known phytochemicals (3–12). Biochemical analysis of crude plant extract, in-vitro and in-silico carbonic anhydrase inhibitory potential of newly isolated compounds Pistacide-A (1) and Pistacide-B (2) were performed. The cytotoxicity of extract in methanol, ethylacetate and n-butanol against Artemia salina brine-shrimp was 34.98 g/ml, 160.81 g/ml, and 135.77 g/ml, respectively. The significant antimicrobial activity was exhibited by crude, ethyl acetate, and n-butanol fractions. Compounds 1 (IC₅₀ = 6.51 ± 0.42 mM) and 2 (IC₅₀ = 2.85 ± 0.09 mM) showed good carbonic anhydrase inhibition compared with standard zonisamide drug (IC₅₀ = 1.87 ± 0.003 mM). In addition, we have also clarified the electronic properties, absorption wavelengths, molecular electrostatic potential and Hirshfeld analysis by first-principles studies. The coherent intra-molecular charge transfer was seen from occupied to unoccupied molecular orbitals. The absorption wavelengths calculated at time dependent B3LYP/6-31G** level in methanol provided excellent accord with the experimental evidence. Molecular docking score revealed that Pistacide-B would be an efficient drug than its other counterpart that is rational to the experimental data.     

Synthesis,characterization and evaluation of biological properties of selenium nanoparticles from Solanum lycopersicum

Synthesis of nanoparticles by green synthesis has a large number of biomedical applications worldwide. In this study, Selenium Nanoparticles (SeNPs) were synthesized by using sodium salt of selenium and Solanum lycopersicum (tomato) fruit juice and seeds extract. The plant extracts were used as a reducing agent in ratio 1:4 i.e. sodium selenite salt (Na₂SeO₃). SeNPs were characterized by UV–visible spectrophotometry, FTIR and Zeta Sizer analysis. The UV-graphs indicated the highest peak of absorbance at 350 nm. Whereas, FTIR analysis of SeNPs indicated absorbance bands at 3262.35–1633.72 cm^?1. Zeta sizer analysis showed the average size of SeNPs for Fruit juice extract as 1020 d.nm. with PDI 0.432. In case of seeds extract, average size was 1155 d.nm. with PDI 0.761; and the PDI value for both extracts showed polyderse nature of these NPs. SeNPs possessed significant antimicrobial activity against selected strains of E. coli, S. aureus, M. luteus, S. enterica, B. subtilis, K. pneumoniae and P. aureginosa. The α-amylase inhibitory assay of these SeNPs indicated that they had antidiabetic role with IC₅₀ value 24.4642 µg/mL. The DPPH assay showed that SeNPs of Solanum lycopersicum have antioxidant activity with IC₅₀ value of 20.7398 µg/mL.     

Polarity guided extraction,HPLC based phytochemical quantification,and multimode biological evaluation of Otostegia limbata (Benth.) Boiss

Purpose of studyOtostegia limbata (Benth.) Boiss. (Family: Lamiacae) is an important underexplored ethnomedicinal plant that has been used as antinflammatory, anticancer and antibacterial herbal remedy previously. The present work was aimed to evaluate the antioxidant, antimicrobial, antileishmanial, and anticancer prospective of O. limbata stem and leaf extracts.ResultsThe highest amount of phenolic and flavonoid content was obtained in the methanol-acetone and methanol stem extracts i.e., 53.29 ± 1.33 and 28.64 ± 1.16, respectively with highest DPPH scavenging in MeH stem extract (IC₅₀ = 34.5 ± 1.34 μg/ml). Significant amount of catechin, gallic acid, apigenin and rutin was quantified. A moderate antibacterial and substantial antifungal activity was observed. Cytotoxicity against brine shrimps categorized 21% of stem (3 out of 14 extracts) and 57% (8 out of 14 extracts) of leaf extracts as potent. Substantial cytotoxicity against THP-1 cell line (IC₅₀ = 3.46 ± 0.25 μg/ml) and Leishmania (IC₅₀ = 1.50 ± 0.23 μg/ml) was exhibited by methanol-distilled water leaf extract while noteworthy antiproliferative activity against Hep-G2 (IC₅₀ = 0.44 ± 0.45 μg/ml) was manifested by n-hexane stem extract. Absence of hemolysis in normal RBCs signified plant’s selective cytotoxicity. Methanol-distilled water and chloroform stem extracts displayed prominent protein kinase inhibition and antidiabetic potential of plant.ConclusionThe results of present study recommend O. limbata as a potential source of antifungal, antileishmanial, anticancer, and α-amylase inhibitory agents.     

In Vitro Alpha-Amylase and Alpha-Glucosidase Inhibitory Activity and In Vivo Antidiabetic Activity of Withania frutescens L. Foliar Extract

Withania frutescens L. is a wild perennial woody plant used by the local population for diverse therapeutic purposes. This work aims to study for the first time the potential inhibitory effect of this plant hydroethanolic extract on α-amylase and α-glucosidase activities using in vitro methods and its antidiabetic and antihyperglycemic activities using alloxan-induced diabetic mice as a model for experimental diabetes. Two doses were selected for the in vivo study (200 and 400 mg/kg) and glibenclamide, a well-known antidiabetic drug (positive control) in a subacute study (28 days) where the antihyperglycemic activity was also assessed over a period of 12 h on diabetic mice. The continuous treatment of diabetic mice with the extract of Withania frutescens for 4 weeks succeeded to slowly manage their high fasting blood glucose levels (after two weeks), while the antihyperglycemic test result revealed that the extract of this plant did not control hyperglycemia in the short term. No toxicity signs or death were noted for the groups treated with the plant extract, and it shows a protective effect on the liver and kidney. The in vitro assays demonstrated that the inhibition of alpha-amylase and alpha-glucosidase might be one of the mechanisms of action exhibited by the extract of this plant to control and prevent postprandial hyperglycemia. This work indicates that W. frutescens have an important long term antidiabetic effect that can be well established to treat diabetes.     

Heterotrophic Culture of <Emphasis Type="Italic">Chlorella protothecoides</Emphasis> in Various Nitrogen Sources for Lipid Production

The influences of urea, yeast extract, and nitrate as the nitrogen source on heterotrophic growth of four strains of Chlorella protothecoides were investigated in 9-day feed-batch cultures. Biomass dry weight concentration (DWC) and lipid yield (LY) of the four strains in all media were compared. The highest LY in 9 days was 654 mg/L/day by UTEX 255 in 2.4 g/L KNO₃ medium with a biomass DWC of 11.7 g/L and lipid content of 50.5%. Using green autotrophic seeds instead of yellow heterotrophic seeds improved the biomass DWC (13.1 vs. 11.7 g/L), LY (850 vs. 654 mg/L/day), and lipid to glucose consumption ratio (0.607 vs. 0.162). Moreover, 17.0 g/L DWC and 489 mg/L/day LY were obtained from the sequentially mixed-nitrogen medium, and the lipid to glucose consumption ratio was improved to 0.197 from 0.162 in 2.4 g/L nitrate medium and from 0.108 in 4.2 g/L yeast extract medium in the first batch.     

A comparative study of selected vitex species for phenolics estimation along with their antioxidant and herbicidal activities

This study aims to quantitative, qualitative estimation of phenolics, antioxidant (DPPH free radical scavenging, nitric oxide radical scavenging, superoxide anion scavenging, reducing power and metal chelating activity), and herbicidal properties of methanol extract of Vitex species {(Vitex negundo L. collected from Haldwani (VNH), Bhimtal (VNB) and Salari (VNS); Vitex agnus-castus L. collected from Pantnagar (VACP); Vitex trifolia L. collected from Pantnagar (VTP)}, Kumaun region, Uttarakhand, India. Herbicidal activity of methanol extracts of Vitex species was evaluated against Raphanus sativus at various concentrations for 120 h. The results revealed that the phenolic content varies from species to species as well as their location. HPLC profiling of Vitex species was carried out to identify the presence of different phenolic acids viz: vanillic acid, ferulic acid, p-coumaric acid, etc. In methanol extracts of Vitex species. VTP showed the highest DPPH (IC₅₀ = 6.84 μg/mL), nitric oxide (IC₅₀ = 2.86 μg/mL) and superoxide radical scavenging (IC₅₀ = 3.12 μg/mL) activity. The maximum reducing power was observed in VNH (RP₅₀ = 28.22 μg/mL) and the highest ion chelating capacity in VNB (IC₅₀ = 6.80 μg/mL). The effective herbicidal activity was shown by VNS, resulting in complete inhibition of seed germination. Based on the heatmap clustering selected species are divided into two clusters. The first cluster comprises VNB and VTP are there whereas in the second cluster there are two sub-clusters including VNS only in one sub-cluster and VNH and VACP in the second sub-cluster.     

Physicochemical parameter influences and their optimization on the biosynthesis of MnO2 nanoparticles using Vernonia amygdalina leaf extract

The manganese dioxide nanoparticles (MnO₂ NPs) were synthesized using Vernonia amygdalina leaf extract which was used as a reducing, capping, and stabilizing agents due to the presence of bioactive phytochemical compounds. Twenty five runs were designed to investigate the effect of V. amygdalina leaf extract ratio (A), initial potassium permanganate (KMnO₄) concentration (B), pH (C), and reaction time (D) on the biosynthesized MnO₂ NPs using 4-factor, 4-level D-Optimal Response Surface Quadratic Design Model approach. The relationship between physicochemical variables and absorption responses were established using transform second degree polynomial quadratic model. The effects of each absorption responses were analyzed by ANOVA principle using quadratic equations. A very low p-values (<0.0001), non-significant Lack of Fit F-values, and reasonable regression coefficient values (coefficient R² = 0.9790, adjusted R² = 0.9496, and predicted R² = 0.8452) suggested that there is an effective correlation between experimental results and predicted values. Numerical and graphical optimized results demonstrated that the optimized conditions for the predicted absorbance at 320 nm (1.095) were suggested at 43.72%, 1.81 mM, 6.02, and 103.42 min for V. amygdalina leaf extract ratio, initial KMnO₄ concentration, pH, and reaction time, respectively. Under these optimal conditions, the average absorbance from four experimental run was recorded to be 0.9678. This result was very closest to the predicted values. The average size elucidated by X-ray diffraction (XRD) analysis was found in the range between 20 nm and 22 nm. The stretching/or and vibrational, surface topography, thermal, and surface roughness as well as its porosity distributions were investigated by UV–Vis spectroscopy, Fourier transforms infrared (FTIR), scanning electron microscopy (SEM), differential scanning calorimeter (DSC), and Gwyddion software analysis.     

A calorimetric study of plant–plant and plant–soil interactions of extracts from Ixorhea tschudiana

The effect of the CHCl₃ and MeOH extracts from aerial parts from the Northwestern Argentina endemic species Ixorhea tschudiana Fenzl. on germination of the dicot tomato and the monoct onion and on soil microbial activity was studied by calorimetric and calorespirometric experiments. The CHCl₃ extract inhibited seedling growth of tomato which increased with increasing concentrations. Seeds imbibed with 250 mg dm^?3 extract germinated 24 h later than control and those imbibed with 100 and 500 mg dm^?3 extract. This was reflected in the calculated low specific seedling growth rate (p_SGΔH_B) as determined from calorespirometric experiments. On the other hand, seedlings obtained in 500 mg dm^?3 extract showed shorter and thicker hairy roots than control with significantly higher p_SGΔH_B. Probably, the extract induces inhibition of water uptake by seedling roots. Germination was reduced 50% in onion seeds imbibed with 500 mg dm^?3 CHCl₃ extract which apparently is due to higher rate of imbibition during the first stages as determined for calorimetry. On the other hand, 83 and 250 mg kg^?1 of the MeOH and CHCl₃ extract seem to selectively inhibit the growth of certain microorganisms and to enhance the activity of soil actinomycetes. Two actinobacteria were isolated from soil treated with these concentrations of both extracts: Kocuria sp. and Kocuria rosea; this latter species is known as a keratinolytic agent and seems to degrade complex carbon compounds of the soil and those incorporated by the MeOH extract. Both Kocuria specie seem to be beneficial for the soil converting substrate into biomass and thus I. tschudiana could be used as a soil phytoremediator.     

The polymorphism of CsThF5

Three new polymorphs of cesium thorium pentafluoride, CsThF₅, have been synthesized hydrothermally and structurally characterized. Of the structures of three polymorphs of CsThF₅ one is described in space group P4/nmm with a = 5.7358(8) and c = 7.4048(15) and two in the space group P2₁/c: one with a = 8.3600(17), b = 7.5780(15), c = 8.9912(18), β = 116.69(3) and the other with a = 8.4196(17), b = 14.645(3), c = 8.5017(17), β = 102.67(3). Comparison of these materials was made based on their structures and synthesis conditions. The formation of these species and other previously reported metal fluoride species in hydrothermal fluids appears to be dependent upon the concentration of the alkali fluoride mineralizer, pressure, temperature, and reaction time. Differential scanning calorimetry (DSC) studies show that all of the different phases of cesium thorium fluoride transition into the same monoclinic phase of CsThF₅ and eventually into the orthorhombic phase of CsTh₃F₁₃.     

Bioinspired synthesis of pure massicot phase lead oxide nanoparticles and assessment of their biocompatibility,cytotoxicity and in-vitro biological properties

Green and ecofriendly route for biosynthesis of lead oxide nanoparticles has been successfully demonstrated using aqueous leaf extracts of Sageretia thea (Osbeck.). Biosynthesized PbO (∼27 nm) nanoparticles were extensively characterized using XRD, FTIR, Raman, EDS etc. Morphology was studied through HR-TEM/SEM. As synthesized nanoparticles were investigated for their iv-vitro biological properties. Antibacterial activities revealed enhancement upon modulation by UV in a concentration dependent manner. Pseudomonas aeruginosa was found to be the most resistant strain (MIC = 250 µg/mL and MIC^uv = 31.25 µg/ml). MTT cytotoxicity on leishmania promastigotes and amastigotes revealed significant inhibition as indicated by their IC₅₀ values of 14.7 µg/mL and 11.95 µg/m respectively. Cytotoxicity was also confirmed using brine shrimp lethality (IC₅₀ = 27.7 µg/mL). Bio-compatibility evaluation indicated cytotoxicity to freshly isolated human macrophages (IC₅₀ = 57.1 µg/mL). Insignificant alpha-amylase inhibition and moderate protein kinase inhibition was revealed. Antioxidant activities indicated free radical scavenging activity (58 ± 2.45) at 200 µg/mL. Moderate total reducing power and total antioxidant activity was also indicated. Overall, we conclude lead oxide as a potential candidate for biological applications, however further studies are recommended on their in vitro and in vivo cytotoxicity.     

Synthesis and structural characterization of a novel two-dimensional 3d-4f heterometallic coordination framework based on pentanuclear lanthanide cluster

A novel 3d-4f heterometallic coordination polymer, {[Tm₅(μ₃-OH)₂(BDC)₆(IN)₂Cu(H₂O)₂]·(H₂O)₃}_n (1) [BDC = benzene-1,2-dicarboxylate, IN = isonicotinate], has been hydrothermally synthesized and structurally characterized by single crystal X-ray diffraction, FTIR, elemental analysis, powder X-ray diffraction and thermogravimetric analysis. The compound crystallizes in monoclinic system, space group P2₁/c (No. 14), a = 13.7302(5) Å, b = 23.5428(3) Å, c = 21.5789(2) Å, β = 91.491(3)°, V = 6973.0(3) ų, and Z = 4. The structure exhibits unusual two-dimensional Tm-carboxylate layer, which is constructed from the expansion of novel pentanuclear {Tm₅} clusters. More interestingly, the heterometallic Cu(I) ions were successfully planted into such Ln-carboxylate layer by the bifunctional IN bridging ligands, resulting in the formation of an unprecedented 2D heterometallic lanthanide-transition-metal framework.     

Synthesis,spectral characterization and crystal structure of a novel trinuclear di-n-butyltin(IV) complex with pyruvic acid-N(4)-cyclohexylthiosemicarbazone (H2PACT)

A new trinuclear di-n-butyltin(IV) complex with pyruvic acid-N(4)-cyclohexylthiosemicarbazone (H₂PACT) ligand was synthesized and characterized by elemental analyses, molar conductivity, UV–Vis, FT-IR, ¹H, ¹¹⁹Sn NMR spectroscopy and single crystal X-ray study. Single crystal X-ray diffraction data revealed that this complex was trinuclear cyclic fashion with the pyruvic acid-N(4)-cyclohexylthiosemicarbazone ligand. In the trinuclear di-n-butyltin(IV) complex, the ligand (H₂PACT) is coordinated to the central tin(IV) atoms via the carboxylato-O, the azomethine-N and the thiolato-S atoms. The trinuclear tin system is formed by the bridges through the carbonyl oxygen atom of the carboxylate moieties and making the tin atom of seven coordinated in distorted pentagonal bipyramidal geometry. Single crystal X-ray data indicates that the complex (1) crystallized in cubic system with space group I-4₃d, a = b = c = 30.3273(17) Å, α = β = γ = 90°, Z = 16, μ(MoKα) = 1.209 mm^?1, F(000) = 12,144, and final R₁ = 0.0390, wR₂ = 0.0843 for observed reflections 4582(I > 2σ(I)).     

Synthesis,spectral characterization and crystal structure of a novel trinuclear di-n-butyltin(IV) complex with pyruvic acid-N(4)-cyclohexylthiosemicarbazone (H2PACT)

A new trinuclear di-n-butyltin(IV) complex with pyruvic acid-N(4)-cyclohexylthiosemicarbazone (H₂PACT) ligand was synthesized and characterized by elemental analyses, molar conductivity, UV–Vis, FT-IR, ¹H, ¹¹⁹Sn NMR spectroscopy and single crystal X-ray study. Single crystal X-ray diffraction data revealed that this complex was trinuclear cyclic fashion with the pyruvic acid-N(4)-cyclohexylthiosemicarbazone ligand. In the trinuclear di-n-butyltin(IV) complex, the ligand (H₂PACT) is coordinated to the central tin(IV) atoms via the carboxylato-O, the azomethine-N and the thiolato-S atoms. The trinuclear tin system is formed by the bridges through the carbonyl oxygen atom of the carboxylate moieties and making the tin atom of seven coordinated in distorted pentagonal bipyramidal geometry. Single crystal X-ray data indicates that the complex (1) crystallized in cubic system with space group I-4₃d, a = b = c = 30.3273(17) Å, α = β = γ = 90°, Z = 16, μ(MoKα) = 1.209 mm⁻¹, F(000) = 12,144, and final R₁ = 0.0390, wR₂ = 0.0843 for observed reflections 4582(I > 2σ(I)).     

Phytochemical analysis and antidiabetic efficacy of Morus rubra

Morus rubra (red mulberry) is a folk medicine used in management of diabetes. The aim of this article to investigate the antidiabetic activity of hydro alcoholic leaf extracts of Morus rubra in the sprague dawley male rats (SD) model. Authentication of plant material, total Phenolic contents, total flavonoid contents, HPLC analysis, in-vitro antioxidant activity, acute toxicity, in-vivo oral glucose tolerance test, in-vivo STZ induced antidiabetic activity along with biochemical parameters (triglycerides, low-density lipoprotein, high-density lipoprotein, total cholesterol, serum glutamate phosphotransferase, serum glutamate oxaloacetic acid transferase, urea and creatinine). The total phenolic contents 60.32 ​± ​0.80 ​mg/g GAE (gallic acid equivalent) were found higher in ethanolic extract. The total flavonoids 16 ​± ​0.42 ​mg/g QE (quercetin equivalent) were found in petroleum ether extract. M. rubra leaf extracts were tested by HPLC for qualitative and quantitative analysis. 100 ​mg of the dried powder of Morus leaves was dissolve in methanol: water (80:20, v/v) for analysis. Chromatograms of HPLC show the presence of chlorogenic acid 0.55 mg/gm, quercetin 1.90 ​mg/g, isoquercetin 0.68 mg/gm and rutin 0.10 mg/gm. IC₅₀ (Inhibitory concentration) value has been found higher in chloroform extract (92.89 ​μg/ml). Metformin drug is used for positive control, which causes 14.6% improvement in glucose tolerance while M. rubra has been found 11.4. % at the dose of 300 ​mg/kg body wt in normal rats. In STZ treated diabetic rats, it reduces 13.0% blood glucose level while metformin reduces 21.9% up to dosing level of 300 ​mg/kg body wt. It produces reduction in biochemical parameters like, total cholesterol (TC), triglycerides (TG), SGPT, LDL, urea, creatinine and SGOT while HDL has been increased. Results show the hydro-alcoholic leaves extract of Morus rubra exhibited antidiabetic, antioxidant and hypolipidemic properties. This suggests that M. rubra has great potential to develop novel antidiabetic drug to manage this disastrous disease.