scholarly journals Pharmacological and ADMET-based pharmacokinetic properties of Syzygium samarangense var. parviflorum leaf extract in in vitro, in vivo and in silico models

2020 ◽  
Vol 48 (3) ◽  
pp. 1155-1175
Author(s):  
Rahni HOSSAIN ◽  
Md A. RAHMAN ◽  
Md. K. J. RAFI ◽  
Tanvir A. SIDDIQUE ◽  
Abdullah A. NOMAN ◽  
...  

This research investigated pharmacological properties mainly the anti-inflammatory, anthelmintic, thrombolytic and anxiolytic potential of methanol extract of Syzygium samarangense (MESS) var. parviflorum. Anti-inflammatory action by bovine serum albumin, egg albumin denaturation and membrane stabilization, anthelmintic by live parasites, thrombolytic by clot lysis and anxiolytic by elevated plus maze (EPM) and light and dark box (LDB) tests were measured. The four targeted pharmacological properties were further justified using the most prevalent compounds, isolated from this plant, to be undergone for their pharmacokinetic property’s analyses, sitemap analyses and lignad-receptor interactions by computational models through SwissADME and Schrödinger, 2018 softwares against PDB 6COX, 6D6T, 1JFF receptors. MESS was found to display statistically significant (P < 0.05) inhibition of Bovine Serum albumin and Egg albumin denaturation compared to reference drug diclofenac sodium. Remarkable vermicidal effect on the paralysis and death of anthelmintic parasites was observed at MESS concentration 200 mg/dL. A nondescript clot lysis of MESS compared to streptokinase was evident in in vitro thrombolytic assay. MESS increased the number of times the animal crossed from one compartment to the other and the time spent in the brightly-lit chamber of the LDB. Three-methylchalcone derivatives out of seven MESS compounds were undertaken, based on cut off value and sitemap prediction score, for further ligand-receptor binding efficiency. All these three compounds showed promising docking score, glide emodel and glide energy against PDB 6COX, 6D6T and 1DDJ, plasmin proteins demonstrating the prospects of MESS to be materialized for anti-inflammatory, anthelmintic, and thrombolytic therapeutics with further clarification.

2019 ◽  
Vol 19 (2) ◽  
pp. 30-34
Author(s):  
Vanlalhruaii ◽  
C. Malsawmtluangi ◽  
H. Lalhlenmawia

The methanolic extract of C. affinis was evaluated for its in-vitro anti-inflammatory activity by bovine serum albumin denaturation method, egg albumin denaturation method and protease inhibition method at different concentrations. Diclofenac sodium was used as the reference drug. The extract exhibits anti-inflammatory activity in a concentration-dependent manner. In bovine serum albumin denaturation method, the extract at concentrations of 100, 200, 400, 600, 800, 1000 µg/ml showed 25.49, 28.43, 31.37, 37.25, 41.17, 48.03% inhibition respectively. In egg albumin denaturation method, the concentrations of 50, 100, 200, 300, 400, 500 µg/ml showed 5.3, 9.89, 28.12, 32.8, 43.2, 52.8% inhibition respectively. In protease inhibition method the extract at concentration of 100, 200, 300, 400, 500 µg/ml showed 8.87, 19.32, 28.56, 43.96, 59.92% inhibition respectively. Therefore, from the results it can be concluded that the methanolic extract of C. affinis possesses anti-inflammatory activity.


2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Steve V. Djova ◽  
Maximilienne A. Nyegue ◽  
Angelique N. Messi ◽  
Alian D. Afagnigni ◽  
François-X. Etoa

Ochna schweinfurthiana has been used in traditional medicine to treat pain, inflammation, and arthritis. It is a rich source of complex dimers of flavonoids with potential use as templates for the development of therapeutic drugs. Hence, the aim of this study was to study the phytochemical content and evaluate the in vitro cytotoxic, genotoxic, and anti-inflammatory activities of the aqueous extract of Ochna schweinfurthiana bark (OSE). Phytochemical study was carried out according to LC-MS procedures, while isolation was carried out using thin layer and column chromatographies. Cytotoxicity was investigated by the mitochondrial viability [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) method while genotoxicity potential of the extract was ascertained using the Salmonella typhimurium test strains TA98 and TA100. The anti-inflammatory effect of OSE was evaluated by the in vitro inhibition of 15-lipooxygenase enzyme and bovine serum albumin denaturation (BSA) assays. The investigation of compounds extracted from OSE led to the identification and isolation of six known compounds, namely, hemerocallone (9), 6,7-dimethoxy-3’-4’-dimethoxyisoflavone (10), lithospermoside (13), amentoflavone (14), agathisflavone (15), and β-D-fructofuranosyl-α-D-glucopyranoside (17). In the anti-inflammatory assay, aqueous extracts of the bark showed selective inhibition of 15-lipooxygenase with IC50 value of 32.2±0.36  μg/mL and the result of the bovine serum albumin denaturation assay with IC50 value of 130± 5.78 μg/mL showed moderate activity. The toxicity assay indicated that OSE are noncytotoxic on Vero cell line with LC50 value of 50 mg/mL and nongenotoxic toward Salmonella typhimurium tester strain TA98 and TA100. Result from this study supports the traditional use of the selected medicinal plants in Cameroon for the treatment of inflammatory conditions. Noncytotoxicity and nongenotoxicity of OSE suggest that this plant is safe for use.


Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3435 ◽  
Author(s):  
Andreea-Iulia Pricopie ◽  
Ioana Ionuț ◽  
Gabriel Marc ◽  
Anca-Maria Arseniu ◽  
Laurian Vlase ◽  
...  

In the context of there being a limited number of clinically approved drugs for the treatment of Candida sp.-based infections, along with the rapid development of resistance to the existing antifungals, two novel series of 4-phenyl-1,3-thiazole and 2-hydrazinyl-4-phenyl-1,3-thiazole derivatives were synthesized and tested in vitro for their anti-Candida potential. Two compounds (7a and 7e) showed promising inhibitory activity against the pathogenic C. albicans strain, exhibiting substantially lower MIC values (7.81 μg/mL and 3.9 μg/mL, respectively) as compared with the reference drug fluconazole (15.62 μg/mL). Their anti-Candida activity is also supported by molecular docking studies, using the fungal lanosterol C14α-demethylase as the target enzyme. The interaction of the most biologically active synthesized compound 7e with bovine serum albumin was investigated through fluorescence spectroscopy, and the obtained data suggested that this molecule might efficiently bind carrier proteins in vivo in order to reach the target site.


1969 ◽  
Vol 26 (5) ◽  
pp. 1392-1397 ◽  
Author(s):  
James E. Stewart ◽  
Diane M. Foley

The levels of fluorescent material in the hemolymph of lobsters injected with serum proteins from lobster hemolymph labelled with fluorescein remained relatively constant over a 6-day test period; the levels in lobsters injected with bovine serum albumin labelled with fluorescein declined rapidly. A precipitin-like reaction was observed when lobster hemolymph serum was titrated with bovine serum albumin in vitro.


2006 ◽  
Vol 16 (9) ◽  
pp. 2450-2453 ◽  
Author(s):  
Xiong-Jie Jiang ◽  
Jian-Dong Huang ◽  
Yu-Jiao Zhu ◽  
Fen-Xiang Tang ◽  
Dennis K.P. Ng ◽  
...  

2021 ◽  
Author(s):  
Alessandra Capezzone de Joannon ◽  
Angela Testa ◽  
Natalie Falsetto ◽  
Michela Procaccini ◽  
Lorella Ragni

Aim: Ethanol is highly effective at inactivating enveloped viruses, including SARS-CoV-2. The aim of this study is to evaluate the virucidal activity of Amuchina Gel Xgerm (74% ethanol) against SARS-CoV-2, according to the European Standard EN14476:2013+A2:2019. Materials & methods: Virucidal activity of the study product was evaluated against SARS-CoV-2 strain USAWA1/2020 in suspension, in the presence of 0.3 g/l of bovine serum albumin. Results: The log10 reduction of SARS-CoV-2 in the presence of bovine serum albumin was ≥4.11 ± 0.12 after 30 s of exposure to the study product (80% dilution). Cytotoxicity was observed in the 100 dilution, affecting the detection limit by 1 log10. Conclusion: Virucidal activity against SARS-CoV-2 supports the effectiveness of this alcohol-based formulation as a prevention measure for COVID-19 illness.


2008 ◽  
Vol 2 (1) ◽  
Author(s):  
Md Ashraful Alam ◽  
Md Abdul Awal ◽  
Mahbub Mostofa ◽  
Md Kamrul Islam ◽  
Nusrat Subhan

1989 ◽  
Vol 6 (3) ◽  
pp. 164-167 ◽  
Author(s):  
Claudio A. Benadiva ◽  
Barbara Kuczynski-Brown ◽  
Tobi G. maguire ◽  
Luigi Mastroianni ◽  
George L. Flickinger

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