Scientific validation of the antimicrobial and antiproliferative potential of Berberis aristata DC root bark, its phytoconstituents and their biosafety

Abstract Berberis aristata is an important part of traditional healing system from more than 2500 years. The aqueous extract of Berberis aristata root bark displayed broad spectrum activity against 13 test pathogens, ranging from 12 to 25 mm. In classical optimization, 15% concentration prepared at 40 °C for 40 min was optimal and thermostable. Statistical optimization enhanced the activity by 1.13–1.30-folds. Ethyl acetate was the best organic solvent to elute out the potential compound responsible for antimicrobial activity. Diterpenes were the most abundant phytoconstituent (15.3%) and showed broad spectrum antimicrobial activity ranging from 16.66 to 42.66 mm. Ethyl acetate extract displayed the lowest minimum inhibitory concentration (0.05–1 mg/mL), followed by diterpenes (0.05–5 mg/mL) and flavonoids (0.05–10 mg/mL). The test extracts were microbicidal in nature and showed a prolonged post antibiotic effect ranging from 2 to 8 h. They were found to be biosafe as per Ames and MTT assay. The in vitro cytotoxicity evaluation of diterpenes against L20B, RD and Hep 2 cell lines revealed its IC50 ranging from 245 to 473 µg/mL. Acute oral toxicity of diterpenes on Swiss albino mice did not show any changes in behavioral pattern, body weight, biochemical parameters as well as organs’ architecture. The study thus indicates B. aristata could be a potential candidate for development of potent drug owing to its antimicrobial potential and biosafe profile.

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ISOLATION OF DIHYDROQUERCETIN GLYCOSIDE FROM THE ROOT BARK OF CALOTROPIS PROCERA AND ANTIOXIDANT AND CYTOTOXIC SCREENING OF THE CRUDE EXTRACTS.

Journal of Chemical Society of Nigeria ◽

10.46602/jcsn.v46i1.576 ◽

2021 ◽

Vol 46 (1) ◽

Author(s):

A. Usman ◽

R.H. Mohammad ◽

A.O. Abdullahi ◽

A.H. Zakari ◽

N.L. Usman

Keyword(s):

Ethyl Acetate ◽

In Vitro Cytotoxicity ◽

Water Soluble ◽

Calotropis Procera ◽

Root Bark ◽

Cytotoxicity Activity ◽

Crude Extracts ◽

Isolated Compound ◽

Soluble Fractions

The root bark of Calotropis procera (Family: Asclepiadaceae) was extracted with methanol. The methanolic extract was separated into hexane, chloroform, ethyl acetate, and water soluble fractions. The ethyl acetate fraction was subjected to bioassay-guided fractionation and final purification was achieved by column chromatography. The structure of the compound was elucidated by spectroscopic methods (ESI-MS, 1H and C NMR, COSY, HSQC, and HMBC) and the comparison of the data obtained with that reported in the literature. It was concluded that the compounds isolated was taxifolin 4’-O-β-D-glucopyranoside, a dihydroquercetin glycoside. The crude extracts of hexane, chloroform, ethylacetate, and water soluble fractions of methanol extract and the isolated compound were subjected to antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and brine shrimp lethality bioassay. The result shows that the maximum inhibitions in the DPPH assays were isolated compound (51.7 %), methanol (80.7 %), and water (29.2 %) fractions while ascorbic acid standard was (84.4 %). However, the results for hexane, chloroform and ethyl acetate fractions in the DPPH assays were poor and hence discarded. The results for the in vitro cytotoxicity activity shows that ethyl acetate and hexane fractions showed significant cytotoxicity with LC50 value of 1.0±0.2 and 2.4 ±0.1 respectively.

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In vitro antimicrobial activity of mexican plants on bovine mastitis bacteria: preliminary studies

Bioscience Journal ◽

10.14393/bj-v36n1a2020-42137 ◽

2020 ◽

Vol 36 (1) ◽

Author(s):

Mariana Macías Alonso ◽

Julio C. López Salazar ◽

Soraya Osegueda Robles ◽

Iván Córdova Guerrero ◽

Fernanda Ledezma García ◽

...

Keyword(s):

Antimicrobial Activity ◽

Low Cost ◽

Bovine Mastitis ◽

Ethanolic Extract ◽

Clinical Mastitis ◽

Potential Candidate ◽

Salmonella Spp ◽

Shigella Spp ◽

In Vitro Antibacterial Activity

The present study aimed to evaluate the efficacy of traditionally used antibacterial plants (Euphorbia prostrata, Schinus molle, Brickellia veronicaefolia and Lepidium virginicum) in Santa Rosa Range in Guanajuato against major mastitis-causing pathogens. The selected plants were phytochemically screened for alkaloids, flavonoids, polyphenols, saponins, anthraquinone, cardiac glycosides, steroids and terpenoids. Moreover, to achieve the main purpose of the present research, extracts of selected plants were tested for in vitro antibacterial activity against Staphylococcus aureus, Escherichia coli, Shigella spp., Bacillus subtilis, Clavibacter spp., Proteus vulgaris and Salmonella spp. All these bacterial were isolated from clinical mastitis in dairy cows. The results indicated that the ethanolic extract of the aerial part of L. virginicum exhibited the strongest antimicrobial activity, and it could be potential candidate specie for the development of novel veterinary drugs with low cost and fewer side effects.

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CONSTITUENTS AND INHIBITORY EFFECT ON HUMAN PATHOGENIC BACTERIA OF THE ROOTS OF SCUTELLARIA BAICALENSIS

Vietnam Journal of Science and Technology ◽

10.15625/2525-2518/57/1/12886 ◽

2019 ◽

Vol 57 (1) ◽

pp. 7

Author(s):

Duc Long Le ◽

Huu Tung Nguyen ◽

Thi Thom Nguyen ◽

Gyung Ja Choi ◽

Dinh Hoang Vu ◽

...

Keyword(s):

Ethyl Acetate ◽

Pathogenic Bacteria ◽

Inhibitory Effect ◽

Scutellaria Baicalensis ◽

Plant Materials ◽

Chemical Structures ◽

Human Pathogenic Bacteria ◽

Antibiotic Effect ◽

Study Results

Abstract-HCTN_16Methanol extract of the roots of Scutellaria baicalensis effectively inhibited the bacterial growth of human pathogenic bacteria Staphylococcus aureus ATCC 6538, Bacillus cereus ATCC 21768 and Bacillus subtilis ATCC 6633 at MICs of 2,000 µg/mL. n-Hexane, ethyl acetate and aqueous residues were prepared by successively partitioning the methanol extract with n-hexane and ethyl acetate. Among them, only ethyl acetate layer showed antibiotic effect; whereas n-hexane and aqueous layers were inactive against tested bacteria. The ethyl acetate residue was fractionated by silica gel column chromatography to afford three flavonoids and an oligosaccharide. Their chemical structures were elucidated as wogonin (SB1), baicalein (SB4), baicalin (SB5) and tetrasaccharide (SB10) on the basis of the analysis of NMR and MS spectroscopic data. The isolates were evaluated for in vitro inhibitory effect against human pathogenic bacteria using micro dilution bioassay method. Baicalein (SB4) showed a broad-spectrum inhibition against various human pathogenic bacteria. In particular, it was found to potently inhibit S. aureus ATCC 6538 and B. cereus ATCC 21768 with MICs of 9.5 and 38 µg/mL, respectively. The study results demonstrated antibiotic effect of the extracts from the roots of S. baicalensis and characterization of compounds isolated from the plant materials.

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Development, Characterization, and Evaluation of Novel Broad-Spectrum Antimicrobial Topical Formulations from Cymbopogon martini (Roxb.) W. Watson Essential Oil

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2018/9812093 ◽

2018 ◽

Vol 2018 ◽

pp. 1-16 ◽

Cited By ~ 3

Author(s):

Negero Gemeda ◽

Ashenif Tadele ◽

Hirut Lemma ◽

Biruktawit Girma ◽

Getachew Addis ◽

...

Keyword(s):

Antimicrobial Activity ◽

Essential Oil ◽

Broad Spectrum ◽

Chemical Constituents ◽

Trichophyton Mentagrophytes ◽

Microsporum Canis ◽

Skin Infections ◽

Topical Formulations ◽

Life Study

Background. Skin infections were the most frequently encountered of all infections and the 4th leading cause of nonfatal disease burden. Topical drugs have been used for the management of skin infections. The growing concern of drug resistance to the topical agents has warned the need for continuous development of novel drug. Essential oils are the best candidate for new drug with different mode of action and target as they are rich in chemical constituents. Objective. To evaluate and develop safe and effective topical antimicrobial formulations from essential oil of Cymbopogon martini. Method. Essential oil was extracted using hydrodistillation aerial part C. martini and topical formulations were prepared in five different semisolid bases. In vitro antimicrobial investigations were performed on essential oil and topical formulations. Skin sensitizations of the formulations were evaluated using guinea pig maximization. Results. The essential oil of C. martini has shown broad-spectrum antimicrobial potency against all tested organisms with MIC value ranging from 0.65 to 10 μg/ml. Absolute inhibitions of growth of fungi were observed against Trichophyton mentagrophytes and Trichophyton rubrum at concentrations above 1% of oil and against Microsporum canis and Trichophyton verrucosum at a concentration of 4% oil. Among topical formulations, the highest antimicrobial activity was recorded in hydrophilic ointment followed by macrogol blend ointment. The antimicrobial activity of oil was higher in fungal pathogen compared to bacteria. Gram positive bacteria were more sensitive than gram negative bacteria. Hydrophilic and macrogol blend ointment containing 5% oil did not produce any skin sensitization on guinea pigs. Conclusion. In conclusion, topical formulations of C. martini essential oil can be alternative topical agents with safe broad-spectrum activity for the treatment of skin disorder. Further studies should focus on shelf life study and clinical study of the product.

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IN VITRO ANTIMICROBIAL ACTIVITY OF CYNODON DACTYLON (L.) PERS. LEAF EXTRACTS. ANTIMICROBIAL ACTIVITY BY ZONE OF INHIBITION ESTIMATION

INDIAN DRUGS ◽

10.53879/id.52.04.10125 ◽

2015 ◽

Vol 52 (04) ◽

pp. 37-41

Author(s):

S. M Pawaskar ◽

◽

K. C. Sasangan

Keyword(s):

Antimicrobial Activity ◽

Antifungal Activity ◽

Ethyl Acetate ◽

Petroleum Ether ◽

Cynodon Dactylon ◽

Diffusion Method ◽

Zone Of Inhibition ◽

Leaf Extracts ◽

In Vitro Antimicrobial Activity

The present study was undertaken to evaluate in vitro antimicrobial activity of the successive leaf extracts of Cynodon dactylon in petroleum ether, ethyl acetate, acetone, ethanol, methanol and water, against various gram positive & gram negative bacterial strains using zone of inhibition. Both Agar well diffusion method & Agar disc diffusion method were used to evaluate the antibacterial efficacy. The microorganisms used in the test were – Escherichia coli, Proteus vulgaris, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Shigella flexneri, Salmonella typhi, Salmonella paratyphi A, Salmonella paratyphi B, Bacillus subtilis, Streptococcus pyogenes, Vibrio cholerac and Enterobacter aerogenes. Two fungal strains - Candida albicans and Saccharomyces cerevisiae were also tested to evaluate the antifungal potential of the said plant extract. The reference antibiotics chloramphenicol & ampicillin (antibacterial); nystatin & clotrimazole and (antifungal) were also tested against these standard microorganisms used in the assay and the results were compared with that of the plant extracts.The results of the study revealed that all the seven successive extracts of the leaf powder of Cynodon dactylon ( L.) Pers. exhibited prominent antimicrobial and antifungal activity against all microorganisms used in the study. The nonpolar extracts i.e. petroleum ether, ethyl acetate and acetone showed the most significant antibacterial and antifungal activity against all tested organisms. The petroleum ether and ethyl acetate extracts showing maximum inhibition in the range of 8 mm - 15 mm. This was closely followed by, acetone extract, which showed the inhibition in the range of 9 mm - 13 mm.

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Punicalagin Regulates Key Processes Associated with Atherosclerosis in THP-1 Cellular Model

Pharmaceuticals ◽

10.3390/ph13110372 ◽

2020 ◽

Vol 13 (11) ◽

pp. 372

Author(s):

Sanaa Almowallad ◽

Etimad Huwait ◽

Rehab Al-Massabi ◽

Salma Saddeek ◽

Kalamegam Gauthaman ◽

...

Keyword(s):

Cholesterol Efflux ◽

Cell Model ◽

In Vitro Cytotoxicity ◽

Intercellular Adhesion Molecule ◽

Potential Candidate ◽

Monocyte Chemoattractant Protein 1 ◽

Cytotoxicity Assays ◽

Monocyte Migration ◽

Ifn Γ

Atherosclerosis may lead to cardiovascular diseases (CVD), which are the primary cause of death globally. In addition to conventional therapeutics for CVD, use of nutraceuticals that prevents cholesterol deposition, reduce existing plaques and hence anti-atherosclerotic effects of nutraceuticals appeared to be promising. As such, in the present study we evaluated the beneficial effects of punicalagin, a phytochemical against an atherosclerotic cell model in vitro. Cytotoxicity assays were examined for 10 µM concentration of punicalagin on THP-1 macrophages. Real-time-polymerase chain reaction (RT-PCR) was used to analyze monocyte chemoattractant protein-1 (MCP-1) and Intercellular adhesion molecule (ICAM-1) expressions. Monocyte migration and cholesterol efflux assays were performed to investigate punicalagin’s further impact on the key steps of atherosclerosis. Cytotoxicity assays demonstrated no significant toxicity for punicalagin (10 µM) on THP-1 macrophages. Punicalagin inhibited the IFN-γ-induced overexpression of MCP-1 and ICAM-1 in macrophages by 10 fold and 3.49 fold, respectively, compared to the control. Punicalagin also reduced the MCP-1- mediated migration of monocytes by 28% compared to the control. Percentages of cellular cholesterol efflux were enhanced in presence or absence of IFN-γ by 88% and 84% compared to control with 58% and 62%, respectively. Punicalagin possesses anti-inflammatory and anti-atherosclerotic effects. Punicalagin also did not exhibit any cytotoxicity and therefore can be considered a safe and potential candidate for the treatment and prevention of atherosclerosis.

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Validation of Cocoa Shell as a Novel Antioxidant Dietary Fiber Food Ingredient: Nutritional Value, Functional Properties, and Safety

Current Developments in Nutrition ◽

10.1093/cdn/nzaa052_042 ◽

2020 ◽

Vol 4 (Supplement_2) ◽

pp. 773-773

Author(s):

Miguel Rebollo-Hernanz ◽

Silvia Cañas ◽

Yolanda Aguilera ◽

Vanesa Benitez ◽

Andrea Gila-Díaz ◽

...

Keyword(s):

Dietary Fiber ◽

Functional Properties ◽

Nutritional Value ◽

Antioxidant Properties ◽

Potential Candidate ◽

Oral Toxicity ◽

Food Ingredient ◽

Sustainable Food ◽

Cocoa Shell

Abstract Objectives To study the nutritional value of cocoa shell, analyzing the chemical composition and functional properties as antioxidant, hypoglycemic and hypocholesterolemic effects, as well as validate the safety of cocoa shell as a sustainable food ingredient. Methods Proximate composition was determined following the AOAC methods. Soluble and insoluble fractions of dietary fiber (DF) were determined using enzymatic-gravimetric and chemical methods. The phenolic profile was analyzed by UPLC-MS/MS and antioxidant properties were tested using ABTS. Furthermore, physicochemical, hypoglycemic, and hypocholesterolemic properties were assessed in vitro. Acute and subchronic oral toxicity experiments were performed following OECD Guidelines 452 and 408 (5 male and 5 female C57BL/6 mice per group, vehicle/cocoa shell) to assess the food safety of cocoa shell flours. Results Cocoa shell was composed of carbohydrates (62%), proteins (16%), and fat (2%). DF represents 59%, being the insoluble dietary fiber (IDF) the main fraction (82%). IDF fraction was constituted by lignin (58%) and polysaccharides (42%); cellulose was inferred as the main polysaccharide of IDF, followed by hemicelluloses (arabinans and galactans). High content of phenolic compounds (33.7 mg/g) was shown, being a significant phenolic fraction (51%) bound to DF, which confers cocoa shell its antioxidant potential (73.1 mg Trolox eq/g). The main phenolics were protocatechuic acid, (−)-epicatechin, and (+)-catechin. Cocoa shell exhibited adequate water and oil holding properties to be included in food matrices. During in vitro digestion, starch hydrolysis and dialyzed glucose diminished (34 and 13%, respectively) due to α-amylase inhibition (18%) and glucose adsorption (31%). Cocoa shell also inhibited cholesterol and bile salts absorption (72 and 70%, respectively). The intake of acute (2000 mg/kg) and subcronical (1000 mg/kg) doses of the ingredient did not cause significant lesions in selected isolated vital organs (liver, spleen, and kidney) nor changes in histological parameters, ensuring the safety of this sustainable food ingredient. Conclusions Results validate the use of cocoa shell as an antioxidant dietary fiber ingredient, being a safe potential candidate to be incorporated in the development of foods for specific health uses. Funding Sources Ministry of Science and Innovation.

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In Vitro and In Vivo Bioactivity of Tricalcium Phosphate and Fluoroapatite Nanoparticles for Medical Implants

Science of Advanced Materials ◽

10.1166/sam.2020.3563 ◽

2020 ◽

Vol 12 (1) ◽

pp. 101-109

Author(s):

H. Algarni ◽

Ibrahim Alshahrani ◽

Essam H. Ibrahim ◽

Refaat A. Eid ◽

Mona Kilany ◽

...

Keyword(s):

Antimicrobial Activity ◽

Antimicrobial Activities ◽

Potential Candidate ◽

Medical Implants ◽

Splenic Cells ◽

Acute Cytotoxicity ◽

Good Potential ◽

Sbf Solution

A novel 40P2O5–20Na2O–10Ca(OH)2–20CaCl2–6.0ZnO–2.0BaF2–2.0TiO2 (BGBaFTi) bioglasses is prepared. The reaction of the glasses in SBF solution is characterized by XRD and SEM indicated that the carbonate hydroxyapatite has formed rapidly on the glasses. BGBaFTi bioglasses was tested for its antimicrobial activity, anti-proliferative/cytotoxicity against normal and activated splenic cells in vitro and in vivo. This results showed that BGBaFTi has antimicrobial activities against Gram negative and positive bacteria as well as fungi. We found that the antimicrobial activity of nanoparticles of BGBaFTI is high than the normal powder of it. Moreover BGBaFTi (powder and nanoparticle) with cytotoxic effect on normal splenic cells was investigated. The products of activated splenic cells did not cause any changes in the structure of BGBaFTi. It did not cause any acute cytotoxicity or lysis to RBCs which was not affected by lytic products of immune cells. The bioactivity and biocompatibility of the present glasses use it a good potential candidate in the field of tissue engineering.

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