Synthesis and Pharmacological Screening of Novelmeso-Substituted Porphyrin Analogs

2012 ◽  
Vol 346 (1) ◽  
pp. 53-61 ◽  
Author(s):  
Ahmed A. Fadda ◽  
Rasha E. El-Mekawy ◽  
Ahmed I. El-Shafei ◽  
Harold Freeman
Keyword(s):  
Pharmacological Screening ◽  
Porphyrin Analogs

Pharmacological Screening of Various Ethnomedicinally Important Plants for their Antibacterial Activities

Planta Medica ◽  
2013 ◽  
Vol 79 (05) ◽  
Author(s):  
KK Sharma ◽  
JBS Kachhawa ◽  
N Sharma ◽  
S Tyagi ◽  
V Sharma
Keyword(s):  
Antibacterial Activities ◽  
Pharmacological Screening

Metabolomics and Pharmacological Screening of Aspergillus versicolor Isolated from Hyrtios erectus Red Sea Sponge; Egypt

2020 ◽  
Vol 16 (7) ◽  
pp. 1083-1102
Author(s):  
Mohamed A. Shreadah ◽  
Nehad M.A. El Moneam ◽  
Samy A. El-Assar ◽  
Asmaa Nabil-Adam
Keyword(s):  
Oxidative Stress ◽  
Red Sea ◽  
Crude Extract ◽  
Quantitative Methods ◽  
Total Phenolic ◽  
Aspergillus Versicolor ◽  
Crude Extracts ◽  
Study Results ◽  
Anti Inflammatory ◽  
Pharmacological Screening

Background: Aspergillus Versicolor is a marine-derived fungus isolated from Hyrtios Erectus Red Sea sponge. Methods: The aim of this study was to carry out a pharmacological screening and investigation for the in vitro biological activity (antioxidant, cholinergic, antidiabetic and anticancer) of Aspergillus Versicolor crude extract’s active compounds by using different qualitative and quantitative methods. Results: The present study results showed that Aspergillus Versicolor crude extracts contain 0.6 mg total phenolic/mg crude extract. Aspergillus Versicolor also showed a potent antioxidative capacity by decreasing the oxidation of ABTS. The anticancer and inhibitory effects of Aspergillus Versicolor crude extracts on PTK and SHKI were found to be 75.29 % and 80.76%; respectively. The AChE inhibitory assay revealed that Aspergillus Versicolor extracts had an inhibitory percentage of 86.67%. Furthermore, the anti-inflammatory activity using COX1, COX2, TNF, and IL6 was 77.32, 85.21 %, 59.83%, and 56.15%; respectively. Additionally, the anti-viral effect using reverse transcriptase enzyme showed high antiviral activity with 92.10 %. Conclusion: The current study confirmed that the Aspergillus versicolor crude extract and its active constituents showed strong effects on diminishing the oxidative stress, neurodegenerative damage, antiinflammatory, anti-cancer and anti-viral, suggesting their beneficial role as a promising fermented product in the treatment of cancer, oxidative stress, Alzheimer's, anti-inflammatory and anti-viral diseases.

3-(s-Hydrindacen-4-yl)propylamines and 4-(s-hydrindacen-4-yl)butylamines; Synthesis and pharmacological screening

1981 ◽  
Vol 46 (8) ◽  
pp. 1800-1807 ◽  
Author(s):  
Zdeněk Vejdělek ◽  
Marie Bartošová ◽  
Miroslav Protiva
Keyword(s):  
Malonic Acid ◽  
Local Anaesthetics ◽  
Lithium Aluminium Hydride ◽  
Spasmolytic Activity ◽  
Lithium Aluminium ◽  
Malonic Acid Derivatives ◽  
Pharmacological Screening ◽  
Hydroxyethyl Piperazine

4-Chloromethyl-s-hydrindacene (VIIa) was transformed via the malonic acid derivatives VIIIa and IXa to the acid Xb which afforded in four steps the homological acid Xc. Reactions of chlorides of both acids (XIbc ) with dimethylamine, 1-methylpiperazine and 1-(2-hydroxyethyl)piperazine led to the amides XIIbc-XIVbc which were reduced with lithium aluminium hydride to the title compounds IVcd-VIcd. The amines obtained show central neuroleptic effects only in subtoxic doses; they are also potent local anaesthetics and have significant spasmolytic activity of the neurotropic as well as musculotropic type.

scholarly journals Phytochemical and Ethnopharmacological Perspectives of Ehretia laevis

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3489
Author(s):  
Pooja Sharma ◽  
Richa Shri ◽  
Fidele Ntie-Kang ◽  
Suresh Kumar
Keyword(s):  
Pentacyclic Triterpenoids ◽  
Diverse Range ◽  
Plant Parts ◽  
Tribal Communities ◽  
Crude Extracts ◽  
Traditional Remedy ◽  
Botanical Description ◽  
Pharmacological Screening ◽  
Therapeutic Activities ◽  
First Time

Ehretia laevis Roxb. (Boraginaceae) has been extensively used as a traditional remedy for the treatment of a diverse range of ailments related to the respiratory system, the gastrointestinal tract, the reproductive system, and against several infections. This review critically assesses and documents, for the first time, the fragmented information on E. laevis, including its botanical description, folklore uses, bioactive phyto metabolites and pharmacological activities. The goal is to explore this plant therapeutically. Ethnomedicinal surveys reveal that E. laevis has been used by tribal communities in Asian countries for the treatment of various disorders. Quantitative and qualitative phytochemical investigations of E. laevis showed the presence of important phytoconstituents such as pentacyclic triterpenoids, phenolic acids, flavonoids, fatty acids, steroids, alkaloids, aliphatic alcohols, hydrocarbons, amino acids, carbohydrates, vitamins and minerals. Fresh plant parts, crude extracts, fractions and isolated compounds have been reported to exhibit broad spectrum of therapeutic activities viz., antioxidant, antiarthritic, antidiabetic, anti-inflammatory, antiulcer, antidiarrheal, antidysenteric, wound healing and anti-infective activities. E. laevis is shown to be an excellent potential source of drugs for the mitigation of jaundice, asthma, dysentery, ulcers, diarrhea, ringworm, eczema, diabetes, fissure, syphilis, cuts and wounds, inflammation, liver problems, venereal and infectious disorders. Although few investigations authenticated its traditional uses but employed uncharacterized crude extracts of the plant, the major concerns raised are reproducibility of therapeutic efficacy and safety of plant material. The outcomes of limited pharmacological screening and reported bioactive compounds of E. laevis suggest that there is an urgent need for in-depth pharmacological investigations of the plant.

scholarly journals Survey of ethnobotanical cocktails commonly used in the treatment of malaria in southwestern Nigeria

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Rachel Omagha ◽  
Emmanuel Taiwo Idowu ◽  
Chibuisi Gideon Alimba ◽  
Adetoro Olubunmi Otubanjo ◽  
Adeniyi Kazeem Adeneye
Keyword(s):  
Herbal Medicines ◽  
Oral Route ◽  
Malaria Treatment ◽  
Herbal Remedies ◽  
Southwestern Nigeria ◽  
Traditional Treatment ◽  
South West ◽  
Pharmacological Screening ◽  
Selection Of ◽  
Structured Questionnaire

Abstract Background Combination of different antimalarials has become the popular method of care for malaria morbidity in conventional and traditional treatment approaches due to the need to increase the efficacy and reduce the selection of drug resistance. A worrisome concern is the critical gaps with regards to the information available on antimalarial herbal cocktails. This study presents cocktail herbal remedies in ethnomedicinal approaches to malaria treatment in Oyo and Ogun states, South West Nigeria. Ethnobotanical information on indigenous antimalarials used in combination remedies was collected from herbal practitioners using a semi-structured questionnaire. Results Findings showed majority of respondents treat malaria with combination herbal remedies. They sighted their beliefs and customs, the efficacy, affordability and availability of these herbs as reasons for their adoption of herbal medicines as their preferred mode of treating malaria. Enquiry revealed 26 sets of cocktail antimalarials from a variety of plant species. The plants and ingredients are extracted and used as decoction, infusion or steam baths. Oral route was the most popular mode of administration. Respondents reported they drink one to two medium-sized cups of the recipe on an average of two times daily within a duration of about 10 days. Conclusions Herbal antimalarial remedies continue to be the popular treatments option in our localities. This study provides knowledge of the diverse ways respondents combine medicinal herbs and other local ingredients for malaria treatment. Pharmacological screening is urgently needed to validate their safety and efficacy in order to protect the health of our locals heavily relying on them to combat high burdens of malaria.

Cyclic amidines derived from benz[c,d]indole and 4,5-dihydro-3H-1-benzazepine including some related compounds: Synthesis and pharmacological screening

1985 ◽  
Vol 50 (8) ◽  
pp. 1888-1898 ◽  
Author(s):  
Miroslav Protiva ◽  
Zdeněk Šedivý ◽  
Jiří Holubek ◽  
Emil Svátek ◽  
Jiří Němec
Keyword(s):  
Titanium Tetrachloride ◽  
Aqueous Sodium Hydroxide ◽  
Secondary Amines ◽  
Primary Amines ◽  
Open Chain ◽  
Lithium Aluminium ◽  
Pharmacological Screening ◽  
Antiinflammatory Effects ◽  
Related Compounds ◽  
Sodium Amide

Reactions of naphthostyril (I) with primary and secondary amines and titanium tetrachloride afforded cyclic amidines III-IX. Hydrogenation of I on Pd-C resulted in the 6,7,8,8a-tetrahydro derivative X which gave by treatment with sodium amide and 3-dimethylaminopropyl chloride the N-(aminoalkyl) compound XI. Reduction of I and its N-methyl derivative II with sodium amalgam in aqueous sodium hydroxide gave the 2a,3,4,5-tetrahydro derivatives XII and XIII. Reaction of XIII with sodium amide and 3-dimethylaminopropyl chloride afforded the 2a-(aminoalkyl) compound XIV. 1,3,4,5-Tetrahydro-1-benzazepin-2-one (XV) treated with primary amines and titanium tetrachloride gave the amidines XVI-XVIII. 3-Methyl-7,8,9,9a-tetrahydro-1H-benz[d,e]isoquinoline (XIX) was reduced with sodium borohydride to compound XX which was alkylated with propargyl bromide to 1-methyl-2-propargyl-2,3,3a,4,5,6-hexahydro-1H-benz[d,e]isoquinoline (XXI). An attempt to prepare the 2-(2-phenylethyl) analogue by treatment of compound XX with phenylacetyl chloride and by the following reduction with lithium aluminium hydride resulted in the open-chain amine XXII. The lactams I, II, X, and XIII showed some discoordinating, hypothermic, peripheral vasodilating, hyperglycaemic, diuretic and antiinflammatory effects. The amidines III-IX and XVI-XVIII had local anaesthetic, slight hypotensive, antiarrhythmic, peripheral myorelaxant, papaverine-like spasmolytic and thiopental potentiating effects.

PHYTOCHEMICAL SCREENING AND PHARMACOLOGICAL EVALUATION OF AEGLE MARMELOS FRUIT

INDIAN DRUGS ◽  
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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