In Vitro Antischistosomal Activity of the Argemone mexicana Methanolic Extract and Its Main Component Berberine

Background: Schistosomiasis has been identified as a major public health problem in tropical countries. The present study aimed to investigate the schistosomicidal effects of the methanolic extract of Argemone mexicana L. and its active component, berberine against Schistosoma mansoni on in-vitro experiments. Methods: S. mansoni adults were used. Various concentrations of the methanolic extract (10 - 200 µg/ml) and berberine (2.5 - 50 µM) were tested from 24 to 72 h. The viability of S. mansoni was confirmed with an invertoscope-microscope. Furthermore, cytotoxic (Hemolysis test), and antioxidant (DPPH radical scavenging assay) capacities were determined. Results: The viability tests on S. mansoni showed that A. mexicana at 50 μg/mL is lethal at 48 h and berberine at 10 μM is lethal at 24 h. The hemolytic activity at 1,000 μg/mL was 2.9% for A. mexicana and 90.2% for berberine. The antioxidant capacities shown by A. mexicana and berberine, were EC50 156.3 and 84.1 μg/mL, respectively. Conclusion: The extract of A. mexicana and berberine demonstrated high antischistosomal activities in low concentration and short exposure time on the in-vitro model.

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Medicinal Plants and Bioactive Compounds for Diabetes Management: Important Advances for Drug Discovery

Current Pharmaceutical Design ◽

10.2174/1381612826666200928160357 ◽

2020 ◽

Vol 26 ◽

Author(s):

Kondeti Ramudu Shanmugam ◽

Bhasha Shanmugam ◽

Gangigunta Venkatasubbaiah ◽

Sahukari Ravi ◽

Kesireddy Sathyavelu Reddy

Keyword(s):

Herbal Medicine ◽

Medicinal Plants ◽

Bioactive Compounds ◽

Diabetes Management ◽

Therapeutic Potential ◽

Public Health Problem ◽

In Vivo Studies ◽

Major Public Health Problem

Background : Diabetes is a major public health problem in the world. It affects each and every part of the human body and also leads to organ failure. Hence, great progress made in the field of herbal medicine and diabetic research. Objectives: Our review will focus on the effect of bioactive compounds of medicinal plants which are used to treat diabetes in India and other countries. Methods: Information regarding diabetes, oxidative stress, medicinal plants and bioactive compounds were collected from different search engines like Science direct, Springer, Wiley online library, Taylor and francis, Bentham Science, Pubmed and Google scholar. Data was analyzed and summarized in the review. Results and Conclusion: Anti-diabetic drugs that are in use have many side effects on vital organs like heart, liver, kidney and brain. There is an urgent need for alternative medicine to treat diabetes and their disorders. In India and other countries herbal medicine was used to treat diabetes. Many herbal plants have antidiabetic effects. The plants like ginger, phyllanthus, curcumin, aswagandha, aloe, hibiscus and curcuma showed significant anti-hyperglycemic activities in experimental models and humans. The bioactive compounds like Allicin, azadirachtin, cajanin, curcumin, querceitin, gingerol possesses anti-diabetic, antioxidant and other pharmacological properties. This review focuses on the role of bioactive compounds of medicinal plants in prevention and management of diabetes. Conclusion: Moreover, our review suggests that bioactive compounds have the potential therapeutic potential against diabetes. However, further in vitro and in vivo studies are needed to validate these findings.

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Hepatoprotective studies on methanolic extract fractions of Lindernia ciliata and development of qualitative analytical profile for the bioactive extract

Clinical Phytoscience ◽

10.1186/s40816-019-0123-1 ◽

2019 ◽

Vol 5 (1) ◽

Author(s):

Praneetha Pallerla ◽

Narsimha Reddy Yellu ◽

Ravi Kumar Bobbala

Keyword(s):

Methanolic Extract ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Liver Homogenate ◽

Reducing Power ◽

Hepatoprotective Activity ◽

Total Phenolic ◽

Effective Fraction

Abstract Background The objective of the study is to evaluate the hepatoprotective activity of methanolic extract fractions of Lindernia ciliata (LC) and development of qualitative analytical profile of the bioactive fraction using HPLC fingerprinting analysis. All the fractions of methanolic extract of Lindernia ciliata (LCME) are assessed for their total phenolic, flavonoid contents and in vitro antioxidant properties by using DPPH, superoxide, nitric oxide, hydroxyl radical scavenging activities and reducing power assay. Acute toxicity study was conducted for all the fractions and the two test doses 50 and 100 mg/kg were selected for the hepatoprotective study. Liver damage was induced in different groups of rats by administering 3 g/kg.b.w.p.o. paracetamol and the effect of fractions were tested for hepatoprotective potential by evaluating serum biochemical parameters and histology of liver of rats. The effective fraction was evaluated for its antihepatotoxic activity against D-Galactosamine (400 mg/kg b.w. i.p.) and in vivo antioxidant parameters viz., Glutathione (GSH), Melondialdehyde (MDA) and Catalase (CAT) levels are estimated using liver homogenate. Results Among all the fractions, butanone fraction of LCME, (BNF-LCME) has shown better hepatoprotective activity and hence it is selected to evaluate the antihepatotoxicity against D-GaIN. The activity of BNF-LCME is well supported in in vitro and in vivo antioxidant studies and may be attributed to flavonoidal, phenolic compounds present in the fraction. Hence, BNF-LCME was subjected to the development of qualitative analytical profile using HPLC finger printing analysis. Conclusions All the fractions of LCME exhibited significant hepatoprotective activity and BNF-LCME (50 mg/kg) was identified as the most effective fraction.

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Microwave-Assisted Synthesis of (Piperidin-1-yl)quinolin-3-yl)methylene)hydrazinecarbothioamides as Potent Inhibitors of Cholinesterases: A Biochemical and In Silico Approach

Molecules ◽

10.3390/molecules26030656 ◽

2021 ◽

Vol 26 (3) ◽

pp. 656

Author(s):

Rubina Munir ◽

Muhammad Zia-ur-Rehman ◽

Shahzad Murtaza ◽

Sumera Zaib ◽

Noman Javid ◽

...

Keyword(s):

Neurodegenerative Disorder ◽

Critical Role ◽

Public Health Problem ◽

Microwave Assisted Synthesis ◽

Major Public Health Problem ◽

Spectroscopic Techniques ◽

Dual Inhibitor ◽

Microwave Assisted ◽

Ic50 Values

Alzheimer’s disease (AD), a progressive neurodegenerative disorder, characterized by central cognitive dysfunction, memory loss, and intellectual decline poses a major public health problem affecting millions of people around the globe. Despite several clinically approved drugs and development of anti-Alzheimer’s heterocyclic structural leads, the treatment of AD requires safer hybrid therapeutics with characteristic structural and biochemical properties. In this endeavor, we herein report a microwave-assisted synthesis of a library of quinoline thiosemicarbazones endowed with a piperidine moiety, achieved via the condensation of 6/8-methyl-2-(piperidin-1-yl)quinoline-3-carbaldehydes and (un)substituted thiosemicarbazides. The target N-heterocyclic products were isolated in excellent yields. The structures of all the synthesized compounds were fully established using readily available spectroscopic techniques (FTIR, 1H- and 13C-NMR). Anti-Alzheimer potential of the synthesized heterocyclic compounds was evaluated using acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The in vitro biochemical assay results revealed several compounds as potent inhibitors of both enzymes. Among them, five compounds exhibited IC50 values less than 20 μM. N-(3-chlorophenyl)-2-((8-methyl-2-(piperidin-1-yl)quinolin-3-yl)methylene)hydrazine carbothioamide emerged as the most potent dual inhibitor of AChE and BChE with IC50 values of 9.68 and 11.59 μM, respectively. Various informative structure–activity relationship (SAR) analyses were also concluded indicating the critical role of substitution pattern on the inhibitory efficacy of the tested derivatives. In vitro results were further validated through molecular docking analysis where interactive behavior of the potent inhibitors within the active pocket of enzymes was established. Quinoline thiosemicarbazones were also tested for their cytotoxicity using MTT assay against HepG2 cells. Among the 26 novel compounds, there were five cytotoxical and 18 showed proliferative properties.

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PHYTOCHEMICAL SCREENING AND PHARMACOLOGICAL EVALUATION OF AEGLE MARMELOS FRUIT

INDIAN DRUGS ◽

10.53879/id.57.04.12172 ◽

2020 ◽

Vol 57 (04) ◽

pp. 59-64

Author(s):

Pratibha Thaware ◽

Pushpa Karale ◽

Mahesh Karale ◽

Pranati Chavan

Keyword(s):

Methanolic Extract ◽

Radical Scavenging ◽

Reducing Power ◽

Pharmacological Action ◽

Diffusion Method ◽

Phytochemical Screening ◽

Aegle Marmelos ◽

Pharmacological Screening ◽

Hplc Data

The objective of this study was to evaluate the phytochemical and pharmacological screening of fruit extracts of Aegle marmelos using various in vitro methods. The antioxidant activity of the extracts was evaluated by using DPPH free radical scavenging and reducing power method, while well diffusion method was used for antimicrobial activity. Phytochemical screening indicated the presence of flavonoids, and phenolics were abundantly present in methanolic and aqueous extracts of A. marmelos. Methanolic extract showed significant antioxidant potential, which was however inferior to that of ascorbic acid. The methanolic extract showed maximum zone of inhibition against the S. aureus (18 mm) and it was higher than that of the standard tetracycline. The HPLC data predict that the presence of scopoletin, marmelosin and umbelliferone, which may contribute to their pharmacological action.

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Non-Toxic Virucidal Macromolecules Show High Efficacy Against Influenza Virus Ex Vivo and In Vivo

10.1101/2020.03.18.996678 ◽

2020 ◽

Author(s):

Ozgun Kocabiyik ◽

Valeria Cagno ◽

Paulo Jacob Silva ◽

Yong Zhu ◽

Laura Sedano ◽

...

Keyword(s):

Broad Spectrum ◽

Viral Infections ◽

Ex Vivo ◽

Public Health Problem ◽

Major Public Health Problem ◽

New Class ◽

Influenza Strain ◽

Low Toxicity

AbstractInfluenza is one of the most widespread viral infections worldwide and represents a major public health problem. The risk that one of the next pandemics is caused by an influenza strain is very high. It is very important to develop broad-spectrum influenza antivirals to be ready for any possible vaccine shortcomings. Anti-influenza drugs are available but they are far from ideal. Arguably, an ideal antiviral should target conserved viral domains and be virucidal, i.e. irreversibly inhibit viral infectivity. Here, we describe a new class of broad-spectrum anti-influenza macromolecules that meets these criteria and displays exceedingly low toxicity. These compounds are based on a cyclodextrin core modified on its primary face with long hydrophobic linkers terminated in 6’sialyl-N-acetyllactosamine (6’SLN) or 3’SLN. SLN enables nanomolar inhibition of the viruses while the hydrophobic linkers confer irreversibility to the inhibition. The combination of these two properties allows for efficacy in vitro against several human or avian influenza strains, as well as against a 2009 pandemic influenza strain ex vivo. Importantly, we show that, in mice, the compounds provide therapeutic efficacy when administered 24h post-infection allowing 90% survival as opposed to no survival for the placebo and oseltamivir..

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Antimalarial Activities of Peptide Antibiotics Isolated from Fungi

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.45.1.145-149.2001 ◽

2001 ◽

Vol 45 (1) ◽

pp. 145-149 ◽

Cited By ~ 42

Author(s):

G. Nagaraj ◽

M. V. Uma ◽

M. S. Shivayogi ◽

Hemalatha Balaram

Keyword(s):

High Performance ◽

Public Health Problem ◽

Chemotherapeutic Agents ◽

Major Public Health Problem ◽

Drug Resistant ◽

Peptide Antibiotics ◽

Mass Spectral Analysis ◽

Mass Spectral ◽

Micromolar Range

ABSTRACT Malaria caused by Plasmodium falciparum is a major public health problem in the developing countries of the world. Clinical treatment of malaria has become complicated due to the occurrence of infections caused by drug resistant parasites. Secondary metabolites from fungi are an attractive source of chemotherapeutic agents. This work reports the isolation and in vitro antiplasmodial activities of peptide antibiotics of fungal origin. The three peptide antibiotics used in this study were efrapeptins, zervamicins, and antiamoebin. The high-performance liquid chromatography-purified peptides were characterized by nuclear magnetic resonance and mass spectral analysis. All three fungal peptides kill P. falciparum in culture with 50% inhibitory concentrations in the micromolar range. A possible mode of action of these peptide antibiotics on P. falciparum is presented.

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Development of new dinuclear Fe(III) coordination compounds with in vitro nanomolar antitrypanosomal activity

Dalton Transactions ◽

10.1039/d1dt01048d ◽

2021 ◽

Author(s):

Felipe Figuerôa Moreira ◽

Juliana de Araujo Portes ◽

Nathalia Florencia Barros Azeredo ◽

Christiane Fernandes ◽

Adolfo Horn ◽

...

Keyword(s):

Public Health ◽

Trypanosoma Cruzi ◽

Chagas Disease ◽

Health Problem ◽

Coordination Compounds ◽

Public Health Problem ◽

Neglected Tropical Disease ◽

Major Public Health Problem ◽

Protozoan Pathogen

Chagas disease is a neglected tropical disease caused by the protozoan pathogen Trypanosoma cruzi. The disease is the major public health problem affecting about 6 to 7 million people worldwide,...

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Platelet-Rich Plasma Improves the Wound Healing Potential of Mesenchymal Stem Cells through Paracrine and Metabolism Alterations

Stem Cells International ◽

10.1155/2019/1234263 ◽

2019 ◽

Vol 2019 ◽

pp. 1-14 ◽

Cited By ~ 9

Author(s):

Barbara Hersant ◽

Mounia Sid-Ahmed ◽

Laura Braud ◽

Maud Jourdan ◽

Yasmine Baba-Amer ◽

...

Keyword(s):

Stem Cells ◽

Wound Healing ◽

Mesenchymal Stem Cells ◽

Platelet Rich Plasma ◽

Public Health Problem ◽

Major Public Health Problem ◽

Dependent Manner ◽

Safe Alternative

Chronic and acute nonhealing wounds represent a major public health problem, and replacement of cutaneous lesions by the newly regenerated skin is challenging. Mesenchymal stem cells (MSC) and platelet-rich plasma (PRP) were separately tested in the attempt to regenerate the lost skin. However, these treatments often remained inefficient to achieve complete wound healing. Additional studies suggested that PRP could be used in combination with MSC to improve the cell therapy efficacy for tissue repair. However, systematic studies related to the effects of PRP on MSC properties and their ability to rebuild skin barrier are lacking. We evaluated in a mouse exhibiting 4 full-thickness wounds, the skin repair ability of a treatment combining human adipose-derived MSC and human PRP by comparison to treatment with saline solution, PRP alone, or MSC alone. Wound healing in these animals was measured at day 3, day 7, and day 10. In addition, we examined in vitro and in vivo whether PRP alters in MSC their proangiogenic properties, their survival, and their proliferation. We showed that PRP improved the efficacy of engrafted MSC to replace lost skin in mice by accelerating the wound healing processes and ameliorating the elasticity of the newly regenerated skin. In addition, we found that PRP treatment stimulated in vitro, in a dose-dependent manner, the proangiogenic potential of MSC through enhanced secretion of soluble factors like VEGF and SDF-1. Moreover, PRP treatment ameliorated the survival and activated the proliferation of in vitro cultured MSC and that these effects were accompanied by an alteration of the MSC energetic metabolism including oxygen consumption rate and mitochondrial ATP production. Similar observations were found in vivo following combined administration of PRP and MSC into mouse wounds. In conclusion, our study strengthens that the use of PRP in combination with MSC might be a safe alternative to aid wound healing.

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Antioxidant and Antimicrobial Properties of the Essential Oil and Extracts ofZanthoxylum alatumGrown in North-Western Himalaya

The Scientific World JOURNAL ◽

10.1155/2013/790580 ◽

2013 ◽

Vol 2013 ◽

pp. 1-9 ◽

Cited By ~ 30

Author(s):

Sanjay Guleria ◽

A. K. Tiku ◽

Apurva Koul ◽

Sahil Gupta ◽

Gurjinder Singh ◽

...

Keyword(s):

Essential Oil ◽

Methanolic Extract ◽

Micrococcus Luteus ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Reducing Power ◽

Preparative Thin Layer Chromatography ◽

Gas Chromatography Mass Spectrometry ◽

Curvularia Lunata

The essential oil obtained from the fresh leaves ofZanthoxylum alatumwas analysed by gas chromatography/mass spectrometry (GC/MS). Fourteen components were identified, and linalool (30.58%), 2-decanone (20.85%),β-fenchol (9.43%), 2-tridecanone (8.86%),β-phellandrene (5.99%), Sabinene (4.82%), andα-pinene (4.11%) were the main components. The EO and methanolic extract ofZ. alatumexhibited potent antifungal activity againstAlternaria alternata,Alternaria brassicae, andCurvularia lunata. The EO also showed significant antibacterial activity againstBacillus subtilis,Micrococcus luteus,Staphylococcus aureus, andEscherichia coli. Further, antimicrobial constituents of the EO were isolated by bioautography and preparative thin layer chromatography (PTLC) and identified asβ-fenchol and linalool using GC/MS analysis. In addition to this, the free radical scavenging activity and antioxidant potential of EO and methanolic extract/fractions ofZ. alatumwere also investigated usingin vitroassays including scavenging ability against DPPH•, reducing power and chelating ability on Fe2+ions. Our results demonstrate thatZ. alatumcould be used as a resource of antioxidant and antimicrobial compounds which may find applications in food and pesticide industries.

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Effect of Different Terpene-Containing Essential Oils on the Proliferation ofEchinococcus granulosusLarval Cells

Interdisciplinary Perspectives on Infectious Diseases ◽

10.1155/2014/746931 ◽

2014 ◽

Vol 2014 ◽

pp. 1-7 ◽

Cited By ~ 7

Author(s):

Clara María Albani ◽

Guillermo María Denegri ◽

María Celina Elissondo

Keyword(s):

Essential Oils ◽

Effective Means ◽

Control Cell ◽

Larval Growth ◽

Public Health Problem ◽

Mentha Piperita ◽

Major Public Health Problem ◽

Isolated Cells ◽

Vitro Effect

Human cystic echinococcosis remains a major public health problem on several countries and the treatment strategies are not solved. The aim of the present work was to determine the in vitro effect of thymol andMentha piperita,M. pulegium,andRosmarinus officinalisessential oils on the proliferation ofE. granulosuslarval cells. Isolated cells and cellular aggregates were obtained from hydatid cyst’s germinal layer and exposed to 1, 5, and 10 μg/ml of thymol and the different essential oils for 7 days. Drug effect was evaluated using test viability and scanning electron microscopy. Control cell culture viability was 2.1 x 106(100%) after 7 days of incubation. At day 7, thymol 5 μg/ml caused a reduction in cell viability of 63% and the essential oils ofM. piperita10 μg/ml,M. pulegium10 μg/ml, andR. officinalis10 μg/ml produced a reduction in the viability of 77, 82, and 71%, respectively. Moreover essential oils caused reduction in cell number, collapsed cells, and loss of normal tridimensional composition of the aggregates. Due to the inhibitory effect caused by essential oils onE. granulosuscells we suggested that it would be an effective means for suppression of larval growth.

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