scholarly journals Lipase Assisted (S)-Ketoprofen Resolution from Commercially Available Racemic Mixture

2021 ◽  
Vol 14 (10) ◽  
pp. 996
Author(s):  
Daniela Estrada-Valenzuela ◽  
Víctor H. Ramos-Sánchez ◽  
Gerardo Zaragoza-Galán ◽  
Jose C. Espinoza-Hicks ◽  
Alejandro Bugarin ◽  
...  
Keyword(s):  
Candida Rugosa ◽  
Enantiomeric Excess ◽  
Candida Rugosa Lipase ◽  
Liquid Extraction ◽  
Racemic Mixture ◽  
Liquid Liquid Extraction ◽  
The Family ◽  
Inflammatory Drugs ◽  
Gastrointestinal Ulceration

Ketoprofen is a commercially available drug sold as a racemic mixture that belongs to the family of non-steroidal anti-inflammatory drugs known as profens. It has been demonstrated (in vitro) that (S)-ketoprofen is around 160 times more potent than its enantiomer (R)-ketoprofen, while accumulation of (R)-ketoprofen can cause serious side effects, such as dyspepsia, gastrointestinal ulceration/bleeding, pain, salt and fluid retention, and hypertension. In this work, four commercially available lipases were systematically assessed. Parameters such as conversion, enantiomeric excess, and enantioselectivity were considered. Among them, and by evaluating lipase load, temperature, solvent, and alcohol, Candida rugosa lipase exhibited the best results in terms of enantioselectivity E = 185 ((S)-enantiopreference) with esterification conversions of c = 47% (out of 50%) and enantiomeric excess of 99%. The unreacted (R)-enantiomer was recovered by liquid-liquid extraction and racemized under basic media, which was recycled as starting material. Finally, the (S)-alkyl ketoprofen ester was successfully enzymatically hydrolyzed to the desired (S)-ketoprofen with c = 98.5% and 99% ee. This work demonstrated the benefit and efficiency of using Candida rugosa lipase to kinetically resolve racemic ketoprofen by an environmentally friendly protocol and with the recycling of the undesired (R)-ketoprofen.

scholarly journals IN VITRO ANTIOXIDANT AND ANTIBACTERIAL POTENTIAL OF MEDICINAL PLANT CERASTIUM FONTANUM

2021 ◽  
Vol 51 (3) ◽  
pp. 145-151
Author(s):  
Himayat Ullah ◽  
Muhammad Mustafa ◽  
Muhammad Israr ◽  
Zahid Ali ◽  
M. Nouman ◽  
...  
Keyword(s):  
Medicinal Plant ◽  
Liquid Extraction ◽  
New Drugs ◽  
Diffusion Method ◽  
Aqueous Fraction ◽  
Gram Negative ◽  
Liquid Liquid Extraction ◽  
Antibacterial Potential ◽  
Agar Well Diffusion Method

Naturally God gifted medicinal plants which contain more potentially active compounds their characterization and isolation are very important and can provide us a great help in making new drugs to cure many diseases. Our current attempt was made to obtain the ethanolic extracts of medicinal plant Cerastium fontanum using a hot continuous soxhlet process and also via maceration method. The concentrated dried fraction extracts of Cerastium fontanum such as aqueous, n-hexane, ethyl acetate and dichloromethane were achieved using liquid-liquid extraction which were then evaluated for in vitro antioxidants potential using DPPH (1,1-diphenyl-2-picryl-hydrazyl) assay and also agar-well diffusion method were used for antimicrobial potential. In vitro antioxidants inhibition potential were measured through spectrophotometer at various concentration (500 to 62.5µg/mL) prepared in standard solvent. Among all extracts aqueous fraction showed IC50 = 2.9 ± 0.05mg/mL maximum potency towards stable DPPH much closer to standard control acarbose IC50 = 2.61 ± 0.01mg/mL. The antibacterial activity results indicated that all fractions found active against both strains (gram positive and gram negative) of bacteria. In various extracts only the aqueous fraction extracts showed excellent inhibition potential against Staphylococcus aureus and Escherichia Coli. While dichloromethane fraction extracts were found active only with gram negative strain. Thus the Cerastium fontanum extracts possess much higher inhibition potential then standard available antibiotics in the market.

scholarly journals Mangiferin Rich Products from Aphloia theiformis (Vahl) Benn Leaves: Extraction, Fractionation, Phytochemical Characterization, and Antioxidant Properties

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2081
Author(s):  
Dovilė Grauzdytė ◽  
Audrius Pukalskas ◽  
Chaker El Kalamouni ◽  
Petras Rimantas Venskutonis
Keyword(s):  
Antioxidant Capacity ◽  
Antioxidant Properties ◽  
Natural Antioxidants ◽  
Liquid Extraction ◽  
In Vitro Assays ◽  
Synthetic Antioxidant ◽  
Liquid Liquid Extraction ◽  
Extraction Solvents ◽  
First Time

Aphloia theiformis is traditionally used in Mauritius, Madagascar, and Reunion Island for treating several diseases. In this study, various extraction solvents and schemes were applied for the recovery of antioxidant rich fractions from the leaves of A. theiformis. The products were evaluated for their antioxidant capacity using well known in vitro assays. Major compounds were characterized by UPLC–QTOF–MS. Hydrophilic extracts of A. theiformis demonstrated strong antioxidant properties, which are comparable with the synthetic antioxidant Trolox. UPLC analysis confirmed mangiferin as the main secondary metabolite of A. theiformis. Tormentic and hydroxytormentic acids as well as their isomers were also abundant in A. theiformis extracts and fractions, while their amounts were determined for the first time. The most potential extract was further separated into the fractions by liquid-liquid extraction and by precipitation at low temperature. Antioxidant capacity and composition of secondary metabolites of derived fractions were determined. Some of the fractions possessed remarkable antioxidant capacity, comparable to pure mangiferin. The results obtained reveal high potential of A. theiformis for recovery of natural antioxidants and other bioactive phytochemicals, particularly mangiferin.

scholarly journals In Vitro Antibacterial Activity of Hibiscus sabdariffa L. Phenolic Extract and Its In Situ Application on Shelf-Life of Beef Meat

Foods ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 1080
Author(s):  
Ana Selene Márquez-Rodríguez ◽  
Susana Nevárez-Baca ◽  
Julio César Lerma-Hernández ◽  
León Raul Hernández-Ochoa ◽  
Guadalupe Virginia Nevárez-Moorillon ◽  
...  
Keyword(s):  
Shelf Life ◽  
Solid Phase ◽  
Ethanolic Extract ◽  
Liquid Extraction ◽  
Natural Food ◽  
Hibiscus Sabdariffa ◽  
Liquid Liquid Extraction ◽  
Phenolic Extract

Compounds from spices and herbs extracts are being explored as natural antibacterial additives. A plant extract used in traditional folk medicine is Hibiscus sabdariffa L., also known as Roselle. Therefore, the potential use of a phenolic hibiscus extract as antibacterial or natural food preservative was analyzed in vitro and in situ. A phenolic extract was obtained from hibiscus calyces and fractionated, and then the fractions were tested against foodborne pathogen bacteria. Liquid–liquid extraction and solid-phase extraction were used to fractionate the hibiscus extract, and HPLC was employed to analyze the fractions’ phenolic composition. Minimum bactericidal concentration (MBC) and minimal inhibitory concentration (MIC) were calculated for brute hibiscus phenolic extract, each of the fractions and pure commercial phenolic compounds. Bacteria tested were Escherichia coli, Salmonella enterica serovar Typhimurium, Staphylococcus aureus, Listeria monocytogenes and Bacillus cereus. The fraction obtained after liquid–liquid extraction presented the best performance of MBC and MIC against the bacteria tested. Furthermore, a hibiscus ethanolic extract was employed as a natural preservative to extend the shelf-life of beef. Microbiological, color and sensory analyses were performed to the meat during the shelf-life test. The application of the phenolic hibiscus extract also showed an increase of the duration of the meat`s shelf life.

Harmaline and hispidin from Peganum harmala and Inonotus hispidus with binding affinity to Candida rugosa lipase: In silico and in vitro studies

2015 ◽  
Vol 62 ◽  
pp. 1-7 ◽  
Author(s):  
Khedidja Benarous ◽  
Isabelle Bombarda ◽  
Isabel Iriepa ◽  
Ignacio Moraleda ◽  
Herbette Gaetan ◽  
...  
Keyword(s):  
Binding Affinity ◽  
In Silico ◽  
Candida Rugosa ◽  
Candida Rugosa Lipase ◽  
In Vitro Studies ◽  
Peganum Harmala

Direct-Contact (Membraneless) Hemoperfusion through Oils

1972 ◽  
Vol 18 (6) ◽  
pp. 554-562 ◽  
Author(s):  
M A Evenson ◽  
D de Vos
Keyword(s):  
Rhesus Monkeys ◽  
Direct Contact ◽  
Total Bilirubin ◽  
Feasibility Studies ◽  
Liquid Extraction ◽  
In Vivo Experiments ◽  
Liquid Liquid Extraction ◽  
Cellular Components

Abstract Oil-hemoperfusion is a highly promising procedure, as indicated by in vitro feasibility studies with human blood and in vivo experiments with rhesus monkeys. Direct liquid—liquid extraction is used to remove toxic or unwanted substances from whole blood. By choosing the proper oil or modification of an oleaginous liquid, cholesterol, total bilirubin, and lipid-soluble drugs such as glutethimide can be selectively removed or adjusted to the desired concentration with a single liquid—liquid extraction. Damage or loss of cellular components such as erythrocytes, leukocytes, and platelets is immeasurably small or nonexistent. Undesirable extraction of other vital biological substances and (or) back extraction of substances from the oil into the blood is so small that side effects or aftereffects of in vivo oil-hemoperfusion studies were considerably less than anticipated.

scholarly journals Extraction of cadmium from phosphoric acid by a synthesized extracting agent

2020 ◽  
Vol 150 ◽  
pp. 02007
Author(s):  
Kaoutar Berkalou ◽  
Abderrahman Nounah ◽  
Mohamed Khamar ◽  
Ratiba Boussen ◽  
Essediya Cherkaoui
Keyword(s):  
Nuclear Magnetic Resonance ◽  
Infrared Spectroscopy ◽  
Magnetic Resonance ◽  
Phosphoric Acid ◽  
Mass Spectroscopy ◽  
Spectroscopic Characterization ◽  
Liquid Extraction ◽  
Liquid Liquid Extraction ◽  
Physico Chemical ◽  
The Family

The Purification of phosphoric acid used several extractants from the family of oxygenates, sulfurous or amino compounds. In this work, we were interested in the synthesis, physico-chemical and spectroscopic characterization, and use of the product C11H18N2O as an extractant of cadmium from phosphoric acid. The synthesized product was characterized by: infrared spectroscopy, nuclear magnetic resonance, and mass spectroscopy. Solubility tests in different solvents have been carried out. Subsequently, liquid-liquid extraction of cadmium from phosphoric acid was carried out using C11H18N2O as an extractant diluted in benzene. The study investigated the influence of concentration of phosphoric acid and the extracting agent. The result obtained ensure that our synthesized product is promising. The percentage of cadmium extraction from phosphoric acid reached 98.58% at a concentration of 2.5M phosphoric acid and an optimal concentration of 0.5×10-2 M of synthesized extractant.

scholarly journals Simultaneous Determination of Docetaxel and Celecoxib in Porous Microparticles and Rat Plasma by Liquid-Liquid Extraction and HPLC with UV Detection: in vitro and in vivo Validation and Application

2020 ◽  
Vol 23 ◽  
pp. 289-303
Author(s):  
Elham Ziaei ◽  
Jaber Emami ◽  
Moloud Kazemi ◽  
Mahboubeh Rezazadeh
Keyword(s):  
Internal Standard ◽  
Rat Plasma ◽  
Liquid Extraction ◽  
Uv Detection ◽  
Pharmacokinetic Studies ◽  
Liquid Liquid Extraction ◽  
Porous Microparticles ◽  
Limit Of Quantitation

Purpose: A simple, rapid, sensitive, and reliable HPLC method with UV detection was developed and validated for simultaneous quantitation of docetaxel and celecoxib and paclitaxel for dissolution characterization and pharmacokinetic studies. Methods: The HPLC assay was performed isocratically on a reversed-phase C18 μ-Bondapack column using a mobile phase of acetonitrile:water (45:55, v/v) at a flow rate of 1.2 mL/min, and the analytes were detected at 230 nm. Paclitaxel was used as an internal standard for analysis of plasma samples following simple liquid-liquid extraction with n-hexane:isoamyl alcohol (97:3). The method was validated for specificity, linearity, sensitivity, precision, accuracy, robustness, and in vitro-in vivo application. Results: The retention times for docetaxel, paclitaxel, and celecoxib were 10.94, 12.4, and 16.81 min, respectively. The standard curves covering 0.1-1 μg/mL and 0.05-4 μg/mL were linear using dissolution medium and rat plasma, respectively. The limit of quantitation of the method was 50 ng/mL using 100 μL of rat plasma sample and injection of 50 μL of the residue. Within- and between-day precision and accuracy did not exceed 16.86% and 12.10%, respectively. This validated method was successfully used to quantify docetaxel and celecoxib simultaneously in the release study of docetaxel-celecoxib -loaded porous microparticles and pharmacokinetics studies. The methods were found to be simple, specific, precise, accurate, and reproducible. In this study, paclitaxel was used as the internal standard while dexamethasone, flutamide, and budesonide proved suitable alternative as an internal standard. Conclusion: Since docetaxel and celecoxib could be co-administered for the treatment of a wide range of cancers such as non-small cell lung carcinoma, the developed method is particularly advantageous for routine therapeutic drug monitoring and pharmacokinetic studies of these drugs.

Preparation of (S)-2-Phenylpropionic Acid by CaCl2/CMC Nanoparticles Immobilized Candida rugosa Lipase-Catalyzed Hydrolysis in Micro Aqueous Mixed Organic Solvent Systems

2020 ◽  
Vol 20 (3) ◽  
pp. 1899-1906 ◽  
Author(s):  
Xueying Liu ◽  
Dongsheng He ◽  
Xiaojuan Li ◽  
Yan Deng ◽  
Jing Deng ◽  
...  
Keyword(s):  
Organic Solvent ◽  
Candida Rugosa ◽  
Enantiomeric Excess ◽  
Candida Rugosa Lipase ◽  
Methyl Tert Butyl Ether ◽  
Isopropyl Ester ◽  
Butyl Ether ◽  
Lipase Hydrolysis ◽  
Phenylpropionic Acid ◽  
Immobilized Candida Rugosa Lipase

Candida rugosa lipase was immobilized in this study using CaCl2/CMC nanoparticles that yielded a lipase loading capacity of 127 mg/g, with better thermal stability and activity of 91.8%. The hydrolysis of racemic 2-phenylpropionic acid isopropyl ester by free and immobilized Candida rugosa lipase was investigated in the mixed organic-solvent composed of isooctane and methyl tert-butyl ether (9.5:0.5, V/V). The optimal conditions were 35 °C and pH 7.5 for free Candida rugosa lipase hydrolysis. We obtained (S)-2-phenylpropionic acid with 44.85% conversion, 95.75% enantiomeric excess and enantiomeric ratio of 112. The CaCl2/CMC nanoparticles immobilized Candida rugosa lipase possesses high enantioselectivity, with E = 237 at 40 °C and pH 7.5. It was efficiently reusable in four cycles and appropriately enhanced enantioselectivity within 120–240.

Optimisation of in vitro sample preparation for LC-MS metabolomics applications on HepaRG cell cultures

2017 ◽  
Vol 9 (24) ◽  
pp. 3704-3712 ◽  
Author(s):  
Matthias Cuykx ◽  
Olivier Mortelé ◽  
Robim M. Rodrigues ◽  
Tamara Vanhaecke ◽  
Adrian Covaci
Keyword(s):  
Sample Preparation ◽  
Cell Cultures ◽  
Liquid Extraction ◽  
Heparg Cell ◽  
Liquid Liquid Extraction

The addition of stabilizers during liquid–liquid extraction improves the precision of untargeted LC-MS metabolomics workflows.

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