Activated carbon derived from Dodonaea Viscosa into beads of calcium-alginate for the sorption of methylene blue (MB): Kinetics, equilibrium and thermodynamics.

Dyes are valuable color compounds used in textile industries but at the same time their toxic and carcinogenic properties distract environmental system due to the chemical intricacy and multiplicity smearing them non-biodegradable. Therefore, the aim of present research rests in the use of cost effective, easily available and eco-friendly reformed novel biosorbents of Dodonaea Viscosa (DV). For this purpose AC-alginate beads were synthesized successfully through clogging AC derived from Dodonaea Viscosa (ACAB) into beads of calcium-alginate for removal of methylene blue (MB) from diluted solution. The external morphology (SEM, EDX) and functional groups (FT-IR) supported the favorable conditions for adsorption. The thermal properties have been evaluated using thermo-gravimetric study (TGA). After proper optimization like at pH 8, and biosorbent dose of 250 mg, temperature 350 K and time at 60 min the obtained adsorption capacity for DV leaves was set up to be 239 mg/g and for ACAB was 370 mg/g. By applying different adsorption isotherm models, the Freundlich was found to be best suited with highest R2 = 0.998 for DV and 0.995 for ACAB biosorbents. While the various kinetics models were also verified and data was well matched to Pseudo-second order kinetics model (R2 = 0.99 for DV and 0.99 for ACAB). Thermodynamics parameters enlightened that the adsorption process was endothermic (ΔH = 19,097 for ACAB and 10,899.6 J/mol for DV, ΔS = 89,087 for ACAB and 5.94 (J/mol for DV) and spontaneous in nature. The desorption study was satisfactory up to five number of absorption-desorption cycles for both the adsorbents particularly ACAB reflected an excellent percent removal (>90%). Consequently, the viability of DV can be used as a possible potential precursor for AC preparation besides cost effective adsorbent in the real sample treatment for dye removal.

Biomolecular Screening of Pimpinella anisum L. for Antioxidant and Anticholinesterase Activity in Mice Brain.

Hundreds of the plants have been explored and evaluated for antioxidant and anti-amnesic activities, so far. This study was designed to report the biomolecules of Pimpinella anisum L. for the said activities. The aqueous extract of dried P. anisum seeds was fractionated via column chromatography and the fractions so obtained were assessed for the inhibition of acetylcholinesterase (AChE) via in vitro analysis. The fraction which best inhibited AChE was so named as the P. anisum active fraction (P.aAF). The P.aAF was then chemically analyzed via GCMS, which indicated that oxadiazole compounds were present in it. The P.aAF was then administered to albino mice to conduct the in vivo (behavioral and biochemical) studies. The results of the behavioral studies indicated the significant (p < 0.001) increase in inflexion ratio, by the number of hole-pokings through holes and time spent in a dark area by P.aAF treated mice. Biochemical studies demonstrated that the oxadiazole present in P.aAF on one hand presented a noteworthy reduction in MDA and the AChE level and on the other hand promoted the levels of CAT, SOD and GSH in mice brain. The LD50 for P.aAF was calculated as 95 mg/Kg/p.o. The findings thus supported that the antioxidant and anticholinesterase activities of P. anisum are due to its oxadiazole compounds.

A Comprehensive Review of the Ethnotraditional Uses and Biological and Pharmacological Potential of the Genus Mimosa.

The Mimosa genus belongs to the Fabaceae family of legumes and consists of about 400 species distributed all over the world. The growth forms of plants belonging to the Mimosa genus range from herbs to trees. Several species of this genus play important roles in folk medicine. In this review, we aimed to present the current knowledge of the ethnogeographical distribution, ethnotraditional uses, nutritional values, pharmaceutical potential, and toxicity of the genus Mimosa to facilitate the exploitation of its therapeutic potential for the treatment of human ailments. The present paper consists of a systematic overview of the scientific literature relating to the genus Mimosa published between 1931 and 2020, which was achieved by consulting various databases (Science Direct, Francis and Taylor, Scopus, Google Scholar, PubMed, SciELO, Web of Science, SciFinder, Wiley, Springer, Google, The Plant Database). More than 160 research articles were included in this review regarding the Mimosa genus. Mimosa species are nutritionally very important and several species are used as feed for different varieties of chickens. Studies regarding their biological potential have shown that species of the Mimosa genus have promising pharmacological properties, including antimicrobial, antioxidant, anticancer, antidiabetic, wound-healing, hypolipidemic, anti-inflammatory, hepatoprotective, antinociceptive, antiepileptic, neuropharmacological, toxicological, antiallergic, antihyperurisemic, larvicidal, antiparasitic, molluscicidal, antimutagenic, genotoxic, teratogenic, antispasmolytic, antiviral, and antivenom activities. The findings regarding the genus Mimosa suggest that this genus could be the future of the medicinal industry for the treatment of various diseases, although in the future more research should be carried out to explore its ethnopharmacological, toxicological, and nutritional attributes.

Ethylene Biosynthesis Inhibition Combined with Cyanide Degradation Confer Resistance to Quinclorac in Echinochloa crus-galli var. mitis.

Echinochloa crus-galli var. mitis has rarely been reported for herbicide resistance, and no case of quinclorac resistance has been reported so far. Synthetic auxin-type herbicide quinclorac is used extensively to control rice weeds worldwide. A long history of using quinclorac in Chinese rice fields escalated the resistance in E. crus-galli var. mitis against this herbicide. Bioassays in Petri plates and pots exhibited four biotypes that evolved into resistance to quinclorac ranking as JS01-R > AH01-R > JS02-R > JX01-R from three provinces of China. Ethylene production in these biotypes was negatively correlated with resistance level and positively correlated with growth inhibition. Determination of the related ethylene response pathway exhibited resistance in biotypes that recorded a decline in 1-aminocyclopropane-1-carboxylic acid (ACC) content, ACC synthase oxidase activities, and less inducible ACS and ACO genes expressions than the susceptible biotype, suggesting that there was a positive correlation between quinclorac resistance and ethylene biosynthesis inhibition. Cyanides produced during the ethylene biosynthesis pathway mainly degraded by the activity of ß-cyanoalanine synthase (ß-CAS). Resistant biotypes exhibited higher ß-CAS activity than the susceptible ones. Nucleotide changes were found in the EcCAS gene of resistant biotypes as compared to sensitive ones that caused three amino acid substitutions (Asn-105-Lys, Gln-195-Glu, and Gly-298-Val), resulting in alteration of enzyme structure, increased binding residues in the active site with its cofactor, and decreased binding free energy; hence, its activity was higher in resistant biotypes. Moreover, these mutations increased the structural stability of the enzyme. In view of the positive correlation between ethylene biosynthesis inhibition and cyanide degradation with resistance level, it is concluded that the alteration in ethylene response pathway or at least variation in ACC synthase and ACC oxidase enzyme activities-due to less relative expression of ACS and ACO genes and enhanced ß-CAS activity, as well as mutation and increased relative expression of EcCAS gene-can be considered as a probable mechanism of quinclorac resistance in E. crus-galli var. mitis.

Natural Products as Alternative Choices for P-Glycoprotein (P-gp) Inhibition.

Multidrug resistance (MDR) is regarded as one of the bottlenecks of successful clinical treatment for numerous chemotherapeutic agents. Multiple key regulators are alleged to be responsible for MDR and making the treatment regimens ineffective. In this review, we discuss MDR in relation to P-glycoprotein (P-gp) and its down-regulation by natural bioactive molecules. P-gp, a unique ATP-dependent membrane transport protein, is one of those key regulators which are present in the lining of the colon, endothelial cells of the blood brain barrier (BBB), bile duct, adrenal gland, kidney tubules, small intestine, pancreatic ducts and in many other tissues like heart, lungs, spleen, skeletal muscles, etc. Due to its diverse tissue distribution, P-gp is a novel protective barrier to stop the intake of xenobiotics into the human body. Over-expression of P-gp leads to decreased intracellular accretion of many chemotherapeutic agents thus assisting in the development of MDR. Eventually, the effectiveness of these drugs is decreased. P-gp inhibitors act by altering intracellular ATP levels which are the source of energy and/or by affecting membrane contours to increase permeability. However, the use of synthetic inhibitors is known to cause serious toxicities. For this reason, the search for more potent and less toxic P-gp inhibitors of natural origin is underway. The present review aims to recapitulate the research findings on bioactive constituents of natural origin with P-gp inhibition characteristics. Natural bioactive constituents with P-gp modulating effects offer great potential for semi-synthetic modification to produce new scaffolds which could serve as valuable investigative tools to recognize the function of complex ABC transporters apart from evading the systemic toxicities shown by synthetic counterparts. Despite the many published scientific findings encompassing P-gp inhibitors, however, this article stand alones because it provides a vivid picture to the readers pertaining to Pgp inhibitors obtained from natural sources coupled with their mode of action and structures. It provides first-hand information to the scientists working in the field of drug discovery to further synthesise and discover new P-gp inhibitors with less toxicity and more efficacies.

One Pot Selective Arylation of 2-Bromo-5-Chloro Thiophene; Molecular Structure Investigation via Density Functional Theory (DFT), X-ray Analysis, and Their Biological Activities.

Synthesis of 2,5-bisarylthiophenes was accomplished by sequential Suzuki cross coupling reaction of 2-bromo-5-chloro thiophenes. Density functional theory (DFT) studies were carried out at the B3LYP/6-31G(d, p) level of theory to compare the geometric parameters of 2,5-bisarylthiophenes with those from X-ray diffraction results. The synthesized compounds are screened for in vitro bacteria scavenging abilities. At the concentration of 50 and 100 µg/mL, compounds 2b, 2c, 2d, 3c, and 3f with IC50-values of 51.4, 52.10, 58.0, 56.2, and 56.5 µg/mL respectively, were found most potent against E. coli. Among all the synthesized compounds 2a, 2d, 3c, and 3e with the least values of IC50 77, 76.26, 79.13 µg/mL respectively showed significant antioxidant activities. Almost all of the compounds showed good antibacterial activity against Escherichia coli, whereas 2-chloro-5-(4-methoxyphenyl) thiophene (2b) was found most active among all synthesized compound with an IC50 value of 51.4 µg/mL. All of the synthesized compounds were screened for nitric oxide scavenging activity as well. Frontier molecular orbitals (FMOs) and molecular electrostatic potentials of the target compounds were also studied theoretically to account for their relative reactivity.

Robust Synthesis of Ciprofloxacin-Capped Metallic Nanoparticles and Their Urease Inhibitory Assay.

The fluoroquinolone antibacterial drug ciprofloxacin (cip) has been used to cap metallic (silver and gold) nanoparticles by a robust one pot synthetic method under optimized conditions, using NaBH4 as a mild reducing agent. Metallic nanoparticles (MNPs) showed constancy against variations in pH, table salt (NaCl) solution, and heat. Capping with metal ions (Ag/Au-cip) has significant implications for the solubility, pharmacokinetics and bioavailability of fluoroquinolone molecules. The metallic nanoparticles were characterized by several techniques such as ultraviolet visible spectroscopy (UV), atomic force microscopy (AFM), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and energy dispersive X-ray (EDX) methods. The nanoparticles synthesized using silver and gold were subjected to energy dispersive X-ray tests in order to show their metallic composition. The NH moiety of the piperazine group capped the Ag/Au surfaces, as revealed by spectroscopic studies. The synthesized nanoparticles were also assessed for urease inhibition potential. Fascinatingly, both Ag-cip and Au-cip NPs exhibited significant urease enzyme inhibitory potential, with IC50 = 1.181 ± 0.02 µg/mL and 52.55 ± 2.3 µg/mL, compared to ciprofloxacin (IC50 = 82.95 ± 1.62 µg/mL). MNPs also exhibited significant antibacterial activity against selected bacterial strains.

Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach.

A new series of N-(6-arylbenzo[d]thiazol-2-yl)acetamides were synthesized by C-C coupling methodology in the presence of Pd(0) using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolyl)benzo[d]thiazol-2-yl)acetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition.

The effects of two common edible herbs, Ipomoea aquatica and Enhydra fluctuans, on cadmium-induced pathophysiology: a focus on oxidative defence and anti-apoptotic mechanism.

BACKGROUND: Ipomoea aquatica (Convolvulaceae) and Enhydra fluctuans (Asteraceae), two aquatic vegetables, are traditionally used against heavy metal toxicity in traditional medicines in India. The present study aimed to explore the protective role of edible (aqueous) extracts of I. aquatica (AEIA) and E. fluctuans (AEEF) against Cd-intoxication. METHODS: The extracts were chemically standardized by spectroscopic and HPLC analysis. The cytoprotective roles of AEIA and AEEF were measured on mouse hepatocytes. The effect on redox status were measured after incubating the hepatocytes with CdCl2 (30 µM) along with AEIA or AEEF (400 µg/ml). The effects on the expressions of apoptotic signal proteins were estimated. The protective roles of AEIA or AEEF were measured by in vivo assay in mice. Haematological, serum biochemical, tissue redox status, Cd bioaccumulation and histological parameters were evaluated to estimate the protective role of AEIA or AEEF (100 mg/kg) against CdCl2 (4 mg/kg) intoxication. RESULTS: Phytochemical analysis revealed presence of substantial quantities of phenolics, flavonoids, saponins, carbohydrates and ascorbic acid in AEIA or AEEF. CdCl2 treated murine hepatocytes showed a gradual reduction of cell viability in a concentration dependent manner with an IC50 of ~30 µM. CdCl2 treated hepatocytes exhibited significantly enhanced levels (p < 0.01) of ROS production, lipid peroxidation, protein carbonylation and NADPH oxidase with concomitant depletion (p < 0.01) of antioxidant enzymes and GSH. However, AEIA or AEEF treatment along with CdCl2 significantly restored the aforementioned parameters in murine hepatocytes near to normalcy. Besides, AEIA or AEEF significantly counteracted (p < 0.05-0.01) with ROS mediated alteration of transcription levels of signal proteins viz. Bcl-2, BAD, Cyt-C, Caspases, Fas and Bid. In in vivo bioassay, CdCl2 treatment caused significantly high Cd bioaccumulation and oxidative stress in the liver, kidney, heart, brain and testes in mice. In addition, the haematological and serum biochemical parameters were significantly altered in the CdCl2 treated animals. Simultaneous administration of AEIA or AEEF could significantly restore the tested parameters to the near-normal status. CONCLUSION: The extracts would offer the overall protective effect via counteracting with Cd mediated oxidative stress and/or promoting the elimination of Cd by chelating.

Ameliorative effect of water spinach, Ipomea aquatica (Convolvulaceae), against experimentally induced arsenic toxicity.

BACKGROUND: Ipomea aquatica (Convolvulaceae) is traditionally used against Arsenic (As) poisoning in folk medicines in India. The present study was designed to explore the therapeutic role of aqueous extract of I. aquatica (AEIA) against As-intoxication. METHODS: AEIA was chemically standardized by spectroscopic and chromatographic analysis. The cytoprotective role of AEIA was measured on isolated murine hepatocytes. The effect on redox status were measured after incubating the hepatocytes with NaAsO2 (10 µM) + AEIA (400 µg/ml). The protective effect of AEIA (400 µg/ml) in expressions of apoptotic proteins were estimated in vitro. The protective role of AEIA was measured by in vivo assay in mice. Haematological, biochemical, As bioaccumulation and histological parameters were evaluated to ensure the protective role of AEIA (100 mg/kg) against NaAsO2 (10 mg/kg) intoxication. RESULTS: Phytochemical analysis revealed presence of substantial quantities of phenolics, flavonoids, saponins and ascorbic acid in AEIA. Incubation of murine hepatocytes with AEIA (0-400 µg/ml) + NaAsO2 (10 µM) exerted a concentration dependent cytoprotective effect. Incubation of murine hepatocytes with NaAsO2 (10 µM, ~ IC50) induced apoptosis via augmenting oxidative stress. NaAsO2 treated hepatocytes exhibited significantly (p < 0.01) enhanced levels of ROS production, lipid peroxidation and protein carbonylation with concomitant depletion of antioxidant enzymes (p < 0.05-0.01) and GSH (p < 0.01) levels. However, AEIA (400 µg/ml) + NaAsO2 (10 µM) could significantly (p < 0.05-0.01) reinstate the aforementioned parameters to near-normal status. Besides, AEIA (400 µg/ml) could significantly counteract (p <0.05-0.01) ROS mediated alteration in the expressions of apoptotic proteins viz. Bcl-2, BAD, Cyt C, Apaf 1, caspases, Fas and Bid. In in vivo bioassay, NaAsO2 (10 mg/kg) treatment in mice caused significantly (p < 0.05-0.01) elevated As bioaccumulation, ATP levels, DNA fragmentations and oxidative stress in the liver, kidney, heart, brain and testes along with alteration in cytoarchitecture of these organs. In addition, the serum biochemical and haematological parameters were significantly (p < 0.05-0.01) altered in the NaAsO2-treated animals. However, concurrent administration of AEIA (100 mg/ml) could significantly reinstate the NaAsO2-induced pathogenesis. CONCLUSION: Presence of substantial quantities of dietary antioxidants within AEIA would be responsible for overall protective effect.

Abroma augusta L. (Malvaceae) leaf extract attenuates diabetes induced nephropathy and cardiomyopathy via inhibition of oxidative stress and inflammatory response.

BACKGROUND: Abroma augusta L. (Malvaceae) leaf is traditionally used to treat diabetes in India and Southern Asia. Therefore, current study was performed to evaluate the protective effect of defatted methanol extract of A. augusta leaves (AA) against type 2 diabetes mellitus (T2DM) and its associated nephropathy and cardiomyopathy in experimental rats. METHODS: Antidiabetic activity of AA extracts (100 and 200 mg/kg, p.o.) was measured in streptozotocin-nicotinamide induced type 2 diabetic (T2D) rat. Fasting blood glucose level (at specific interval) and serum biochemical markers (after sacrifice) were measured. Redox status, transcription levels of signal proteins (NF-κB and PKCs), mitochondria dependent apoptotic pathway (Bad, Bcl-2, caspase cascade) and histological studies were performed in kidneys and hearts of controls and AA treated diabetic rats. RESULTS: Phytochemical screening of extracts revealed the presence of taraxerol, flavonoids and phenolic compounds in the AA. T2D rats showed significantly (p < 0.01) elevated fasting blood glucose level. Alteration in serum lipid profile and release of membrane bound enzymes like lactate dehydrogenase and creatine kinase, which ensured the participation of hyperlipidemia and cell membrane disintegration in diabetic pathophysiology. T2DM caused alteration in the serum biochemical markers related to diabetic complications. T2DM altered the redox status, decreased the intracellular NAD and ATP concentrations in renal and myocardial tissues of experimental rats. Investigating the molecular mechanism, activation PKC isoforms was observed in the selected tissues. T2D rats also exhibited an up-regulation of NF-κB and increase in the concentrations of pro-inflammatory cytokines (IL-1ß, IL-6 and TNF-α) in the renal and cardiac tissues. The activation of mitochondria dependent apoptotic pathway was observed in renal and myocardial tissues of the T2D rats. However, Oral administration of AA at the doses of 100 and 200 mg/kg body weight per day could reduce hyperglycemia, hyperlipidemia, membrane disintegration, oxidative stress, vascular inflammation and prevented the activation of oxidative stress induced signaling cascades leading to cell death. Histological studies also supported the protective characteristics of AA. CONCLUSIONS: Results suggest that AA could offer prophylactic role against T2DM and its associated reno- and cardio- toxicity.

Preventive role of green tea catechins from obesity and related disorders especially hypercholesterolemia and hyperglycemia.

BACKGROUND: During the last few years, scientific investigations have proposed diet based regimens to prevent several health ailments including obesity, hypercholesterolemia and diabetes. In this regard, a promising tool is the use of functional foods/nutraceuticals. Present research project was an attempt to explore nutraceutical worth of locally grown green tea variety (Qi-Men) against lifestyle related disorders. METHODS: Functional drinks (T2 and T3) were prepared by adding catechins and epigallocatechin gallate (EGCG) @ 550 mg/500 mL and compared with control (T1). These functional drinks were tested in experimental rats modeling (Sprague Dawley). Based on diets, four studies were conducted i.e. trial-I (normal diet), trial-II (high cholesterol diet), trial-III (high sucrose diet), trial-IV (high cholesterol + high sucrose diet). Rats were monitored daily for their feed and drink intake while body weight was measured on weekly basis. After period of 56 days rats were sacrificed and evaluated their serum lipid (cholesterol, LDL and HDL), glucose and insulin levels. RESULTS: Results for feed consumption by rats revealed that highest feed intake was recorded in group provided control drink than other groups. However, non significant differences were noted among all groups for drink consumption. Functional drinks resulted in significant reduction in body weight with maximum lowering noted in trial-II and III i.e. 10.73 to 8.49% and 10.12 to 10.49%, respectively. Likewise, cholesterol and LDL were substantially reduced with 14.42% decrease observed in trial-IV and 30.43% in trial-II, respectively. Furthermore, serum glucose and insulin levels were also lowered significantly in the trial-III and IV while in trial-I and II differences were non-significant. In contrast to lipid profile, experimental drink containing EGCG reduced the trait better than catechins based functional drink. CONCLUSIONS: The drinks supplemented with catechins and EGCG are effective against obesity, hypercholesterolemia and hyperglycemia.

Pharmacological justification of use of Solena heterophylla Lour. in gastrointestinal, respiratory and vascular disorders.

BACKGROUND: Solena heterophylla Lour. has traditionally been used in the management of diseases pertaining to gastrointestinal, respiratory and vascular system and present study was undertaken to validate its traditional uses. METHODS: The aqueous ethanolic extract of Solena heterophylla Lour (Sh.Cr) was tested in-vitro on isolated rabbit jejunum, tracheal and aorta preparations. The responses of tissues were recorded using isotonic transducers coupled with PowerLab data acquisition system. RESULTS: The aqueous ethanolic extract of Solena heterophylla Lour (Sh.Cr) (0.03-1.0 mg/ml) on application to spontaneous contractions in isolated rabbit jejunum preparation exerted relaxant effect through decrease in magnitude and frequency of contractions, caused relaxation of K(+)(80 mM)-induced contractions and shifted the Ca(2+) concentration response curves toward right in isolated rabbit jejunum preparations in a manner similar to verapamil (a standard Ca(2+) channel blocker), thus confirming its Ca(2+) channel blocking activity. The Sh.Cr also caused relaxation of carbachol (1 µM)- and K(+)(80 mM)-induced contractions in isolated rabbit tracheal preparations in a manner comparable to dicyclomine. CONCLUSIONS: The observed relaxant effect may be outcome of anti-muscarinic and Ca(2+) channel blocking activities. The Sh.Cr (0.03-1.0 mg/ml) against phenyephrine (1 µM)- and K(+)(80 mM)-induced contractions in isolated rabbit aortic preparations exerted a relaxant effect, possibly through Ca(2+) channel blocking activity. These findings provide a rationale for the folkloric uses of the plant in the management of ailments pertaining to gastrointestinal, respiratory and vascular system.

Cadmium toxicity affects chlorophyll a and b content, antioxidant enzyme activities and mineral nutrient accumulation in strawberry.

BACKGROUND: Cadmium (Cd) is well known as one of the most toxic metals affecting the environment and can severely restrict plant growth and development. In this study, Cd toxicities were studied in strawberry cv. Camarosa using pot experiment. Chlorophyll and malondialdehyde (MDA) contents, catalase (CAT), superoxide dismutase (SOD), ascorbate peroxidase (APX) activities and mineral nutrient concentrations were investigated in both roots and leaves of strawberry plant after exposure Cd. RESULTS: Cd content in both roots and leaves was increased with the application of increasing concentrations of Cd. We found higher Cd concentration in roots rather than in leaves. Chlorophyll a and b was decreased in leaves but MDA significantly increased under increased Cd concentration treatments in both roots and leaves. SOD and CAT activities was also increased with the increase Cd concentrations. K, Mn and Mg concentrations were found higher in leaves than roots under Cd stress. In general, increased Cd treatments increased K, Mg, Fe, Ca, Cu and Zn concentration in both roots and leaves. Excessive Cd treatments reduced chlorophyll contents, increased antioxidant enzyme activities and changes in plant nutrition concentrations in both roots and leaves. CONCLUSION: The results presented in this work suggested that Cd treatments have negative effect on chlorophyll content and nearly decreased 30% of plant growth in strawberry. Strawberry roots accumulated higher Cd than leaves. We found that MDA and antioxidant enzyme (CAT, SOD and APX) contents may have considered a good indicator in determining Cd tolerance in strawberry plant.

Pharmacological basis of the use of the root bark of Zizyphus nummularia Aubrev. (Rhamnaceae) as anti-inflammatory agent.

BACKGROUND: The root bark of Zizyphus nummularia (Rhamnaceae) is traditionally used as an anti-inflammatory agent. The current study aimed to explore the anti-inflammatory activity (in vivo) of a crude ethanolic extract (EE) and the pure identified octadecahydro-picene-2,3,14,15-tetranone (IC) in the root bark of Z. nummularia. IC was further subjected to suitable in vitro and in silico studies to find out the mechanistic pharmacology. METHODS: EE (100 and 200 mg/kg, p.o.) and (IC) (400 and 600 µg/kg, p.o.) were subjected to in vivo anti-inflammatory assays to evaluate the anti-inflammatory activity and predict the probable mechanism(s) of action. Suitable acute (carrageenan-induced paw edema, arachidonic acid-induced ear edema, xylene-induced ear edema) and chronic (cotton pellet granuloma) models were employed to investigate in vivo the anti-inflammatory activity. Based on in vivo observation, IC was further subjected to in vitro assays to estimate the inhibition of nitric oxide (NO), prostaglandin-E2 (PGE-2) and tumor necrosis factor-α (TNF-α) production in PBS stimulated RAW 264.7 cells. Based on the observation of in vitro studies, finally, ADME prediction and molecular docking studies of IC were performed for better understanding of interaction of IC with TNF-α. RESULTS: Oral administration of EE (100 and 200 mg/kg) exhibited significant inhibition of carrageenan (p < 0.05) and arachidonic acid (p < 0.05) induced oedema, and the reduced the granuloma tissue formation (p < 0.05) in experimental mice. IC (400 and 600 µg/kg, p.o.) exhibited significant (p < 0.01) inhibition of carrageenan, xylene and arachidonic acid-induced edema, and reduced the granuloma tissue formation. In in vitro assays, IC caused a concentration-dependent inhibition of LPS stimulated NO (up to ~ 67.4% at 50 µM) and TNF-α (~84.5% at 50 µM) production. However, the PGE-2 inhibition did not follow dose dependent pattern. Based on in vitro observations, the molecular docking has been performed on the basis of interaction with TNF-α. In in silico studies, it was observed that IC showed hydrogen bonding with GLN 47 amino acid residue of TNF-α protein. CONCLUSIONS: IC possibly produces anti-inflammatory activity through inhibition of TNF-α and NO production.

Validation of ethnopharmacological uses of Murraya paniculata in disorders of diarrhea, asthma and hypertension.

BACKGROUND: Murraya paniculata is traditionally used for management of gut, air way and cardiovascular disorders. The study was conducted for provision of pharmacological rationalization for folkloric uses of Murraya paniculata in gut, air way and cardiovascular problems. METHODS: Aqueous-ethanolic extract of Mp.Cr was tested using in vitro techniques on isolated tissue of rabbit (jejunum, trachea and aorta) to detect the possible presence of spasmolytic activity. The responses of tissues were recorded using isotonic transducers coupled with PowerLab data acquisition system. RESULTS: Application of the extract of Mp.Cr relaxed spontaneous and high K(+) (80mM)-induced contraction in rabbit jejunum preparation. Because it shifted the CRCs (Calcium response curve) towards the right side so the possible blockade was of calcium channel similar to verapamil. In rabbit trachea, extract of Mp.Cr produced relaxation of carbachol and high K(+) induced contractions. When plant extract was checked further on isolated aorta for its possible vasodilator effect, it caused relaxation of phenylephrine and high K(+)-induced spastic contractions at different doses. CONCLUSION: These results indicate that Murraya paniculata shows anti-spasmodic, bronchodilator and vasodilator activity facilitated through Ca(++) antagonist mechanisms.

Validation of ethnopharmacological uses of Heliotropium strigosum Willd. as spasmolytic, bronchodilator and vasorelaxant remedy.

BACKGROUND: Heliotropium strigosum is used in traditional medicine to manage gastrointestinal pain, respiratory distress and vascular disorders. The present study was undertaken to provide scientific evidences for these folkloric uses by in vitro experimental settings. METHODS: A crude methanol extract of the Heliotropium strigosum (Hs.Cr) was tested in vitro on isolated rabbit jejunum preparations to detect the possible presence of spasmolytic activity. Moreover, isolated rabbit tracheal and aorta preparations were used to ascertain the relaxant effects of the extract. RESULTS: The Hs.Cr exhibited relaxant effects in rabbit jejunum in a concentration dependent manner (0.01-3.0 mg/ml). The Hs.Cr also relaxed K(+) (80 mM)-induced spastic contractions in rabbit jejunum and shifted the Ca(2+) concentration response curves towards right. The extract relaxed carbachol (1 µM)- as well as K(+) (80 mM)-induced contractions in rabbit trachea at concentrations ranging from 0.01 to 10 mg/ml. Moreover, Hs.Cr. also relaxed (0.01-3.0 mg/ml) the phenylephrine (1 µM)- and K(+) (80 mM)-induced contractions in isolated rabbit aorta. CONCLUSIONS: The Hs.Cr was found to exhibit spasmolytic, bronchodilator and vasorelaxant activities on isolated rabbit jejunum, trachea and aorta preparations, likely mediated through Ca(2+) channel blockade. This finding may provide a scientific basis for the folkloric uses of the plant.

Anti-platelet effects of nimesulide in isoproterenol-induced myocardial ischaemia and infarction in rabbits.

BACKGROUND: The present study was designed to determine the effects of cyclooxygenase-2 (COX-2) inhibitor-nimesulide on platelet activating factor (PAF) and arachidonic acid (AA)-induced platelet aggregation during myocardial infarction (Ml) and ischaemia in rabbits. METHODS: Rabbits were divided into three groups; group I served as control and contains normal rabbits that received saline, group II rabbits received saline before induction of Ml, and group Ill rabbits received nimesulide (25 mg/kg) before Ml induction. Myocardial infarction was induced by isoproterenol (ISP) (65 mg/kg) and confirmed by biochemical, electrophysiological and histopathological methods. Platelet aggregation was induced with arachidonic acid (AA) and platelet activating factor (PAF), and monitored by using light transmission aggregometery. RESULTS: When platelets were challenged with two different aggregating agents, nimesulide-treated infarcted rabbits showed resistance to platelet aggregation while non-treated infarcted rabbits were found prone to aggregation with both aggregating agents (P < 0.05). CONCLUSION: These results suggest platelet inhibitory effects of nimesulide during experimental ischaemia and infarction in rabbits.

Synthesis, Density Functional Theory (DFT), Urease Inhibition and Antimicrobial Activities of 5-Aryl Thiophenes Bearing Sulphonylacetamide Moieties.

A variety of novel 5-aryl thiophenes 4a-g containing sulphonylacetamide (sulfacetamide) groups were synthesized in appreciable yields via Pd[0] Suzuki cross coupling reactions. The structures of these newly synthesized compounds were determined using spectral data and elemental analysis. Density functional theory (DFT) studies were performed using the B3LYP/6-31G (d, p) basis set to gain insight into their structural properties. Frontier molecular orbital (FMOs) analysis of all compounds 4a-g was computed at the same level of theory to get an idea about their kinetic stability. The molecular electrostatic potential (MEP) mapping over the entire stabilized geometries of the molecules indicated the reactive sites. First hyperpolarizability analysis (nonlinear optical response) were simulated at the B3LYP/6-31G (d, p) level of theory as well. The compounds were further evaluated for their promising antibacterial and anti-urease activities. In this case, the antibacterial activities were estimated by the agar well diffusion method, whereas the anti-urease activities of these compounds were determined using the indophenol method by quantifying the evolved ammonia produced. The results revealed that all the sulfacetamide derivatives displayed antibacterial activity against Bacillus subtiles, Escherichia coli, Staphylococcus aureus, Shigella dysenteriae, Salmonella typhae, Pseudomonas aeruginosa at various concentrations. Furthermore, the compound 4g N-((5-(4-chlorophenyl)thiophen-2-yl)sulfonyl) acetamide showed excellent urease inhibition with percentage inhibition activity ~46.23 ± 0.11 at 15 µg/mL with IC50 17.1 µg/mL. Moreover, some other compounds 4a-f also exhibited very good inhibition against urease enzyme.

Synthesis and Consecutive Reactions of α-Azido Ketones: A Review.

This review paper covers the major synthetic approaches attempted towards the synthesis of α-azido ketones, as well as the synthetic applications/consecutive reactions of α-azido ketones.