Rutin Inhibits F, G, N and O gonorrhea strains, 2008 WHO N-gonorrhea Reference strains, in vitro

2020 ◽  
Vol 1 ◽  
pp. 41-49
Author(s):  
Mutendela Tabize Olivier ◽  
Freddy Munyololo Muganza ◽  
Leshweni Jeremia Shai ◽  
Stanley Sechene Gololo
Keyword(s):  
Precipitation Method ◽  
Published Data ◽  
Traditional Use ◽  
South Africans ◽  
Neisseria Gonorrhoea ◽  
Inhibition Concentration ◽  
Résonance Magnétique ◽  
Neisseria Gonorrhea ◽  
Reference Strains

Rutin was isolated from methanol extract of the aerial part of Asparagus suaveolens using precipitation method. South Africans use Asparagus suaveolens to treat gonorrhea infections. The obtained Nuclear Magnetic Resonance (NMR) and Liquid Chromatography-Mass Spectroscopy (LC-MS) data and visiting the published data on the isolation of rutin confirmed the structure. The 2008 WHO Neisseria gonorrhea reference strains were used to evaluate microbial activity of rutin against the gonorrhea strains. Rutin found to be bacteriostatic against WHO 2008 Neisseria gonorrhoea F, G, N and O strains with the minimum inhibition concentration of 0.40, 0.65, 0.22 and 0.65 mg/ml, respectively. In addition, rutin fare better than the reference drugs and bactericidal against K, L, M, and P strains. These results support the traditional use of Asparagus suaveolens against gonorrhea infections by South African indigenous people. To our knowledge, this is the first study indicating the activity of rutin against N.gonorrhea strains. Résumé: La rutine a été isolée à partir d'un extrait au méthanol de la partie aérienne d'Asparagus suaveolens en utilisant la méthode de précipitation. Les SudAfricains utilisent Asparagus suaveolens pour traiter les infections gonorrhées. Les données obtenues par résonance magnétique nucléaire (RMN) et par chromatographie liquide-spectroscopie de masse (LCMS) et la consultation des données publiées sur l'isolement de la rutine ont confirmé la structure. Les souches de référence OMS de Neisseria gonorrhea de 2008 ont été utilisées pour évaluer l'activité microbienne de la rutine contre les souches de gonorrhée. La rutine s'est révélée bactériostatique contre les souches de Neisseria gonorrhea F, G, N et O de l'OMS 2008 avec une concentration minimale d'inhibition de 0,40, 0,65, 0,22 et 0,65 mg/ml, respectivement. De plus, la rutine se porte mieux que les médicaments de référence et bactéricide contre les souches K, L, M et P. Ces résultats soutiennent l'utilisation traditionnelle d'Asparagus suaveolens contre les infections gonorrhées par les populations autochtones sud-africaines. À notre connaissance, il s'agit de la première étude indiquant l'activité de la rutine contre les souches de N. gonorrhée.

scholarly journals In Vitro Activity of Lawsonia inermis (Henna) on Some Pathogenic Fungi

2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
Elham Abdelbasit Suleiman ◽  
Elbasheir Ahmed Mohamed
Keyword(s):  
Antifungal Activity ◽  
Fungal Infections ◽  
Pathogenic Fungi ◽  
Diffusion Method ◽  
In Vitro Activity ◽  
Lawsonia Inermis ◽  
Traditional Use ◽  
Yeast Strains ◽  
Inhibition Concentration

The present study was conducted to investigate antifungal activity of Lawsonia inermis (Henna plant). Leaf samples of the plant were collected from Eastern Nile of Khartoum State, Sudan. Ethanol and petroleum ether extracts were obtained by maceration (cold method). The extracts were bioassayed in vitro to know their bioactivity to inhibit the growth of tested fungi. The cup-plate agar diffusion method was adopted to assess the antifungal activity of the extracts against tested yeasts, while agar incorporated method was used for other molds. Both extracts revealed antifungal activity against all yeast strains except Pichia fabianii which was found resistant to both ethanol and ether extracts. The results displayed antifungal activity against tested fungi. Minimum inhibition concentration (MIC) of 5, 7.5, and 10 mg/mL was found to inhibit the growth of tested dermatophytes. The obtained results revealed antifungal activity of Henna leaves extracts which support the traditional use of Henna in therapy of fungal infections. The possibility of therapeutic use of Sudanese Henna as antifungal agent is recommended.

scholarly journals In vitro Antigonorrhea Activity of the Aerial Part of Asparagus suaveolens n-Hexane Fraction and Palmitone as a Bioactive Compound

2016 ◽  
Vol 11 (9) ◽  
pp. 1934578X1601100
Author(s):  
Mutendela Tabize Olivier ◽  
Freddy Munyololo Muganza ◽  
Leshweni Jeremia Shai ◽  
Stanley Sechene Gololo
Keyword(s):  
South Africa ◽  
Aerial Part ◽  
Antimicrobial Properties ◽  
Bioactive Compound ◽  
Current Investigation ◽  
Traditional Use ◽  
Anticonvulsant Agent ◽  
Neisseria Gonorrhea ◽  
Who 2008

Asparagus suaveolens is a medicinal plant used in Lesotho and South Africa to treat epilepsy and gonorrhea. The current investigation identifies the compound responsible for the antiepileptic and antimicrobial properties as palmitone which showed antigonorrhea activities against WHO 2008 Neisseria gonorrhea F and O strains more than the standard used, gentamicin. These results support the traditional use of A. suaveolens for treatment of gonorrhea and epilepsy since palmitone is known as an anticonvulsant agent. This is the first study indicating the presence of palmitone in the Asparagus genus and demonstrates the in vitro antigonorrhea activity of palmitone.

Development and Characterization Colchicine-Loaded PEGylated Gelatin Nanoparticles for Targeted Delivery to Tumor

2013 ◽  
Vol 6 (2) ◽  
pp. 2058-2063
Author(s):  
G D Chandrethiya ◽  
P K Shelat ◽  
M N Zaveri
Keyword(s):  
Drug Delivery ◽  
Targeted Delivery ◽  
High Performance ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Spherical Particles ◽  
Precipitation Method ◽  
Antitumoral Activity ◽  
Gelatin Nanoparticles

PEGylated gelatin nanoparticles loaded with colchicine were prepared by ethanol precipitation method. Poly-(ethylene glycol)-5000-monomethylether (MPEG 5000), a hydrophilic polymer, was used to pegylate gelatin.  Gluteraldehyde was used as cross-linking agent. To obtain a high quality product, major formulation parameters were optimized.  Spherical particles with mean particles of 193 nm were measured by a Malvern particle size analyzer. Entrapment efficiency was found to be 71.7 ± 1.4% and determined with reverse phase high performance liquid charomatography (RP-HPLC). The in vitro drug release study was performed by dialysis bag method for a period of 168 hours. Lyophilizaton study showed sucrose at lower concentrations proved the best cryoprotectant for this formulation.  Stability study revealed that lyophilized nanoparticles were equally effective (p < 0.05) after one year of storage at 2-8°C with ambient humidity. In vitro antitumoral activity was accessed using the MCF-7 cell line by MTT assay.  The IC50 value was found to be 0.034 μg/ml for the prepared formulation. The results indicate that PEGylated gelatin nanoparticles could be utilized as a potential drug delivery for targeted drug delivery of tumors.  

Solubility Enhancement of Poorly Water-Soluble Antifungal Drug Acyclovir by Nanocrystal Formulation Approach

2018 ◽  
Vol 11 (2) ◽  
pp. 4036-4042
Author(s):  
Prakash Goudanavar ◽  
Ankit Acharya ◽  
Vinay C.H
Keyword(s):  
Chemical Interaction ◽  
Research Work ◽  
Antiviral Drug ◽  
In Vitro Release ◽  
Oral Route ◽  
Water Soluble ◽  
Precipitation Method ◽  
Dsc Studies ◽  
Ft Ir

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. 

Ethnomedicinal uses, Phytochemistry and Pharmacological Aspects of the Genus Berberis Linn: A Comprehensive Review

2020 ◽  
Vol 23 ◽  
Author(s):  
Roohi Mohi-ud-din ◽  
Reyaz Hassan Mir ◽  
Prince Ahad Mir ◽  
Saeema Farooq ◽  
Syed Naiem Raza ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Pharmacological Activities ◽  
Traditional Use ◽  
Comprehensive Review ◽  
Wide Range ◽  
Anti Cancer ◽  
Comprehensive Survey ◽  
Ethnomedicinal Uses

Background: Genus Berberis (family Berberidaceae), which contains about 650 species and 17 genera worldwide, has been used in folklore and various traditional medicine systems. Berberis Linn. is the most established group among genera with around 450-500 species across the world. This comprehensive review will not only help researchers for further evaluation but also provide substantial information for future exploitation of species to develop novel herbal formulations. Objective: The present review is focussed to summarize and collect the updated review of information of Genus Berberis species reported to date regarding their ethnomedicinal information, chemical constituents, traditional/folklore use, and reported pharmacological activities on more than 40 species of Berberis. Conclusion: A comprehensive survey of the literature reveals that various species of the genus possess various phytoconstituents mainly alkaloids, flavonoid based compounds isolated from different parts of a plant with a wide range of pharmacological activities. So far, many pharmacological activities like anti-cancer, anti-hyperlipidemic, hepatoprotective, immunomodulatory, anti-inflammatory both in vitro & in vivo and clinical study of different extracts/isolated compounds of different species of Berberis have been reported, proving their importance as a medicinal plant and claiming their traditional use.

Flavonoids Extracted from Asteriscus graveolens Improve Glucose Metabo-lism and Lipid Profile in Diabetic Rats

2020 ◽  
Vol 20 ◽  
Author(s):  
Fadwa El-ouady ◽  
Fatima Bachir ◽  
Mohamed Eddouks
Keyword(s):  
Glucose Tolerance ◽  
Lipid Profile ◽  
Histopathological Examination ◽  
Oral Treatment ◽  
Hdl Cholesterol ◽  
Diabetic Rats ◽  
Oral Glucose ◽  
Traditional Use ◽  
Soxhlet Apparatus

Aim: This study aimed to evaluate the antidiabetic and antihyperlipidemic effects of Asteriscus graveolens. Background: Asteriscus graveolens (Asteraceae) is a medicinal plant widely used by the Moroccan population to treat various diseases including diabetes. Objective: This work aimed to assess the capacity of flavonoids extracted from Asteriscus graveolens (FEE) to improve diabetes mellitus and dyslipidemia in normal and STZ-induced diabetic rats. Methods: Flavonoids were extracted from A. graveolens using the Soxhlet apparatus and using different organic solvents. Normal and streptozotocin-induced diabetic rats were treated orally by the extract of A. graveolens at a dose of 10 mg/kg. The oral treatment during 15 days was used to evaluate the effect of the flavonoids extracted from A. graveolens on blood glucose level and lipid profile in normal and diabetic rats. The oral glucose tolerance test as well as the analysis of histopathological examination of liver was performed. The antioxidant activity of FEE was also assessed by the method of trapping of free radical 2,2-diphenyl-1 picrylhydrazyl (DPPH), in order to estimate the mechanisms of action involved by FEE to improve hyperglycemia and lipid profile in normal and diabetic rats. Results: FEE reduced serum glucose concentrations in both normal and diabetic rats and exhibited in the last group lowering total cholesterol and triglycerides effects as well as improvement of the HDL-cholesterol serum level. In addition, a remarkable influence on glucose tolerance was also noticed after FEE treatment. Moreover, FEE was able to improve histopathological status of liver and possess a potential antioxidant effect in vitro. Conclusion: In conclusion, this study demonstrates the hypoglycemic and antihyperlipidemic effects of FEE in rats supporting then its traditional use for the management of diabetes.

Evaluation of Snake Venom’s PhospholipaseA2 Enzyme Inhibition Activity of Cyphostemma adenocoule

2020 ◽  
Vol 14 (3) ◽  
pp. 196-202
Author(s):  
Atul Kaushik ◽  
Teamrat S. Tesfai ◽  
Daniel K. Barkh ◽  
Furtuna K. Ghebremeskel ◽  
Habtom G. Zerihun ◽  
...  
Keyword(s):  
Enzyme Inhibition ◽  
Snake Venom ◽  
Ethanol Extract ◽  
Egg Yolk ◽  
Chloroform Extract ◽  
Inhibition Activity ◽  
Traditional Use ◽  
Snake Bites ◽  
Ethanol Extracts

Background: A snake bite is fundamentally an injury often resulting in puncture wounds meted out by the animal's fangs and occasionally resulting in envenomation. Rate of snake bites around 5,400,000 bites per year leads to over 2,500,000 envenomings and around 125,000 fatal cases annually. Snake venom enzymes are rich in metalloproteinases, phospholipaseA2, proteinases, acetylcholinesterases and hyaluronidases. Objective: Cyphostemma adenocoule is traditionally being used for the treatment of snake bites in Eritrea. The present research was aimed at evaluating the snake venom enzyme inhibition activity of C. adenocoule against puff adder venom and developing a base for the traditional use of the plant against snakebites in Eritrea. Methods: The anti-venom activity of C. adenocoule was assessed in-vitro through phospholipaseA2 enzyme inhibition assay using egg yolk as a cell. The ethanol and chloroform extracts of C. adenocoule showed in vitro anti phospholipase A2 activity, whereas the water extracts of the plant showed no activity. Results: Among the extracts of C. adenocoule, the highest percentage of inhibition was obtained from chloroform extract (95.55% at 100mg/ml). The extract showed prominent activity at different concentrations (34.7% at10mg/ml, 48.8% at 20mg/ml, 54.8% at 40mg/ml, 60.9% at 60mg/ml, 80.5% at 80mg /ml). The ethanol extract also showed certain activity at various concentrations (25.22% at10mg/ml, 14.78% at 20mg/ml, 2.6% at40mg/ml). The activity of the chloroform extracts increases as concentration increases, whereas the activity of the ethanol extracts decreases as concentration increases. The aqueous extract of C. adenocoule did not show any activity at all concentrations. Conclusion: In this study, the chloroform and ethanol extracts of the plant inhibited the enzyme of interest and thus proved the efficacy of anti-snake venom activity of the plant.

scholarly journals Anti-Inflammatory Properties of Injectable Betamethasone-Loaded Tyramine-Modified Gellan Gum/Silk Fibroin Hydrogels

Biomolecules ◽  
2020 ◽  
Vol 10 (10) ◽  
pp. 1456
Author(s):  
Isabel Matos Oliveira ◽  
Cristiana Gonçalves ◽  
Myeong Eun Shin ◽  
Sumi Lee ◽  
Rui Luis Reis ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Mechanical Properties ◽  
Silk Fibroin ◽  
Therapeutic Efficacy ◽  
Composite Structures ◽  
Gelation Time ◽  
Polymeric Materials ◽  
Gellan Gum ◽  
Traditional Use

Rheumatoid arthritis is a rheumatic disease for which a healing treatment does not presently exist. Silk fibroin has been extensively studied for use in drug delivery systems due to its uniqueness, versatility and strong clinical track record in medicine. However, in general, natural polymeric materials are not mechanically stable enough, and have high rates of biodegradation. Thus, synthetic materials such as gellan gum can be used to produce composite structures with biological signals to promote tissue-specific interactions while providing the desired mechanical properties. In this work, we aimed to produce hydrogels of tyramine-modified gellan gum with silk fibroin (Ty–GG/SF) via horseradish peroxidase (HRP), with encapsulated betamethasone, to improve the biocompatibility and mechanical properties, and further increase therapeutic efficacy to treat rheumatoid arthritis (RA). The Ty–GG/SF hydrogels presented a β-sheet secondary structure, with gelation time around 2–5 min, good resistance to enzymatic degradation, a suitable injectability profile, viscoelastic capacity with a significant solid component and a betamethasone-controlled release profile over time. In vitro studies showed that Ty–GG/SF hydrogels did not produce a deleterious effect on cellular metabolic activity, morphology or proliferation. Furthermore, Ty–GG/SF hydrogels with encapsulated betamethasone revealed greater therapeutic efficacy than the drug applied alone. Therefore, this strategy can provide an improvement in therapeutic efficacy when compared to the traditional use of drugs for the treatment of rheumatoid arthritis.

scholarly journals Review of T-2307, an Investigational Agent That Causes Collapse of Fungal Mitochondrial Membrane Potential

2021 ◽  
Vol 7 (2) ◽  
pp. 130
Author(s):  
Nathan P. Wiederhold
Keyword(s):  
Membrane Potential ◽  
Mitochondrial Membrane Potential ◽  
Candida Species ◽  
Mammalian Cells ◽  
Mitochondrial Membrane ◽  
Fungal Infections ◽  
Published Data ◽  
Candida Auris

Invasive infections caused by Candida that are resistant to clinically available antifungals are of increasing concern. Increasing rates of fluconazole resistance in non-albicans Candida species have been documented in multiple countries on several continents. This situation has been further exacerbated over the last several years by Candida auris, as isolates of this emerging pathogen that are often resistant to multiple antifungals. T-2307 is an aromatic diamidine currently in development for the treatment of invasive fungal infections. This agent has been shown to selectively cause the collapse of the mitochondrial membrane potential in yeasts when compared to mammalian cells. In vitro activity has been demonstrated against Candida species, including C. albicans, C. glabrata, and C. auris strains, which are resistant to azole and echinocandin antifungals. Activity has also been reported against Cryptococcus species, and this has translated into in vivo efficacy in experimental models of invasive candidiasis and cryptococcosis. However, little is known regarding the clinical efficacy and safety of this agent, as published data from studies involving humans are not currently available.

scholarly journals Novel Insights on the Role of Nitric Oxide in the Ovary: A Review of the Literature

2021 ◽  
Vol 18 (3) ◽  
pp. 980
Author(s):  
Maria Cristina Budani ◽  
Gian Mario Tiboni
Keyword(s):  
Nitric Oxide ◽  
In Vivo Studies ◽  
Published Data ◽  
Vitro Fertilization ◽  
Peripheral Neurons ◽  
Relevant Role ◽  
Oocyte Meiotic Maturation

Nitric oxide (NO) is formed during the oxidation of L-arginine to L-citrulline by the action of multiple isoenzymes of NO synthase (NOS): neuronal NOS (nNOS), endotelial NOS (eNOS), and inducible NOS (iNOS). NO plays a relevant role in the vascular endothelium, in central and peripheral neurons, and in immunity and inflammatory systems. In addition, several authors showed a consistent contribution of NO to different aspects of the reproductive physiology. The aim of the present review is to analyse the published data on the role of NO within the ovary. It has been demonstrated that the multiple isoenzymes of NOS are expressed and localized in the ovary of different species. More to the point, a consistent role was ascribed to NO in the processes of steroidogenesis, folliculogenesis, and oocyte meiotic maturation in in vitro and in vivo studies using animal models. Unfortunately, there are few nitric oxide data for humans; there are preliminary data on the implication of nitric oxide for oocyte/embryo quality and in-vitro fertilization/embryo transfer (IVF/ET) parameters. NO plays a remarkable role in the ovary, but more investigation is needed, in particular in the context of human ovarian physiology.

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