scholarly journals Potent In Vitro α-Glucosidase and β-Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus (Angel’s Trumpet) Fruits

2020 ◽  
Vol 2020 ◽  
pp. 1-5
Author(s):  
Saud Bawazeer ◽  
Abdur Rauf ◽  
Sami Bawazeer
Keyword(s):  
Soluble Fraction ◽  
Precursor Protein ◽  
Chloroform Fraction ◽  
Significant Activity ◽  
Datura Metel ◽  
Angel’S Trumpet ◽  
Phytochemical Investigation ◽  
Excellent Activity ◽  
Inhibitory Potential

This study deals with α-glucosidase and β-secretase inhibitory screening of extract/fractions and isolated daturaolone (1), namely, 3-oxo-6-β-hydroxy-β-amyrin (daturaolone) from chloroform fraction of Datura metel L. Among entire fractions, the chloroform soluble fraction showed excellent activity against α-glucosidase with % inhibition 90.8 with IC50160.2±1.85 μg and daturaolone (1) with 98.7% inhibition with IC50840.4±1.74 μM, respectively. Similarly, extract and daturaolone (1) also exhibited significant activity against the β-secretase enzyme (BACE1) with % activities 88.27 and 95.19 and with IC50 values 304.21±2.98 μg and 260.70±1.87 μM, respectively, as compared to the standard inhibitor (Ans670, Sta671, Val672)-amyloid-β/A4 precursor protein 770 fragments 662-675) with % activity 94.21 and IC50 value 289.24±1.60 μM. This finding encourages and opens a new window for further detail phytochemical investigation on D. metel in order to isolate novel compounds with promising enzyme inhibitory potential.

scholarly journals EVALUATION OF ANTI-INFLAMMATORY AND ANTI-ARTHRITIC POTENTIAL OF FRACTIONS OF ECLIPTA PROSTRATA LINN

2019 ◽  
pp. 158-166
Author(s):  
HITESH MALHOTRA ◽  
MANJUSHA CHOUDHARY
Keyword(s):  
Ethyl Acetate ◽  
In Vitro Models ◽  
Chloroform Fraction ◽  
Significant Activity ◽  
Alcoholic Extract ◽  
Eclipta Prostrata ◽  
Edema Model ◽  
Anti Inflammatory

Objective: The objective of the study was to establish the anti-inflammatory and anti-arthritic potential of various fractions of Eclipta prostrata Linn. Methods: The four fractions, i.e., n-butanol, ethyl acetate, chloroform, and n-hexane from hydro-alcoholic extract were obtained. First, the fractions were evaluated through in vitro models, and then they were evaluated by in vivo anti-inflammatory model, i.e., carrageenan-induced paw edema model. Further, two active fractions were evaluated for the anti-arthritic activity using formaldehyde induced arthritis model. Results: The fractions at a dose of 100 and 200 mg/kg showed an anti-inflammatory activity, but the ethyl acetate and chloroform fraction will show maximum anti-inflammatory potential. Hence, they are further evaluated for anti-arthritic potential where they show significant activity. Conclusion: From the results, it is concluded that the ethyl acetate and chloroform fraction show significant anti-arthritic activity.

scholarly journals A New Immunosuppressive Pregnane Glycoside and Two Known Analogues from Epigynum cochinchinensis

2018 ◽  
Vol 13 (6) ◽  
pp. 1934578X1801300
Author(s):  
Yuting Shao ◽  
Yan Zhao ◽  
Hong Zhang ◽  
Mengjun Jiang ◽  
Afsar Khan ◽  
...  
Keyword(s):  
Concanavalin A ◽  
Soluble Fraction ◽  
Spectroscopic Techniques ◽  
Dependent Manner ◽  
Immunosuppressive Activity ◽  
Con A ◽  
Phytochemical Investigation ◽  
Pregnane Glycoside ◽  
Dose Dependent

Phytochemical investigation of the ethyl acetate soluble fraction from the leaves of Epigynum cochinchinensis led to the isolation of one new C21 pregnane glycoside, epigycoside C (1), along with two known analogues epigycoside A (2) and epigynoside G (3). Their structures were elucidated on the basis of extensive spectroscopic techniques. The in vitro immunosuppressive activity of compound 1 was evaluated against concanavalin A (Con A)- and lipopolysaccharides (LPS)-stimulated proliferation of mice splenocytes. Compound 1 displayed significant immunosuppressive activities in a dose-dependent manner.

scholarly journals In Vitro Antibacterial and Antifungal Potential of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus

2021 ◽  
Vol 2021 ◽  
pp. 1-5
Author(s):  
Sami Bawazeer ◽  
Abdur Rauf
Keyword(s):  
Chloroform Fraction ◽  
Bacterial Strains ◽  
Inhibitory Zone ◽  
Traditional Use ◽  
Chromatography Analysis ◽  
Antibacterial Screening ◽  
Datura Metel ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal

The aim of the present investigation was to evaluate the effect of the combined crude extract, fractions, and compound 1 isolated from the fruits of Datura metel against selected microbial (bacteria and fungi) strains. Results of antibacterial screening indicated marked susceptibility of the extract and its fractions against tested bacterial strains. Among the extract and various fractions, the chloroform fraction exhibited a significant effect against different bacterial strains including Escherichia coli, Staphylococcus aureus, and Bacillus subtilis with an inhibitory zone ranging from 18 to 24 mm. Similarly, results of antifungal activity revealed that the chloroform fraction displays a promising effect against various fungal strains. The chloroform fraction was subjected to repeated chromatography analysis, which yielded compound 1 (daturaolone). Daturaolone exhibited potent activity against selected bacterial strains including Klebsiella pneumoniae, B. subtilis, S. epidermidis, and S. aureus with an inhibitory zone ranging from 12 to 30 mm. In addition, the extracts and daturaolone exhibited significant sensitivity against T. longifusus, C. albicans, A. flavus, M. canis, F. solani, and C. glabrata. Taken all together, it is concluded that our findings validated the traditional use of D. metel to treat various infectious diseases, which is supported by daturaolone.

Antimalarial activity of the isolates from the marine sponge Hyrtios erectus against the chloroquine-resistant Dd2 strain of Plasmodium falciparum

2018 ◽  
Vol 73 (9-10) ◽  
pp. 397-400 ◽  
Author(s):  
Eunsin Ju ◽  
Abdul Latif ◽  
Chang-Suk Kong ◽  
Youngwan Seo ◽  
Yeon-Ju Lee ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Marine Sponge ◽  
Soluble Fraction ◽  
Antimalarial Activity ◽  
Spectroscopic Techniques ◽  
Significant Activity ◽  
In Vitro Screening

Abstract This work reports the isolation of the three known compounds, smenotronic acid (1), ilimaquinone (2), and pelorol (3), from the 85% methanol (MeOH)-soluble fraction of the sponge Hyrtios erectus. The structures of the isolated compounds were determined with the help of modern spectroscopic techniques, and the resulting compounds were then subjected to in vitro screening to determine their antimalarial potential against the chloroquine-resistant Dd2 strain of Plasmodium falciparum. Amongst the three compounds, pelorol (3) showed significant activity against P. falciparum with an IC50 value of 0.8 μM. For smenotronic acid (1) and ilimaquinone (2), moderate activities were observed with IC50 values of 3.51 and 2.11 μM, respectively.

An Attempt at Biological Control of Blossom Blight of Rose Caused by Botrytis cinerea Using some Local Trichoderma spp. Strains

2020 ◽  
Vol 55 (1) ◽  
pp. 27-34
Author(s):  
G. Zadehdabagh ◽  
K. Karimi ◽  
M. Rezabaigi ◽  
F. Ajamgard
Keyword(s):  
Botrytis Cinerea ◽  
Mycelial Growth ◽  
Limiting Factor ◽  
Dual Culture ◽  
Trichoderma Spp ◽  
Khuzestan Province ◽  
Inhibitory Potential ◽  
Cut Rose

The northern of Khuzestan province in Iran is mainly considered as one of the major areas of miniature rose production. Blossom blight caused by Botrytis cinerea has recently become a serious limiting factor in rose production in pre and post-harvest. In current study, an attempt was made to evaluate the inhibitory potential of some local Trichoderma spp. strains against B. cinerea under in vitro and in vivo conditions. The in vitro results showed that all Trichoderma spp. strains were significantly able to reduce the mycelial growth of the pathogen in dual culture, volatile and non-volatile compounds tests compared with control, with superiority of T. atroviride Tsafi than others. Under in vivo condition, the selected strain of T. atroviride Tsafi had much better performance than T. harzianum IRAN 523C in reduction of disease severity compared with the untreated control. Overall, the findings of this study showed that the application of Trichoderma-based biocontrol agents such as T. atroviride Tsafi can be effective to protect cut rose flowers against blossom blight.

Drug Design of Inhibitors of Alzheimer’s Disease (AD): POM and DFT Analyses of Cholinesterase Inhibitory Activity of β-amino di-Carbonyl Derivatives

2019 ◽  
Vol 19 (8) ◽  
pp. 688-705
Author(s):  
Taibi Ben Hadda ◽  
Abdur Rauf ◽  
Hsaine Zgou ◽  
Fatma Sezer Senol ◽  
Ilkay Erdogan Orhan ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Cholinesterase Inhibitors ◽  
Metal Accumulation ◽  
Microtiter Plate ◽  
Metal Chelation ◽  
Carbonyl Derivatives ◽  
Cholinesterase Inhibitory Activity ◽  
Inhibitory Potential

Background:Since deficit of acetylcholine has been evidenced in the Alzheimer’s disease (AD) patients, cholinesterase inhibitors are currently the most specified drug category for the remediation of AD.Method:In the present study, 16 compounds (1-16) with dicarbonyl skeletons have been synthesized and tested for their inhibitory potential in vitro against AChE and BChE using ELISA microtiter plate assays at 100 μg/mL. Since metal accumulation is related to AD, the compounds were also tested for their metal-chelation capacity.Results and Conclusion:All the investigated dicarbonyl compounds exerted none or lower than 30% inhibition against both cholinesterases, whereas compounds 2, 8 and 11 showed 37, 42, 41% of inhibition towards BChE, being the most active. The highest metal-chelation capacity was observed with compound 8 (53.58 ± 2.06%). POM and DFT analyses are in good harmonization with experimental data.

In Vitro, In Silico and Ex Vivo Studies of Dihydroartemisinin Derivatives as Antitubercular Agents

2019 ◽  
Vol 19 (8) ◽  
pp. 633-644 ◽  
Author(s):  
Komal Kalani ◽  
Sarfaraz Alam ◽  
Vinita Chaturvedi ◽  
Shyam Singh ◽  
Feroz Khan ◽  
...  
Keyword(s):  
Bone Marrow ◽  
In Silico ◽  
Ex Vivo ◽  
Virulent Strain ◽  
Infection Model ◽  
Mouse Bone Marrow ◽  
Significant Activity ◽  
Macrophage Infection ◽  
In Silico Studies

Introduction: As a part of our drug discovery program for anti-tubercular agents, dihydroartemisinin (DHA-1) was screened against Mtb H37Rv, which showed moderate anti-tubercular activity (>25.0 µg/mL). These results prompted us to carry out the chemical transformation of DHA-1 into various derivatives and study their antitubercular potential. Materials and Methods: DHA-1 was semi-synthetically converted into four new acyl derivatives (DHA-1A – DHA-1D) and in-vitro evaluated for their anti-tubercular potential against Mycobacterium tuberculosis H37Rv virulent strain. The derivatives, DHA-1C (12-O-(4-nitro) benzoyl; MIC 12.5 µg/mL) and DHA-1D (12-O-chloro acetyl; MIC 3.12µg/mL) showed significant activity against the pathogen. Results: In silico studies of the most active derivative (DHA-1D) showed interaction with ARG448 inhibiting the mycobacterium enzymes. Additionally, it showed no cytotoxicity towards the Vero C1008 cells and Mouse bone marrow derived macrophages. Conclusion: DHA-1D killed 62% intracellular M. tuberculosis in Mouse bone marrow macrophage infection model. To the best of our knowledge, this is the first-ever report on the antitubercular potential of dihydroartemisinin and its derivatives. Since dihydroartemisinin is widely used as an antimalarial drug; these results may be of great help in anti-tubercular drug development from a very common, inexpensive, and non-toxic natural product.

Computational Evaluation and In Vitro Validation of New Epidermal Growth Factor Receptor Inhibitors

2020 ◽  
Vol 20 (18) ◽  
pp. 1628-1639
Author(s):  
Sergi Gómez-Ganau ◽  
Josefa Castillo ◽  
Andrés Cervantes ◽  
Jesus Vicente de Julián-Ortiz ◽  
Rafael Gozalbes
Keyword(s):  
Cell Proliferation ◽  
Epidermal Growth Factor Receptor ◽  
Growth Factor ◽  
Epidermal Growth Factor ◽  
Binding Affinity ◽  
Cell Lines ◽  
Growth Factor Receptor ◽  
Significant Activity ◽  
Epidermal Growth

Background: The Epidermal Growth Factor Receptor (EGFR) is a transmembrane protein that acts as a receptor of extracellular protein ligands of the epidermal growth factor (EGF/ErbB) family. It has been shown that EGFR is overexpressed by many tumours and correlates with poor prognosis. Therefore, EGFR can be considered as a very interesting therapeutic target for the treatment of a large variety of cancers such as lung, ovarian, endometrial, gastric, bladder and breast cancers, cervical adenocarcinoma, malignant melanoma and glioblastoma. Methods: We have followed a structure-based virtual screening (SBVS) procedure with a library composed of several commercial collections of chemicals (615,462 compounds in total) and the 3D structure of EGFR obtained from the Protein Data Bank (PDB code: 1M17). The docking results from this campaign were then ranked according to the theoretical binding affinity of these molecules to EGFR, and compared with the binding affinity of erlotinib, a well-known EGFR inhibitor. A total of 23 top-rated commercial compounds displaying potential binding affinities similar or even better than erlotinib were selected for experimental evaluation. In vitro assays in different cell lines were performed. A preliminary test was carried out with a simple and standard quick cell proliferation assay kit, and six compounds showed significant activity when compared to positive control. Then, viability and cell proliferation of these compounds were further tested using a protocol based on propidium iodide (PI) and flow cytometry in HCT116, Caco-2 and H358 cell lines. Results: The whole six compounds displayed good effects when compared with erlotinib at 30 μM. When reducing the concentration to 10μM, the activity of the 6 compounds depends on the cell line used: the six compounds showed inhibitory activity with HCT116, two compounds showed inhibition with Caco-2, and three compounds showed inhibitory effects with H358. At 2 μM, one compound showed inhibiting effects close to those from erlotinib. Conclusion: Therefore, these compounds could be considered as potential primary hits, acting as promising starting points to expand the therapeutic options against a wide range of cancers.

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