Ameliorative effect of ethanolic extract of Limnophila rugosa (Scrophulariaceae) in paracetamol- and carbon tetrachloride-induced hepatotoxicity in rats

Background Limnophila rugosa (Scrophulariaceae) is a perennial aquatic plant used as a diuretic and digestive tonic as well as in the treatment of diarrhea, dysentery, dyspepsia and urinary ailments. Genus Limnophila has been reported as hepatoprotective. The present study was undertaken to evaluate the hepatoprotective activity of the ethanolic extract of L. rugosa aerial part in paracetamol- and carbon tetrachloride-induced (CCl4) hepatotoxicity in albino Wistar rats. Ethanolic extract was subjected to high-performance liquid chromatography (HPLC) analysis for the estimation of phenolic and flavonoid compounds and gas chromatography–mass spectrometry (GC–MS) analysis for phytochemical analysis. The in vitro antioxidant activity was carried out by 2,2-diphenyl-1-picrylhydrazyl, nitric oxide radical and hydrogen peroxide assay. Hepatoprotective potential of L. rugosa was studied in paracetamol (750 mg/mg)- and CCl4 (1.25 ml/kg)-induced liver damage in albino rats at dose 200 and 300 mg/kg using silymarin (100 mg/kg) as standard. Lipid peroxidation, superoxide dismutase (SOD), catalase (CAT) and glutathione (GSH) were determined in liver tissue homogenate. Serum biochemical and histopathological examination was performed. Molecular docking analysis was performed to understand the molecular mechanism of hepatoprotective activity. Results HPLC analysis revealed predominance of rutin. GC–MS analysis revealed camphor as principal component. Ethanolic extract exhibited significant concentration-dependent scavenging efficacy. The altered biochemical chemical parameters: aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, bilirubin, cholesterol, albumin, globulin and total protein, were significantly improved at 200 and 300 mg/kg in experimental rats. Extract signified hepatoprotective by decreasing lipid peroxidation and upregulating SOD, CAT and GSH. The findings were well supported by histological analysis. 2-Butyl-2, 7-octadien-1-ol (-5.8) and camphor (-4.8) gave the highest docking score on the transforming growth factor-β1. Conclusions The ameliorative effect of L. rugosa in the rat model of hepatotoxicity could be attributed to its antioxidant potential and bioactive principles such as betulin, 5-hydroxy-6,7,4′-trimethoxyflavone (salvigenin), betulinic acid, ursolic acid, 3-octanol, acetophenone, anisylacetone, caryophyllene, cis-anethole and the compounds camphor and 2-butyl-2,7-octadien-1-ol identified from GC–MS analysis.

Free-radical Scavenging and Quantitative Estimation of Flavonoids from the Polar Extracts of Corchorus depressus Leaves

Background: The investigation of total flavonoids and antioxidant activity of polar extracts of Corchorus depressus is the major aim of this study. As observed from ancient literatures and folkloric claims the plant Corchorus depressus worshipped by the married women of Odisha, India, in the rituals called as “Jama Jutia”, possesses different biological activities including antioxidant property. Methods: The diphenyl picryl hydrazine, hydroxyl radical and nitric oxide radical scavenging methods were performed for measurement of the antioxidant activity at different extracts. The flavonoid and phenolic content of the extracts were determined by using aluminium chloride and Folin-Ciocalteau’s reagent (FCR) methods respectively. Results: The results for estimation of total phenolic content (mg/ 100 g) expressed as gallic acid equivalent (GAE) and total flavonoid (mg/ 100 g) in weight of quercetin equivalent (QE) was highest in methanolic extract 78.46 and 21.2 respectively, followed by 18.18 mg/100 g in GAE and 1.80 mg/100 g in QE for aqueous extract. Conclusion: The methanolic extract of C. depressus at 100µg/ml showed highest DPPH, hydroxyl and nitric oxide radical scavenging activity and this activity may be attributed to the presence of saponins and flavonoids as detected in the extract.

In-vitro Anti-Oxidant Property of Vallarai (Centella asiatica) cultivated by conventional and traditional Methods

In ancient times, Siddhars have been described and also used the traditional methods to cultivate the anti-oxidant herbs for rejuvenation purpose and also they are listed some plants as anti-oxidant herbs. They were used Semicarpus anacardium manure for cultivation of anti-oxidant plants. In Siddha, these anti-oxidant herbs are mentioned as Kayakarpam (Rejuvenation therapy). Most of the Non Communicable Diseases (NCD) are caused by oxidative stress. These anti-oxidant herbs are helps to reduce oxidative stress and prevent the incidence of NCDs. Centella asiatica (Vallarai) is one of the Kayakarpa medicinal plants. The traditional cultivation method for Kayakarpa herbs are also described in Siddha especially for Centella asiatica (Vallarai). Therefore, this study was aimed to validate the in-vitro anti-oxidant property of Vallarai cultivated by conventional (sample A) and traditional methods (sample B). The study samples were screened for anti-oxidant activity by DPPH assay, Nitric Oxide radical scavenging assay, ABTS assay and H2O2 radical scavenging assay and the IC50 value of the study drug, sample-A was 88.6 ± 8.536 (μg /ml), 183 ± 15.55 (μg/ml), 78.92 ± 8.43 (μg /ml) and 183 ± 11.64 (μg /ml) whereas sample- B was 57.06 ± 1.221 (μg /ml); 145.1 ± 13.12 (μg/ml); 96.45 ± 3.966 (μg /ml) and 132.3 ± 18.71 (μg /ml) respectively. This study results revealed that, both samples are possessing anti-oxidant property and sample B have greater scavenging activity compared to sample A. Hence, The Traditional method can be adopted for cultivation of anti-oxidant herbs, which helps to retain the active components and enhances the anti-oxidant potency of medicinal herbs.

Evaluation of the Leaf Extracts of Kalanchoe pinnata and Kalanchoe daigremontiana Chemistry, Antioxidant and Anti-inflammatory Activity

The aim of this study was to analyze the chemical components and evaluate the biological activity of the extracts from the leaves Kalanchoe pinnata and Kalanchoe daigremontiana, which are cultivated in the province of Chiriqui, Republic of Panama. Phytochemicals components, antioxidant and anti-inflammatory activities were studied. The composition of the obtained petroleum ether, ethanol and aqueous extracts was analyzed by phytochemical screening. The antioxidant activity of the extracts was studied using three in vitro model systems (DPPH radical scavenging assay, nitric oxide radical scavenging assay, and superoxide radical scavenging activity). The anti-inflammatory activity of these species was studied using an in vivo model (ʎ-carrageenan-induced paw edema in rats). Phytochemical analysis of the extracts showed the presence of alkaloids, steroids, triterpenes, flavonoids, phenolic compounds, saponins and glycosides. The greatest radical inhibitory effect was observed in the DPPH model where the ethanolic extracts of both species developed a concentration-dependent inhibitory effect, the K. pinnata extract reached a maximum inhibitory effect of 49.5 ± 5.6% (2000

Phytochemical Screening, In-vitro Antioxidant and Cytotoxic potentials of Brachychiton rupestris Leaves

Few studies had been conducted on the phytochemical profile and the biological activities of Brachychiton rupestris. The antioxidant activity of 85% methanolic extract of B. rupestris leaves and its derived fractions was assessed using five different in-vitro assays which are DPPH• assay, phosphomolybdenum assay (TAC), hydroxyl radical (•OH) scavenging assay, nitric oxide radical (NO•) scavenging assay and permanganate reducing antioxidant capacity (PRAC). The total phenolic, flavonoid and flavonol contents were also determined for the different plant samples using Folin-Ciocalteu, aluminum chloride and aluminum chloride/ sodium acetate methods, respectively. In-vitro cytotoxic activity of the crude extract and its fractions against HepG2 cell line was also evaluated via SRB assay. The ethyl acetate fraction obtained from the aqueous methanolic extract of the plant leaves possessed the most potent antioxidant potential according to the different applied assays (DPPH• SC50 = 25.50±0.76 µg/mL, TAC= 311.98±1.19 mg AAE/g ext., •OH SA= 68.42±0.15%, NO• SA= 33.68±1.98% & PRAC = 62.88±0.27%). It also owed the highest amount of phenolics (TPC= 342.10±2.08 mg GAE/ g ext.) whose majority were flavonoids (TFC= 309.82±3.64 mg QE/ g ext.). A strong positive correlation was found between the total phenolic contents of various plant samples and their antioxidant activity. The butanol derived fraction exhibited the most potent cytotoxic activity (IC50 = 8.60 µg/mL). To the best of our knowledge, it is the first study reporting the antioxidant and the cytotoxic activities of B. rupestris leaves. The study revealed that the B. rupestris leaves could be a good source of natural antioxidants which may be applied in food and pharmaceutical industries. They could also be a new opportunity of discovering anti-mutagenic agents.

Antioxidant, nutritional and physicochemical quality of yoghurt produced from milk- based fermentation mix enhanced with food spices

Utilization of natural additives, which could meet the growing need for ‘clean label’ and value addition with respect to diseases prevention and health promotion in humans, is a current interest in the yoghurt industry. In this study, yoghurt recipes derived from standard milk -based fermentation mix enhanced with African black pepper (ABP), Turmeric, or Cloves extracts were evaluated for antioxidant, nutritional and physico-chemical quality. Each fermentation mix was pasteurized; inoculated with 0.5% industrial starter culture containing Streptococcus thermophillus and Lactobacillus delbrueckii subsp. Bulgaricus (1:1); and then allowed to ferment in fermentation tank for 9 hours at 40OC. The results revealed that, clove- enriched yoghurt recipe exhibit the strongest antioxidant capacity as indicated by significant increase (p < 0.05) in total phenolics, total flavonoids, Total Antioxidant Capacity (TAC), DPPH radical scavenging activity, nitric oxide radical scavenging activity, Ferric ion reducing power (FRAP), and inhibition of lipid peroxidation but also reduced apparent viscosity and organoleptic properties. Similarly, ABP increased the antioxidant characteristics, with increased protein content and gel viscosity. Turmeric extracts significantly increased (p < 0.05) the calcium content and reduced syneresis. In conclusion, fermentation of milk-based mix containing ABP extract resulted in yoghurt which combines improved antioxidant characteristics with increased protein and enhanced techno-functionality.

Determination of Total Phenolic Content and Antioxidant Activity of the Whole Plant Extracts of Argyreia imbricata (Roth) Sant. & Patel

Plants of the genus Argyreia posses’ ethno medicinal importance and various pharmacological activities are also reported. In this study, phenolic content, anti-oxidant potential of different extracts of Argyreia imbricata was evaluated. Extraction of powdered whole plant material was done with different solvents viz., petroleum ether, chloroform, ethyl acetate and methanol by soxhelation. The estimation of phenolics in the selected extracts of Argyreia imbricata was done by using a Folin-Ciocalteau reagent. The antioxidant potential of different extracts was evaluated by total anti-oxidant capacity, DPPH, hydroxyl and nitric oxide radical scavenging and reducing power assay methods. In the phenolics estimation, the methanol extract showed a significant presence of phenolic content followed by ethyl acetate extract. In case of anti-oxidant activity, the methanol and ethyl acetate extract showed a significant activity based on their concentration. The findings of this study clearly revealed the potential of methanol extract of A. imbricata in phenolic content and anti-oxidant activity. Also, the ethyl acetate extract showed significant results. Further studies on identification, isolation of the active constituents, toxicity evaluations may give useful results.

Radical Releasing Anti-Tuberculosis Agents and the Treatment of Mycobacterial Tuberculosis Infections – An Overview

: The treatment and management of tuberculosis (TB) is a major global concern. Approved drugs for the treatment of TB to date displayed various modes of action which can be grouped into radical releasing and non-radical releasing anti TB agents. Radical releasing agents are of special interest because they diffuse directly into the mycobacterium cell wall, interact with the host cell DNA causing DNA strand breakages and fatal destabilization of the DNA helix inhibiting nucleic acid synthase. As a therapeutic agent with aforementioned activity, nitroimidazoles and most especially bicyclic nitroimidazoles are currently in clinical use for the treatment of tuberculosis. However, the approved drugs, pretomanid (PR) and delamanid (DE) are limited in their nitric oxide radical (NO•) releasing abilities to cause effective bactericidity. It is believed that their bactericidal activity can be improved by harnessing alternative strategies to increase NO• release. The last decade has witness the strategic inclusion of NO-donors into native drugs to improve their activities and/or reverse resistance. The rationale behind this strategy is the targeting of NO• release at specific therapeutic sites. This review therefore aims to highlight various radical releasing agents that may be effective in the treatment of TB. The review also investigates various structural modification to PR and DE and suggests alternative strategies to improve NO• release as well as some applications where NO-donor hybrid drugs have been used with good therapeutic effect.

In Vitro Synthesis, Structure elucidation and its antioxidant properties of Platinum(IV)-hydrazide complexes: Molecular modeling of free-hydrazides suggested as potent lipoxygenase inhibitor

Background: Combination of biologically active ligand and metal in one molecule may increase the activity and reduce the toxicity. Objectives: In this study synthesis and characterization of platinum(IV) complexes with bioactive hydrazide ligands is discussed. Method: Elemental analysis, conductivity measurements and spectroscopic studies were used to elucidate the structure of complexes. Results: Our study suggests that hydrazide ligands coordinate with Pt(IV) in bidenate fashion. The platinum(IV) complexes have octahedral geometry with metal to ligand ratio of 1:2. Hydrazide ligands coordinated with central metal platinum(IV) by oxygen of carbonyl group and nitrogen of primary amine. Synthesized complexes exhibited variable DPPH radical scavenging and lipoxygenase inhibition activity. Furthermore, it is also found that Pt(IV)-hydrazide complexes are more potent superoxide and nitric oxide radical scavengers than their uncoordinated hydrazide ligands while in case of lipoxygenase enzyme inhibition, some of the free hydrazide ligands are more active than their respective Pt(IV) complexes. In silico docking technique explores molecular interactions of synthesized ligands in the active site of lipoxygenase enzyme. Predicted docking energies are in good agreement with experimental data suggesting that in silico studies might be useful for discovery of therapeutic candidates. Conclusion: Structure function relationship demonstrates that the radical scavenging and enzyme inhibition activities of the Pt(IV) compounds are effected by nature of ligand, position of substituent, electronic and steric effects. However, electronic factor seem to play more important role than other factors.

Phytochemical Contents and Antioxidant Activity of Medicinal Plants from the Rubiaceae Family in Thailand

Several plants of the Rubiaceae family possess potential pharmacological properties, such as antioxidant activity, for subsequent drug development. We investigated the methanolic extracts from the bark and wood of five Rubiaceae species for phenolic and flavonoid contents and antioxidant activity. Regarding the phytochemical contents and antioxidant activity, Mitragyna diversifolia wood (437.57 ± 9.90 mg GAE g-1) and Haldina cordifolia wood (30.11 ± 0.20 mg QE g-1) displayed the highest total phenolic content (TPC) and total flavonoid content (TFC) respectively. Morinda coreia bark followed the highest antioxidant activities (IC50 = 360.58 ± 19.28 µg ml-1) in the 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (DPPH), Catunaregam tomentosa bark (IC50 = 13.96 ± 5.32 µg ml-1) in the nitric oxide radical scavenging activity (NO), M. coreia wood (IC50 = 918.27 ± 0.16 µg ml-1) in the superoxide radical scavenging activity (SO) and M. coreia wood (IC50 = 236.65 ± 1.66 µg ml-1) in ferric reducing antioxidant power activity (FRAP). The TPC and TFC displayed strong correlations with DPPH in M. diversifolia wood and with FRAP in M. diversifolia bark and wood. We found high correlation between TFC and FRAP in all plant extracts except C. tomentosa wood, while no relation was detected between TFC and NO in all plant extracts. Comparing Rubiaceae species, the highest antioxidant potential were showed in C. tomentosa bark. Overall, it is worth mentioning that the Rubiaceae species exhibit potential as a promising source of natural antioxidants.