scholarly journals Compounds from Terminalia mantaly L. (Combretaceae) Stem Bark Exhibit Potent Inhibition against some Pathogenic Yeasts and Enzymes of Metabolic Significance

2016 ◽  
Author(s):  
Marthe Aimée Tchuente Tchuenmogne ◽  
Thierry Kammalac Ngouana ◽  
Sebastian Gohlke ◽  
Rufin M. T. Kouipou ◽  
Abdulselam Aslan ◽  
...  
Keyword(s):  
Stem Bark ◽  
Published Data ◽  
Reference Compound ◽  
Glutathione S Transferase ◽  
Pathogenic Yeast ◽  
Potent Inhibition ◽  
Ic50 Values ◽  
Erythrocyte Carbonic Anhydrase ◽  
Metabolic Significance

The chemical investigation of the anti-yeast methanol extract from the stem bark of Terminalia mantaly led to the isolation of seven compounds: 3-O-methyl-4-O-α-rhamnopyranoside ellagic acid (1), 3-O-mehylellagic acid (2), arjungenin or 2,3,19,23-tetrahydroxyolean-12-en-28-oïc acid (3), arjunglucoside or 2,3,19,23-tetrahydroxyolean-12-en-28-oïc acid glucopyranoside (4), 2α,3α,24-trihydroxyolean-11,13(18)-dien-28-oïc acid (5), stigmasterol (6), stigmasterol 3-O-β-D-glucopyranoside (7). Their structures were established by means of spectroscopic analysis and comparison with published data. Compounds 1-5 were tested in vitro for activity against three pathogenic yeast isolates, Candida albicans, Candida parapsilosis and Candida krusei. The activity of compounds 1, 2 and 4 were comparable to that of the reference compound fluconazole (MIC values below 32 µg/ml) against the three tested yeast isolates. They were also tested for inhibitory properties against four enzymes of metabolic significance: Glucose-6-Phosphate Deshydrogenase (G6PD), human erythrocyte Carbonic anhydrase I and II (hCA I and hCA II), Glutathione S-transferase (GST). Compound 4 showed highly potent inhibitory property against the four tested enzymes with overall IC50 values below 4 µM and inhibitory constant (Ki) <3 µM.

Novel Iodinated Hydrazide-hydrazones and their Analogues as Acetyl- and Butyrylcholinesterase Inhibitors

2020 ◽  
Vol 20 (23) ◽  
pp. 2106-2117
Author(s):  
Martin Krátký ◽  
Šárka Štěpánková ◽  
Michaela Brablíková ◽  
Katarína Svrčková ◽  
Markéta Švarcová ◽  
...  
Keyword(s):  
Biological Activities ◽  
Structural Parameters ◽  
Covalent Binding ◽  
Docking Studies ◽  
Potent Inhibition ◽  
Brain Barrier Permeability ◽  
Electric Eel ◽  
Ic50 Values ◽  
Ellman’S Method

Background: Hydrazide-hydrazones have been known as scaffold with various biological activities including inhibition of acetyl- (AChE) and butyrylcholinesterase (BuChE). Cholinesterase inhibitors are mainstays of dementias’ treatment. Objective: Twenty-five iodinated hydrazide-hydrazones and their analogues were designed as potential central AChE and BuChE inhibitors. Methods: Hydrazide-hydrazones were synthesized from 4-substituted benzohydrazides and 2-/4- hydroxy-3,5-diiodobenzaldehydes. The compounds were investigated in vitro for their potency to inhibit AChE from electric eel and BuChE from equine serum using Ellman’s method. We calculated also physicochemical and structural parameters for CNS delivery. Results: The derivatives exhibited a moderate dual inhibition with IC50 values ranging from 15.1-140.5 and 35.5 to 170.5 μmol.L-1 for AChE and BuChE, respectively. Generally, the compounds produced a balanced or more potent inhibition of AChE. N'-[(E)-(4-Hydroxy-3,5-diiodophenyl)methylidene]-4- nitrobenzohydrazide 2k and 4-fluoro-N'-(2-hydroxy-3,5-diiodobenzyl)benzohydrazide 3a were the most potent inhibitors of AChE and BuChE, respectively. Structure-activity relationships were established, and molecular docking studies confirmed interaction with enzymes. Conclusion: Many novel hydrazide-hydrazones showed lower IC50 values than rivastigmine against AChE and some of them were comparable for BuChE to this drug used for the treatment of dementia. They interact with cholinesterases via non-covalent binding into the active site. Based on the BOILEDEgg approach, the majority of the derivatives met the criteria for blood-brain-barrier permeability.

scholarly journals In Vitro Anti-Diabetic Activities and UHPLC-ESI-MS/MS Profile of Muntingia calabura Leaves Extract

Molecules ◽  
2022 ◽  
Vol 27 (1) ◽  
pp. 287
Author(s):  
Nur Khaleeda Zulaikha Zolkeflee ◽  
Nurul Shazini Ramli ◽  
Azrina Azlan ◽  
Faridah Abas
Keyword(s):  
Published Data ◽  
Drying Methods ◽  
Esi Ms ◽  
Synthetic Drugs ◽  
Ic50 Values ◽  
Phytochemical Profile ◽  
Ultrahigh Performance Liquid Chromatography ◽  
Diabetic Treatment ◽  
Muntingia Calabura

Anti-diabetic compounds from natural sources are now being preferred to prevent or treat diabetes due to adverse effects of synthetic drugs. The decoction of Muntingia calabura leaves was traditionally consumed for diabetes treatment. However, there has not been any published data currently available on the processing effects on this plant’s biological activity and phytochemical profile. Therefore, this study aims to evaluate the effect of three drying methods (freeze-drying (FD), air-drying (AD), and oven-drying (OD)) and ethanol:water ratios (0, 50, and 100%) on in vitro anti-diabetic activities of M. calabura leaves. In addition, an ultrahigh-performance-liquid chromatography–electrospray ionization tandem mass spectrometry (UHPLC-ESI-MS/MS) method was used to characterize the metabolites in the active extract. The FD M. calabura leaves, extracted with 50% ethanol, is the most active extract that exhibits a high α-glucosidase and α-amylase inhibitory activities with IC50 values of 0.46 ± 0.05 and 26.39 ± 3.93 µg/mL, respectively. Sixty-one compounds were tentatively identified by using UHPLC-ESI-MS/MS from the most active extract. Quantitative analysis, by using UHPLC, revealed that geniposide, daidzein, quercitrin, 6-hydroxyflavanone, kaempferol, and formononetin were predominant compounds identified from the active extract. The results have laid down preliminary steps toward developing M. calabura leaves extract as a potential source of bioactive compounds for diabetic treatment.

scholarly journals Inhibition of Androgen Synthesis in Human Testicular and Prostatic Microsomes and in Male Rats by Novel Steroidal Compounds*

Endocrinology ◽  
1999 ◽  
Vol 140 (6) ◽  
pp. 2891-2897 ◽  
Author(s):  
Ivo P. Nnane ◽  
Katsuya Kato ◽  
Yang Liu ◽  
Brian J. Long ◽  
Qing Lu ◽  
...  
Keyword(s):  
Male Rats ◽  
Normal Male ◽  
Rat Tissues ◽  
The Novel ◽  
Androgen Synthesis ◽  
Potent Inhibition ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Wet Weight

Abstract The C17,20-lyase and 5α-reductase are key enzymes in the biosynthesis of androgens. The effects of novel steroidal compounds were evaluated as inhibitors against both human C17,20-lyase and 5α-reductase in vitro. The concentrations of testosterone (T) and dihydrotestosterone (DHT) in the prostate, testis and serum and changes in the tissue weights were also determined in rats treated with the novel inhibitors. L-12 and L-26 showed potent inhibition of human testicular C17,20-lyase with IC50 values of 50 and 25 nm, respectively. L-12, L-38, and I-47 showed moderate inhibition of human testicular C17,20-lyase with IC50 values of 75, 108, and 70 nm, respectively similar to ketoconazole (78 nm). Interestingly, L-6, L-26, and L-38 also showed some inhibitory activity against 5α-reductase with IC50 values of 75, 125, and 377 nm, respectively. Finasteride, an inhibitor of 5α-reductase had an IC50 value of 33 nm. However, ketoconazole did not inhibit 5α-reductase nor did finasteride inhibit C17,20-lyase. Treatment of normal male rats with several of these novel inhibitors (50 mg/kg·day, sc, for 14 consecutive days) caused about 45–91% decrease in serum, testicular and prostatic T concentration. Similarly, serum and prostatic DHT concentration were significantly decreased in rats treated with these novel compounds by 50–90% compared with controls. Surgical castration caused almost complete elimination of circulating T and DHT concentration in rat tissues. L-6 and L-12 were the most effective and reduced the wet weight of the prostate by 50%. Although future improvements in their bioavailability are necessary, these novel steroidal compounds show promise as potential agents for reducing T and DHT levels in patients with androgen dependent diseases.

Anti-plasmodial Effects of Zanthoxylum zanthoxyloides

Planta Medica ◽  
2019 ◽  
Vol 85 (13) ◽  
pp. 1073-1079 ◽  
Author(s):  
Christopher Dean Goodman ◽  
An Thuy Hoang ◽  
Drissa Diallo ◽  
Karl Egil Malterud ◽  
Geoffrey I. McFadden ◽  
...  
Keyword(s):  
Brine Shrimp ◽  
Methanol Extract ◽  
Stem Bark ◽  
Artemia Salina ◽  
Root Bark ◽  
Ic50 Values ◽  
Zanthoxylum Zanthoxyloides ◽  
Parasitic Activity ◽  
Resistant Strains

Abstract Zanthoxylum zanthoxyloides, syn. Fagara zanthoxyloides, is a tree growing in West Africa and is used in traditional medicine against a variety of diseases, including malaria. In the work reported here, root bark and stem bark extracts of this tree, as well as compounds isolated from the extracts, have been investigated for activity in vitro against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. In addition, toxicity against nauplii of the brine shrimp Artemia salina has been studied. Dichloromethane extracts of the root bark and stem bark, and a methanol extract of the stem bark, showed anti-parasitic activity towards chloroquine-sensitive as well as chloroquine-resistant P. falciparum, with IC50 values between 1 and 10 µg/mL. Among the isolated compounds, bis-dihydrochelerythrinyl ether, buesgenine, chelerythrine, γ-fagarine, skimmianine, and pellitorine were the most active, with IC50 values of less than 5 µg/mL. The dichloromethane extracts were toxic to brine shrimp nauplii, with LC50 values of less than 1 µg/mL. Methanol extracts were much less toxic (LC50 between 50 and 100 µg/mL). Among the isolated substances, bis-dihydrochelethrinyl ether was the most toxic (LC50 ca. 2 µg/mL).

scholarly journals Compounds from Terminalia mantaly L. (Combretaceae) Stem Bark Exhibit Potent Inhibition against Some Pathogenic Yeasts and Enzymes of Metabolic Significance

Medicines ◽  
2017 ◽  
Vol 4 (1) ◽  
pp. 6 ◽  
Author(s):  
Marthe Tchuente Tchuenmogne ◽  
Thierry Kammalac ◽  
Sebastian Gohlke ◽  
Rufin Kouipou ◽  
Abdulselam Aslan ◽  
...  
Keyword(s):  
Stem Bark ◽  
Potent Inhibition ◽  
Metabolic Significance

Cytotoxic Flavones from the Stem Bark of Bougainvillea spectabilis Willd

Planta Medica ◽  
2017 ◽  
Vol 84 (02) ◽  
pp. 129-134 ◽  
Author(s):  
Lien Do ◽  
Thammarat Aree ◽  
Pongpun Siripong ◽  
Nga Vo ◽  
Tuyet Nguyen ◽  
...  
Keyword(s):  
Cell Lines ◽  
Stem Bark ◽  
In Vitro Cytotoxicity ◽  
Crystallographic Analysis ◽  
Ionization Mass ◽  
Etoac Extract ◽  
Ic50 Values ◽  
Bougainvillea Spectabilis ◽  
Mcf 7

AbstractFive new flavones possessing a fully substituted A-ring with C-6 and C-8 methyl groups, bougainvinones I – M (1–5), along with three known congeners, 2′-hydroxydemethoxymatteucinol (6), 5,7,3′,4′-tetrahydroxy-3-methoxy-6,8-dimethylflavone (7) and 5,7,4′-trihydroxy-3-methoxy-6,8-dimethylflavone (8), were isolated from the EtOAc extract of the stem bark of Bougainvillea spectabilis. Their structures were established by means of spectroscopic data (ultraviolet, infrared, high-resolution electrospray ionization mass spectrometry, and one-dimensional and two-dimensional nuclear magnetic resonance) and single-crystal X-ray crystallographic analysis. The in vitro cytotoxicity of all isolated compounds against five cancer cell lines (KB, HeLa S-3, MCF-7, HT-29, and HepG2) was evaluated. Compound 5 showed promising cytotoxic activity against the KB and HeLa S-3 cell lines, with IC50 values of 7.44 and 6.68 µM. The other compounds exhibited moderate cytotoxicity against the KB cell line.

scholarly journals Antioxidant, anti-enzymatic, antimicrobial and cytotoxic properties of Euphorbia tirucalli L

2019 ◽  
Author(s):  
Mohammad Altamimi ◽  
Nidal Jaradat ◽  
Saad Alham ◽  
Motasem Al-Masri ◽  
Ala Bsharat ◽  
...  
Keyword(s):  
Plant Extract ◽  
Water Extract ◽  
Antioxidant Property ◽  
Pathogenic Yeast ◽  
Euphorbia Tirucalli ◽  
Mtt Method ◽  
Freeze Dried ◽  
Ic50 Values ◽  
Medicinal Properties

AbstractMedicinal properties of Euphorbia tirucalli L. have been investigated in vitro. Water extract from the plant latex was freeze dried and tested against 3 digestive enzymes and showed IC50 as 39.8±0.22, 79.43±0.38 and 316.22±0.3 for lipase, alpha- glucosidase and alpha- amylase, respectively. These results were incomparable with drugs such as acarbose and orlistat. Antioxidant property showed that the IC50 values of E. tirucalli and Trolox were 79.43±0.69 and 3.1 ±0.92 respectively. Also, the plant extract exhibited a range of antimicrobial activity against gram-positive and gram-negative bacteria and pathogenic yeast and fungi. Cytotoxicity of the plant extract tested on Caco-2 cells was determined using MTT method. The effect was linear and almost 0.5 mg/ml extract has inhibited 50% of cells relative to the control. Euphorbia tirucalli showed promising activities and is potential source of active ingredient with functional properties.

scholarly journals Flavonoids in Decorticated Sorghum Grains Exert Antioxidant, Antidiabetic and Antiobesity Activities

Molecules ◽  
2020 ◽  
Vol 25 (12) ◽  
pp. 2854 ◽  
Author(s):  
Fred Kwame Ofosu ◽  
Fazle Elahi ◽  
Eric Banan-Mwine Daliri ◽  
Su-Jung Yeon ◽  
Hun Ju Ham ◽  
...  
Keyword(s):  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Potent Inhibition ◽  
Glycation End Products ◽  
Sorghum Grains ◽  
Ic50 Values ◽  
Treatment Of Diabetes ◽  
Sorghum Grain ◽  
Diabetes And Obesity

Eight new genotypes of brown sorghum grain were decorticated and assessed for their antioxidant, antidiabetic and antiobesity activities in vitro. The DPPH and ABTS radical scavenging assays of the soluble fractions were evaluated, followed by digestive enzymes and advanced glycation end-products (AGEs) formation inhibition assays. DSOR 33 and DSOR 11 exhibited the highest DPPH (IC50 = 236.0 ± 1.98 µg/mL and 292.05 ± 2.19 µg/mL, respectively) and ABTS radical scavenging activity (IC50 = 302.50 ± 1.84 µg/mL and 317.05 ± 1.06 µg/mL, respectively). DSOR 17, DSOR 11 and DSOR 33 showed significantly higher inhibitory activity of both α-glucosidase and α-amylase (IC50 = 31.86, 35.10 and 49.40 µg/mL; and 15.87, 22.79 and 37.66 µg/mL, respectively) compared to acarbose (IC50 = 59.34 and 27.73 µg/mL, respectively). Similarly, DSOR 33, DSOR 11 and DSOR 17 showed potent inhibition of both AGEs and lipase with IC50 values of 18.25, 19.03 and 38.70 µg/mL; and 5.01, 5.09 and 4.94 µg/mL, respectively, compared to aminoguanidine (52.30 µg/mL) and orlistat (5.82 µg/mL). Flavonoids were the predominant compounds identified, with flavones being the major subclass in these three extracts. Our findings suggest that decorticated sorghum grains contain substantial amounts of flavonoids and could be promising candidates for the prevention and treatment of diabetes and obesity.

Cussonia arborea Hochst (Araliaceae): Ethnobotany, Pharmacology and Phytochemistry

2021 ◽  
Vol 14 (2) ◽  
pp. 6-10
Author(s):  
Modjinan Kayangar ◽  
N. Raymond Nono ◽  
T. Romuald Fouedjou ◽  
T. Billy Tchegnitegni ◽  
K. Beaudelaire Ponou ◽  
...  
Keyword(s):  
Short Review ◽  
Stem Bark ◽  
Published Data ◽  
Etoac Extract ◽  
Anticancer Properties ◽  
Isolation And Characterization ◽  
First Time

Background:  C. arborea belonging to Araliaceae family is used traditionally to cure many alien diseases including gonorrhoeae infection, diarrhea, malaria, and diabetes mellitus. The plant has been examined on the basis of scientific in vitro and in vivo evaluations possessing the major pharmacological activities including antimicrobial, antibacterial, antihyperglycemic,  antiplasmodial and anticancer properties. Aim of the study: In the present paper, we reported the isolation and characterization of secondary metabolites from the methanol extract of the stem bark of Cussonia arborea Hochst after a short review of the traditional and pharmacological studies done on this important medicinal plant. Materials and methods: MeOH extract of stem bark of C. arborea was suspended in water and successively extracted with EtOAc and n-BuOH. The EtOAc extract (18 g) was subjected to repeated column chromatography to yield seven (1-7) compounds. Their structures were determined by means of NMR, and published data. Results: The isolated compounds were identified as: protocatechuic acid (1), mixture of 3,23-dihydroxyolean-12-en-28-oic acid (2a) and 3,23-dihydroxyurs-12-en-28-oic acid (2b) in ratio 5/4, 3-O-β-D-xylopyranosylolean-12-en-28-oic acid (3), 3-O-α-L-arabinopyranosylolean-12-en-28-oic acid (4), β-resorcylic acid (5), mixture of 3-O-β-D-glucopyranosyl-23-hydroxyolean-12-en-28-oic acid (6a) and 3-O-β-D-glucopyranosyl-23-hydroxyurs-12-en-28-oic acid (6b) in ration 4/1, 3-O-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-3β-hydroxyolean-12-en-28-oic acid (7). Compounds 3, 4, 5, 7, 2b and 6b are herein reported for the first time in this plant

scholarly journals In vitro Studies on Antioxidant Potential of Aqueous Extract of Bridelia ferruginea Stem Bark in Brain and Liver of Wistar-albino Rats using Sodium Nitroprusside as Pro-oxidant

2020 ◽  
pp. 39-45
Author(s):  
Adesola Oluwaseun Adeleye
Keyword(s):  
Sodium Nitroprusside ◽  
Aqueous Extract ◽  
Thiobarbituric Acid ◽  
Stem Bark ◽  
Antioxidant Potential ◽  
Albino Rats ◽  
Bridelia Ferruginea ◽  
Ic50 Values ◽  
Tissue Homogenates

Thiobarbituric acid reactive species (TBARS) assay was used to study the antioxidant potential of Bridelia ferruginea, a widely used medicinal plant in Nigeria, sub-tropical Africa and parts of Asia. The aqueous extract of Bridelia ferruginea stem bark showed inhibition against the formation of TBARS induced by the pro-oxidant, sodium nitroprusside, in the liver and brain tissue homogenates of the locally bred male and female albino-Wistar rats. The inhibition of TBARS is an indication of the antioxidant potential of the plant extract. The extent of antioxidant potential depends on concentrations, showing varying degrees of inhibition with different concentrations. It showed a 54.16% inhibition in the liver and 60.65% in the brain, both at a concentration of 0.33 mg/ml, with IC50 values of 3.00 ± 1.58 mg/ml and 2.99 ± 1.59 mg/ml for the liver and brain homogenates respectively. The results suggest the effectiveness of the aqueous extract of Bridelia ferruginea stem bark in reversing the effect of lipid peroxidation that may result from sodium nitroprusside overload.

Sign in / Sign up

Export Citation Format

Share Document