160 results match your criteria bio-guided fractionation


Bio-guided isolation of anti-leishmanial natural products from Diospyros gracilescens L. (Ebenaceae).

BMC Complement Med Ther 2021 Mar 31;21(1):106. Epub 2021 Mar 31.

Antimicrobial and Biocontrol Agents Unit, Laboratory for Phytobiochemistry and Medicinal Plants Studies, Department of Biochemistry, Faculty of science University of Yaounde I, P. O Box 812, Yaounde, Cameroon.

Background: Plants represent an intricate and innovative source for the discovery of novel therapeutic remedies for the management of infectious diseases. The current study aimed at discovering new inhibitors of Leishmania spp., using anti-leishmanial activity-guided investigation approach of extracts from Diospyros gracilescens Gürke (1911) (Ebenaceae), targeting the extracellular (promastigotes) and intracellular (amastigotes) forms of Leishmania donovani. Read More

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Identification of compounds responsible for the anthelmintic effects of chicory (Cichorium intybus) by molecular networking and bio-guided fractionation.

Int J Parasitol Drugs Drug Resist 2021 Feb 11;15:105-114. Epub 2021 Feb 11.

Department of Veterinary and Animal Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Frederiksberg, Denmark. Electronic address:

Increasing resistance towards anthelmintic drugs has necessitated the search for alternative treatments for the control of gastrointestinal nematode parasites. Animals fed on chicory (Cichorium intybus L.), a temperate (pasture) crop, have reduced parasite burdens, hence making C. Read More

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February 2021

Isoquinolinequinone Derivatives from a Marine Sponge ( sp.) Regulate Inflammation in In Vitro System of Intestine.

Mar Drugs 2021 Feb 4;19(2). Epub 2021 Feb 4.

Department of Agronomy and Medicinal Plant Resources, Gyeongnam National University of Science and Technology, Jinju 52725, Korea.

Using bio-guided fractionation and based on the inhibitory activities of nitric oxide (NO) and prostaglandin E2 (PGE2), eight isoquinolinequinone derivatives (-) were isolated from the marine sponge sp. Among these, methyl -demethylrenierate () is a noble ester, whereas compounds and are new -demethyl derivatives of known isoquinolinequinones. Compound was assigned as a new 21-dehydroxyrenieramycin F. Read More

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February 2021

Bio-guided isolation of leishmanicidal and trypanocidal constituents from Pituranthos battandieri aerial parts.

Parasitol Int 2021 Jun 2;82:102300. Epub 2021 Feb 2.

Instituto Universitario de Bio-Orgánica Antonio González, Departamento de Química Orgánica, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Canary Islands, Spain. Electronic address:

Protozoan pathogens that cause neglected tropical diseases are a major public health concern in tropical and developing countries. In the course of our ongoing search for new lead compounds as potential antiprotozoal agents, this study aims to perform a bio-guided fractionation of Pituranthos battandieri, using an in vitro assay against Leishmania amazonensis and Trypanosoma cruzi. Two known polyacetylenes, (-)-panaxydiol (1) and (-)-falcarindiol (2) were identified from the ethanolic extract of the aerial parts of P. Read More

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Ajuga iva water extract antihypertensive effect on stroke-prone spontaneously hypertensive rats, vasorelaxant effects ex vivo and in vitro activity of fractions.

J Ethnopharmacol 2021 Apr 11;270:113791. Epub 2021 Jan 11.

Louvain Drug Research Institute, Pharmacognosy Research Group, Université catholique de Louvain, UCLouvain, Brussels, Belgium. Electronic address:

Ethnopharmacological Relevance: Ajuga iva (L.) Schreb. (Labiatae) (AI) is used in folk medicine for a variety of ailments, including diabetes mellitus and hypertension. Read More

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Synthetic Lethal Activity of Benzophenanthridine Alkaloids From Against BRCA1-Deficient Cancer Cells.

Front Pharmacol 2020 3;11:593845. Epub 2020 Dec 3.

Centro de Investigaciones en Bioquímica Clínica e Inmunología, CIBICI-CONICET, Córdoba, Argentina.

Several plants from South America show strong antitumoral properties based on anti-proliferative and/or pro-apoptotic activities. In this work we aimed to identify selective cytotoxic compounds that target BRCA1-deficient cancer cells by Synthetic Lethality (SL) induction. Using a high-throughput screening technology developed in our laboratory, we analyzed a collection of extracts from 46 native plant species from Argentina using a wide dose-response scheme. Read More

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December 2020

Identification of Chemopreventive Components from Halophytes Belonging to Aizoaceae and Cactaceae Through LC/MS-Bioassay Guided Approach.

J Chromatogr Sci 2020 Dec 23. Epub 2020 Dec 23.

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Kasr El Aini Street, 11562 Cairo, Egypt.

Six halophytes, namely, Aptenia cordifolia var. variegata, Glottiphyllum linguiforme, Carpobrotus edulis, Ferocactus glaucescens, F. pottsii and F. Read More

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December 2020

Hydroalcoholic extract of Tagetes minuta L. inhibits inflammatory bowel disease through the activity of pheophytins on the NF-κB signalling pathway.

J Ethnopharmacol 2021 Mar 23;268:113603. Epub 2020 Nov 23.

Department of Organic Chemistry, Faculty of Sciences, University Autónoma of Madrid. Cantoblanco, 28049, Madrid, Spain.

Ethno-pharmacological Relevance: Species of the genus Tagetes are well known for their anti-inflammatory properties. Tagetes minuta "Huacatay" is an endemic species of South America that has been used in traditional medicine since ancient times as a remedy for stomach and intestinal discomfort.

Aim Of The Study: The aim of this study is to investigate the anti-inflammatory activity of the aqueous and hydroalcoholic extracts of the Huacatay, identifying the compounds responsible for this activity. Read More

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The Inhibition of NLRP3 Inflammasome and IL-6 Production by Derived Constituents Provides a Link to Its Anti-Inflammatory Therapeutic Potentials.

Molecules 2020 Oct 14;25(20). Epub 2020 Oct 14.

Department of Molecular Biology, Institute for Molecular Biology and Medicine, Université Libre de Bruxelles, 6041 Gosselies, Belgium.

The activation of NOD-, LRR-, and pyrin domain-containing protein 3 (NLRP3) inflammasome and/or its components is associated with the physio-pathogenesis of many respiratory diseases including asthma, COPD (chronic obstructive pulmonary disease), SARS Cov-2 (severe acute respiratory syndrome coronavirus 2), and in several autoimmune diseases. . has been widely reported to be traditionally used in the treatment of different ailments, some of which are of inflammatory background such as asthma, wounds, headache, etc. Read More

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October 2020

Identification of a Proanthocyanidin from Sonn. Root with Anti-Tyrosinase and Antioxidant Activity.

Biomolecules 2020 09 21;10(9). Epub 2020 Sep 21.

Laboratory of Chemistry of Natural Molecules, Gembloux Agro-Bio Tech, University of Liège, 4000 Liège, Belgium.

This work follows an ethnobotanical study that took place in the island of Mayotte (France), which pointed out the potential properties of Sonn. roots when used to enhance skin health and appearance. Through in vitro testing of a crude methanolic extract, high anti-tyrosinase (skin whitening effect) and antioxidant activities (skin soothing effect) could be measured. Read More

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September 2020

Bio-Guided Fractionation Driven by In Vitro α-Amylase Inhibition Assays of Essential Oils Bearing Specialized Metabolites with Potential Hypoglycemic Activity.

Plants (Basel) 2020 Sep 21;9(9). Epub 2020 Sep 21.

Department of Drug Science and Technology, University of Turin, Via Pietro Giuria 9, 10125 Turin, Italy.

Type 2 diabetes mellitus (T2DM) is a metabolic disorder characterized by unpaired blood glycaemia maintenance. T2DM can be treated by inhibiting carbohydrate hydrolyzing enzymes (α-amylases and α-glucosidases) to decrease postprandial hyperglycemia. Acarbose and voglibose are inhibitors used in clinical practice. Read More

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September 2020

Assessment of in vitro anthelmintic activity and bio-guided chemical analysis of BRS Boyrá pineapple leaf extracts.

Vet Parasitol 2020 Sep 20;285:109219. Epub 2020 Aug 20.

Universidade Estadual de Feira de Santana, Av. Transnordestina, s/n, Novo Horizonte, Feira de Santana, 44036-900, Bahia, Brazil. Electronic address:

Species of the Bromeliaceae are known for their pharmacological actions, including anthelmintic effects. The aim of this study was to investigate the in vitro anthelmintic activity of extracts and fractions of BRS Boyrá pineapple leaf against the eggs and infective larvae of gastrointestinal nematodes (Trichostrongylidae) of goats and to identify the compounds involved in this activity. Crude methanol, hexane, dichloromethane, ethyl acetate and residual hydromethanol extracts were investigated by quantitative analysis of phenolic and flavonoid contents, antioxidant activity, anthelmintic activity against gastrointestinal nematodes of goats. Read More

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September 2020

Anti-nociceptive and anti-inflammatory effects of stem bark extract of Ficus capensis Thunb (Moraceae) by bioactivity fractionation.

Antiinflamm Antiallergy Agents Med Chem 2020 Aug 25. Epub 2020 Aug 25.

Department of Microbiology and Parasitology, Ladoke Akintola University of Technology Ogbomoso. Nigeria.

Objective: This study investigated the anti-nociceptive and anti-inflammatory activities of the aqueous extract of Ficus capensis (AEFC) by bio-guided fractionation.

Methods: The anti-nociceptive and anti-inflammatory effects of AEFC (250, 500, 1000 mg/kg, i.p) were assessed using acetic acid-induced writhing, hot plate, tail-flick, formalin tests, and carrageenan-induced paw oedema respectively. Read More

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Toad Venom Antiproliferative Activities on Metastatic Melanoma: Bio-Guided Fractionation and Screening of the Compounds of Two Different Venoms.

Biology (Basel) 2020 Aug 10;9(8). Epub 2020 Aug 10.

Laboratory of Human Anatomy and Experimental Oncology, Faculty of Medicine and Pharmacy, University of Mons, 7000 Mons, Belgium.

Melanoma is the most common cancer in young adults, with a constantly increasing incidence. Metastatic melanoma is a very aggressive cancer with a 5-year survival rate of about 22-25%. This is, in most cases, due to a lack of therapies which are effective on the long term. Read More

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Daphnanes diterpenes from the latex of Hura crepitans L. And activity against human colorectal cancer cells Caco-2.

Bioorg Chem 2020 10 23;103:104132. Epub 2020 Jul 23.

UMR 152 PharmaDev, Université de Toulouse, IRD, UPS, France.

Hura crepitans (Euphorbiaceae) is a tree from South America that produces an irritant latex used as a fish poison. A bio-guided fractionation of an ethanolic extract of the latex led to the isolation and structural identification of three known daphnane-type diterpenes (1-3) including huratoxin (1), together with two new analogs (4, 5). Compound 1 was found to exhibit significant and selective cell growth inhibition against the colorectal cancer cell line Caco-2, with morphological modifications suggesting formations mimicking the intestinal crypt architecture. Read More

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October 2020

In vivo and in vitro evaluation of the osteogenic potential of Davallia mariesii T. Moore ex Baker.

J Ethnopharmacol 2021 Jan 5;264:113126. Epub 2020 Aug 5.

Clinical Drug Development of Herbal Medicine, College of Pharmacy, Taipei Medical University, 250 Wuxing Street, Taipei, 11031, Taiwan; Graduate Institute of Pharmacognosy, College of Pharmacy, Taipei Medical University, 250 Wuxing Street, Taipei, 11031, Taiwan; Center for Reproductive Medicine & Sciences, Taipei Medical University Hospital, 252 Wuxing Street, Taipei, 11031, Taiwan. Electronic address:

Ethnopharmacological Relevance: Postmenopausal osteoporosis is a major bone health issue worldwide. There is an unmet medical need for osteoporosis treatments, a disease which disproportionately impacts women. Exploring botanicals to prevent or treat osteoporosis is currently an interest of investigations. Read More

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January 2021

Ethanolic extract of Artemisia campestris subsp. glutinosa (Besser) Batt. inhibits HIV-1 replication in vitro through the activity of terpenes and flavonoids on viral entry and NF-κB pathway.

J Ethnopharmacol 2020 Dec 3;263:113163. Epub 2020 Aug 3.

Department of Pharmacology, Pharmacognosy and Botany, Faculty of Pharmacy, Universidad Complutense de Madrid, Plza. Ramón y Cajal S/n, 28040, Madrid, Spain; AIDS Immunopathology Department, National Centre of Microbiology, Instituto de Salud Carlos III, Ctra. Pozuelo Km. 2, 28224, Madrid, Spain. Electronic address:

Ethno-pharmacological Relevance: The genus Artemisia spp. is well known for its anti-infectious properties and its high content in anti-infectious compounds, like the well-known sweet wormwood (Artemisia annua L.). Read More

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December 2020

Sesquiterpenoids and flavonoids from Inula viscosa induce programmed cell death in kinetoplastids.

Biomed Pharmacother 2020 Oct 13;130:110518. Epub 2020 Jul 13.

Instituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Universidad de La Laguna, Avda. Astrofísico Fco. Sánchez, S/N, La Laguna, Tenerife, Islas Canarias 38203, Spain; Red de Investigación Colaborativa en Enfermedades Tropicales (RICET); Departamento de Obstetricia, Ginecología, Pediatría, Medicina Preventiva y Salud Pública, Toxicología, Medicina Legal y Forense y Parasitología, Universidad De La Laguna, La Laguna, Tenerife, Islas Canarias 38203, Spain.

Neglected tropical diseases such as leishmaniasis and American trypanosomiasis represent an increasing health problem. Current treatments are not satisfactory which remains an urgent need for novel, cheap and safe chemotherapies. In the course of our ongoing search for new potential anti-protozoal agents, this study aimed to perform a bio-guided fractionation of Inula viscosa (Asteraceae) using in vitro assays against three strains of Leishmania and Trypanosma genus. Read More

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October 2020

Bioassay Guided Isolation and Docking Studies of a Potential β-Lactamase Inhibitor from .

Molecules 2020 May 31;25(11). Epub 2020 May 31.

Department of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.

Infectious diseases are the second major cause of death worldwide, and the ability to resist multiple classes of antibiotics is the key factor in enabling pathogenic organisms to survive and spread in the nosocomial environment. Unfortunately, the available β-lactamase inhibitors are not efficient against β-lactamase B, C, and D which necessitates discovering either broad spectrum β-lactamase inhibitors or new β-lactam antibiotics resistant to bacterial enzymes. In this regard, products of natural origin have prompted the disclosure of new compounds and medicinal leads. Read More

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Niosomes of active phytochemicals: antidiabetic, antineuropathic, anti-inflammatory, and possible mechanisms of action.

Chin Med 2020 1;15:40. Epub 2020 May 1.

2Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, Alexandria, Egypt.

Background: ( FO) has been used in many inflammatory and painful-ailments. The main aim of this work is to perform an in-depth bio-guided phytochemical investigation of by identifying its main-active ingredients. Optimizing pharmacokinetics via niosomal-preparation will also be done to enhance their in vivo antineuropathic and anti-inflammatory potentials, and to explore their possible-mechanism of actions. Read More

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In Vitro Antifungal Activity of (Spreng.) Taub. extracts against .

Plants (Basel) 2020 Apr 2;9(4). Epub 2020 Apr 2.

Instituto de Patobiología Veterinaria, (IPvet), CICVyA, Instituto Nacional de Tecnología Agropecuaria, Hurlingham 1686, Prov. de Buenos Aires, Argentina.

is a filamentous, saprophytic fungus, whose colonization occurs mainly in cereal grains and oilseeds once harvested. Under certain conditions, it could produce mycotoxins called aflatoxins, known as powerful human liver carcinogens. The aim of the present study was to describe the antifungal activity of extracts of , a species from northern Argentina (Oriental Chaco), against . Read More

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Antioxidant and a-amylase Inhibitory Activities and Phytocompounds of Fruits.

Medicines (Basel) 2020 Feb 28;7(3). Epub 2020 Feb 28.

Department of Development Technology, Graduate School for International Development and Cooperation, Hiroshima University, Hiroshima 739-8529, Japan.

fruit is commonly used for food ingredients and traditional medicines in tropical countries, however, information about its biological activities and chemical profiles has been inadequately reported. In this study, a bio-guided fractionation of antioxidants and α-amylase inhibitors from hexane (MH) and ethyl acetate (ME) extracts of fruit (pericarp and seed) was carried out. Eleven fractions from MH (D1-D11) and 17 fractions from ME (T1-T17) were obtained from column chromatography over silica gel, which were then examined for anti-radical capacity by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays, and pancreatic α-amylase inhibition, a key enzyme linked to type 2 diabetes. Read More

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February 2020

Antimalarial alkaloid from Hypoestes forskaolii.

Exp Parasitol 2020 Feb 6;211:107851. Epub 2020 Feb 6.

Kitasato Institute for Life Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan; Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.

Following on from previous studies, we brought further our quest for anti-malarial agents isolated from plants grown in the Saudi Arabian Peninsula. Methanolic extracts were prepared from eighteen Saudi plants and then tested in vitro to assess their anti-malarial effects on Plasmodium falciparum K1, (a chloroquine-resistant strain) as well as their cytotoxicity on MRC5 (human diploid embryonic lung cell line) cells. Moderate anti-malarial activity was observed in extracts prepared from Hypoestes forskaolii (Vahl) R. Read More

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February 2020

Tracheal relaxation through calcium channel blockade of Achillea millefolium hexanic extract and its main bioactive compounds.

J Ethnopharmacol 2020 May 5;253:112643. Epub 2020 Feb 5.

Unidad de Biomedicina, Facultad de Estudios Superiores Iztacala, Universidad Nacional Autónoma de México, Tlalnepantla, Estado de México, 54090, Mexico.

Ethnopharmacological Importance: Achillea millefolium L. (Asteraceae) is used for the treatment of respiratory diseases, diabetes, and hypertension.

Aim: to explore its tracheal relaxant properties and clarify its functional mechanism of action on smooth muscle cells, which allow us to propose it as a potential anti-asthmatic drug. Read More

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In-depth hepatoprotective mechanistic study of Phyllanthus niruri: In vitro and in vivo studies and its chemical characterization.

PLoS One 2020 15;15(1):e0226185. Epub 2020 Jan 15.

Pharmacognosy Department, Faculty of Pharmacy, Cairo University, Kasr El-Ainy Street, Cairo, Egypt.

Phyllanthus niruri L. is a widespread tropical plant which is used in Ayurvedic system for liver and kidney ailments. The present study aims at specifying the most active hepatoprotective extract of P. Read More

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Bio-Guided Isolation of Prospective Bioactive Constituents from Roots of (Dalzell) Oliv.

Molecules 2019 Dec 4;24(24). Epub 2019 Dec 4.

Faculty of Biotechnology, Nguyen Tat Thanh University, 298A-300A Nguyen Tat Thanh Street, Ward 13, District 4, Ho Chi Minh City 72820, Vietnam.

fruits are routinely used for the culinary purpose as natural spices, whereas leaves and roots are folk medicine with various health benefits in southern China, South and Southeast Asia. In this study, the bioassay-guided fractionation by column chromatography yielded three pure compounds including dentatin, nordentatin, and clausine K and five active fractions () from roots. These known anticancer compounds were confirmed by X-ray diffraction, H-, C-nuclear magnetic resonance (NMR), and electrospray ionization tandem mass spectrometric (ESI-MS-MS) analyses. Read More

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December 2019

Bio-Guided Fractionation of Prenylated Benzaldehyde Derivatives as Potent Antimicrobial and Antibiofilm from L. Fruits-Associated .

Molecules 2019 Nov 14;24(22). Epub 2019 Nov 14.

Pharmacognosy and Medicinal Plants Department, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt, Cairo 11835, Egypt.

L.; Family Apiaceae; is a plant indigenous to Egypt. Its fruits contain bioactive compounds such as furanocoumarins and flavonoids of important biological activities. Read More

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November 2019

Bio-Guided Fractionation of Ethanol Extract of Leaves of Kunt (Rutaceae) Led to the Isolation of Two Cytotoxic Quinoline Alkaloids: Evidence of Selectivity Against Leukemia Cells.

Biomolecules 2019 10 8;9(10). Epub 2019 Oct 8.

Bioorganic Chemistry Laboratory, Facultad de Ciencias Básicas y Aplicadas, Universidad Militar Nueva Granada, Cajicá 250247, Colombia.

Bio-guided fractionation performed on the leaves-derived ethanol extract of (Rutaceae), a plant used in traditional medicine, led to the isolation of two alkaloids, kokusaginine and flindersiamine , as main cytotoxic agents. Primary ethanolic extract and raw fractions exhibited cell inhibition against five cancer cell lines at different levels (25-97% inhibition at 50 µg/mL) as well as isolated alkaloids - (30-90% inhibition at 20 µM). Although alkaloid generally was the most active compound, both alkaloids showed a selective effect on K562, a human chronic myelogenous leukemia cell line. Read More

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October 2019

Anthelmintic-like activity of polyphenolic compounds and their interactions against the cattle nematode Cooperia punctata.

Vet Parasitol 2019 Oct 18;274:108909. Epub 2019 Sep 18.

Centro de Enseñanza Investigación y Extensión en Ganadería Tropical, Facultad de Medicina Veterinaria y Zootecnia, Universidad Nacional Autónoma de México, Km 5.5 Carretera Federal Tlapacoyan-Martínez de la Torre, C.P. 93600, Veracruz, Mexico. Electronic address:

Polyphenolic compounds (PCs) have been proposed as one of the most bioactive group of secondary metabolites occurring in nature and have been associated to anthelmintic (AH)-like activity of plants against cattle nematodes. However, little is known regarding their synergetic / antagonistic interactions. This study assessed the in vitro AH-like activity of commercial PCs: quercetin, caffeic acid, rutin and coumarin, and their combinations against the egg hatching and larval exsheathment of Cooperia punctata; one of the most prevalent nematodes affecting grazing cattle in tropical regions. Read More

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October 2019

Bioactivity-based analysis and chemical characterization of hypoglycemic and antioxidant components from Artemisia argyi.

Bioorg Chem 2019 11 12;92:103268. Epub 2019 Sep 12.

School of Traditional Chinese Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China. Electronic address:

Diabetes is one of the metabolic disorders in the world. It is the prime reason of mortality and morbidity owing to hyperglycemia which is link with numerus obstacles. Artemisia argyi is commonly used as an ingredient in healthy foods as well as an herbal medicine in Asian countries. Read More

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November 2019