Evaluation of antioxidant, antibacterial and cytotoxicity activities of exopolysaccharide from Enterococcus strains isolated from traditional Iranian Kishk

2021 ◽  
Author(s):  
Paria Rahnama Vosough ◽  
Mohammad Bagher Habibi Najafi ◽  
Mohammad Reza Edalatian Dovom ◽  
Ali Javadmanesh ◽  
Baltasar Mayo
Keyword(s):  
Cytotoxicity Activities

Design, Synthesis and Antiplasmodial Evaluation of Sulfoximine-triazole Hybrids as Potential Antimalarial Prototypes

2019 ◽  
Vol 15 (6) ◽  
pp. 685-692 ◽  
Author(s):  
Tommy F. Mabasa ◽  
Babatunde Awe ◽  
Dustin Laming ◽  
Henok H. Kinfe
Keyword(s):  
Alkyl Substituent ◽  
Antimalarial Drugs ◽  
Significant Activity ◽  
Design Synthesis ◽  
Antimalarial Agents ◽  
Falciparum Strain ◽  
Physiological Properties ◽  
Resistant Strains ◽  
Cytotoxicity Activities ◽  
Drug Resistant Strains

Background:Malaria, caused by the deadly Plasmodium falciparum strain, claims the lives of millions of people annually. The emergence of drug-resistant strains of P. falciparum to the artemisinin-based combination therapy (ACT), the last line of defense against malaria, is worrisome and urges for the development of new chemo-types with a new mode of action. In the search of new antimalarial agents, hybrids of triazoles and other known antimalarial drugs have been reported to possess better activity than either of the parent compounds administered individually. Despite their better activity, no hybrid antimalarial drugs have been developed so far.Objective:In the hope of developing new antimalarial prototypes, we propose the design, synthesis and antimalarial evaluation of novel sulfoximine-triazole hybrids owing to their interesting biological and physiological properties.Methods:The sulfoximine part of the hybrid will be synthesized via imidation of the corresponding sulfoxide. Propargylation of the NH moiety of the sulfoximine followed by copper-catalyzed click chemistry with benzyl azide was envisaged to provide the target sulfoximine-triazole hybrids.Results:Five novel sulfoximine-triazole hybrids possessing various substituents on the sulfoximine moiety have been successfully synthesized and evaluated for their antiplasmodial and cytotoxicity activities. The results revealed that the co-presence of the sulfoximine and triazole moieties along with a lipophilic alkyl substituent on the sulfur atom impart significant activity.Conclusion:Sulfoximine-triazole hybrids could be used as a prototype for the synthesis of new derivatives with better antiplasmodial activities.

scholarly journals Plumbagin-Loaded Glycerosome Gel as Topical Delivery System for Skin Cancer Therapy

Polymers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 923
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Mohammad Husain ◽  
Nazia Khan ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Zeta Potential ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Skin Layer ◽  
Vesicle Size ◽  
Cytotoxicity Activities

Plumbagin (PLM) is a phytochemical which has shown cytotoxicity against of cancer cells both in vitro and in vivo. However, the clinical application of PLM has been hindered due to poor aqueous solubility and low bioavailability. The aim of the present study was to develop, optimize and evaluate PLM-loaded glycerosome (GM) gel and compare with conventional liposome (CL) for therapeutic efficacy against skin cancer. The GM formulations were optimized by employing design expert software by 3-level 3-factor design. The prepared GMs were characterized in vitro for vesicle size, size distribution, zeta potential, vesicle deformability, drug release, skin permeation, retention, texture, antioxidant and cytotoxicity activities. The optimized formulation showed a vesicle size of 119.20 ± 15.67 nm with a polydispersity index (PDI) of 0.145 ± 0.02, the zeta potential of −27 ± 5.12 mV and entrapment efficiency of 76.42 ± 9.98%. The optimized PLM-loaded GM formulation was transformed into a pre-formed gel which was prepared using Carbopol 934 polymer. The drug diffusion fluxes of CL gel and GM-loaded gel were 23.31 ±6.0 and 79.43 ± 12.43 µg/ cm2/h, respectively. The result of texture analysis revealed the adequate hardness, cohesiveness, consistency, and viscosity of the developed GM-loaded gel compared to CL gel. The confocal images showed that glycerosomal gel has deeper skin layer penetration as compared to the control solution. GM-loaded gel treated rat skin showed significantly (p < 0.05) higher drug accumulation in the dermis, higher cytotoxicity and higher antioxidant activity as compared to CL gel and PLM suspension. Thus, findings revealed that novel GM-loaded gel could be potential carriers for therapeutic intervention in skin cancer.

Gymnanthemum coloratum: Review of its Medicinal uses, Phytochemistry and Pharmacological Properties -

2020 ◽  
Vol 10 (5) ◽  
pp. 196-204
Author(s):  
Alfred Maroyi
Keyword(s):  
Traditional Medicine ◽  
Skin Diseases ◽  
Pharmacological Properties ◽  
Sources Of Information ◽  
Scientific Publications ◽  
Medicinal Uses ◽  
Sexually Transmitted ◽  
Plant Parts ◽  
Aerial Parts ◽  
Cytotoxicity Activities

Gymnanthemum coloratum is a shrub or a small tree widely used as traditional medicine throughout its distributional range in tropical Africa. The current study is aimed at reviewing the phytochemistry, pharmacological properties and medicinal uses of G. coloratum. Literature on pharmacological properties, phytochemistry and medicinal uses of G. coloratum was obtained from numerous internet sources such as Scopus, Elsevier, SciFinder, Google Scholar, Pubmed, ScienceDirect, BMC and Web of Science. Other sources of information included pre-electronic sources such as journal articles, theses, book chapters, books and other scientific publications obtained from the university library. The articles published between 1964 and 2020 were used in this study. The current study showed that G. coloratum is used as an anthelmintic, and traditional medicine for reproductive problems, schistosomiasis, liver diseases, sexually transmitted infections, diabetes, sores and wounds, respiratory problems, malaria, skin diseases, fever and gastro-intestinal problems. Ethnopharmacological research identified glaucolides, lactones, amino acids, essential oils, alkaloids, anthocyanins, cardenolids, coumarins, flavonoids, glycosides, leucoanthocyanins, phenols, quinones, reducing sugars, saponins, steroids, tannins, terpenoids and triterpenes from the aerial parts, leaves, roots and stems of G. coloratum. The aerial parts, leaves, roots and whole plant parts of G. coloratum and compounds isolated from the species exhibited anthelmintic, antimicrobial, anti-Blastocystis, anti-inflammatory, anti-sickling, insecticidal and larvicidal, antiplasmodial, antimalarial, antioxidant, antiproliferative, anti-Toxoplasma, hypoglycaemic and antidiabetic and cytotoxicity activities. Gymnanthemum coloratum should be subjected to detailed phytochemical, pharmacological and toxicological evaluations aimed at correlating its medicinal uses with its phytochemistry and pharmacological activities.

scholarly journals Maerua juncea Pax and M. schinzii Pax (Capparaceae): A comparative analysis of their ethnobotany and ethnomedicinal uses

2020 ◽  
Vol 11 (4) ◽  
pp. 6017-6022
Author(s):  
Alfred Maroyi
Keyword(s):  
Leaf Extracts ◽  
Scientific Publications ◽  
Respiratory Problems ◽  
Traditional Medicines ◽  
Plant Parts ◽  
Online Databases ◽  
Toxicological Studies ◽  
History Of ◽  
Cytotoxicity Activities ◽  
Ethnomedicinal Uses

Maerua juncea Pax and M. schinzii Pax have a long history of medicinal use in southern Africa. This study aimed to review the ethnomedicinal uses, phytochemistry and pharmacological properties of the two species. Results of this study are based on data derived from several online databases such as Scopus, Google Scholar, PubMed and Science Direct, and pre-electronic sources such as scientific publications, books, dissertations, book chapters and journal articles. The leaves, roots, stems or whole plant parts of M. juncea and M. schinzii are mainly used as protective charm and tonic, and traditional medicines for fever, heart problems, headache, earache, skin disorders, fatigue and respiratory problems. This study showed that betaines and quaternary ammonium compounds such as 3-hydroxyprolinebetaine, proline betaine and 3-hydroxy-1,1-dimethyl pyrrolidinium had been identified from the aerial parts of M. juncea. In contrast, alkaloids, bitter principles, coumarins, flavonoids, saponins and terpenes have been identified from the leaves of M. schinzii. The leaf extracts and compounds isolated from the species exhibited antibacterial, antifungal, anti-HIV and cytotoxicity activities. There is a need for extensive phytochemical, pharmacological and toxicological studies of crude extracts of M. juncea and M. schinzii to establish the safety profiles of different preparations of the two species.

scholarly journals Antibacterial and Cytotoxicity Activities of Major Compounds from Tinospora cordifolia Willd. Growing on Mangifera indica L.

2019 ◽  
Vol 3 (4) ◽  
pp. 32-42
Author(s):  
Thongchai Taechowisan
Keyword(s):  
Antibacterial Activity ◽  
Cell Lines ◽  
Crude Extract ◽  
Hek293 Cell ◽  
Colorimetric Assay ◽  
Mangifera Indica ◽  
Tinospora Cordifolia ◽  
Cytotoxicity Activity ◽  
Stem Extract ◽  
Cytotoxicity Activities

Objective To investigate the major constituents of Tinosporacordifolia Willd. growing on Mangiferaindica, and to evaluate the efficacy of their antibacterial and cytotoxicity activities. Methods The ethanolic stem extract of T. cordifolia was subjected to silica gel 60 column chromatography, thin layer chromatography and medium pressure liquid chromatography for isolation of the major compounds. Identification of purified compounds was achieved by spectroscopic methods.. The crude extract and purified compounds were screened for their antibacterial and cytotoxicity properties using standard procedures. Results Two alkaloids were purified and identified as Magnoflorin (1) and Tembetarine (2). These compounds showed high antibacterial activity against Bacillus cereus and Staphylococcus aureus with both MIC (32-64 µg/ml) and MBC (128-256 µg/ml). The cytotoxicity activity of the purified compounds and crude extract was determined using MTT colorimetric assay against L929 and HEK293 cell lines. This showed weak cytotoxicity activity with IC50 values of 1162.24 to 2290.00 µg/ml and 1376.67 to 2585.06 µg/ml towards L929 and HEK293 cell lines, respectively. Conclusion The major compounds present in ethanolic stem extract of T. cordifolia growing on M. indica were extracted, purified and identified. This study suggests that these compounds exhibit great potential for antibacterial activity with weak cytotoxicity activity. They may be useful for their medicinal functions.

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