scholarly journals EVALUATION OF α-GLUCOSIDASE INHIBITORY POTENTIAL OF METHANOLIC LEAF EXTRACT OF OCIMUM CANUM

2018 ◽  
Vol 10 (1) ◽  
pp. 126
Author(s):  
Kumari Smita
Keyword(s):  
High Performance ◽  
Leaf Extract ◽  
Soxhlet Extraction ◽  
Inhibitory Effect ◽  
Polyphenolic Compounds ◽  
Glucosidase Activity ◽  
Glucosidase Inhibitors ◽  
Vitro Model ◽  
Inhibitory Potential

Objective: The present investigation was designed to study the inhibitory effects of methanolic leaf extract of Ocimum canum (O. canum) on α-glucosidase using in vitro model followed by an assessment of bioactive compounds.Methods: The methanolic leaf extract was prepared by Soxhlet extraction method and partially purified by thin layer chromatography (TLC). Each band was subjected to α-glucosidase inhibition study. The positive bands were further characterized by high-performance liquid chromatography (HPLC) and quadrupole time of flight (Q-TOF) micro mass spectrometer.Results: Out of the several combinations of solvent systems, toluene, ethyl acetate and formic acid combination in the ratio of 7:2:1 revealed 5 bands on the TLC sheet. Among all the TLC bands, 2 bands (band A and B) showed the significant inhibitory effect on α-glucosidase activity. HPLC analysis of band A and B revealed the presence of two important polyphenolic compounds, namely rosmarinic acid (RA) and ursolic acid (UA). Q-TOF micromass spectrometer analysis revealed the percentage availability of RA, caffeic acid, tartaric acid, quercetin and other polyphenolic components in the bioactive bands.Conclusion: The study revealed that methanolic leaf extract of O. canum exhibits potent inhibition of α-glucosidase activity. Inhibition of α-glucosidase activity might be attributed to the presence of the polyphenolic compounds like RA and UA. Therefore, this finding can lead to the development of natural α-glucosidase inhibitors by the O. canum leaf extract.

scholarly journals In-vitro Antivenom Potential of Solanum dasyphyllum Methanolic Leaf and Fruit Extracts against Naja nigricollis Venom

2020 ◽  
pp. 38-45
Author(s):  
Adewunmi Rofiat Funmilola ◽  
Gidado Abubakar ◽  
Zanna Hassan
Keyword(s):  
Medicinal Plants ◽  
Leaf Extract ◽  
Inhibitory Effect ◽  
Fruit Extract ◽  
Southwestern Part ◽  
Fruit Extracts ◽  
Snake Envenomation ◽  
The Family ◽  
Inhibitory Potential

Solanum dasyphyllum belongs to the family of plants called Solanaceae, it is commonly called "Africa eggplant" and one of the medicinal plants used in the treatment of snake envenomation in the southwestern part of Nigeria, but investigation concerning its anti-venom activity has not been established. The present study evaluates the in-vitroenzyme inhibition potential of S.dasyphyllum leaf and fruit extracts against Naja nigricollis (Black-necked spitting cobra) venom. The inhibitory potential of S. dasyphyllum leaf and fruit on proteases, acetylcholinesterase, phospholipase A2 and hyaluronidase enzymes present in the snake venom was evaluated. The methanolic leaf and fruit extracts of S. dasyphyllum inhibited the activity of all enzymes evaluated, however, the leaf extract exhibited better enzyme inhibitory effect on N. nigricollis venom when compared with the fruit. This could be due to the presence of various phytochemicals in leaf and fruit extract.  This result substantiates the ethnomedicinal usage of S. dasyphyllum and would help to develop potent antidote therapy against N. nigricollis envenomation.

scholarly journals INHIBITORY EFFECT OF A STANDARDIZED HYDROETHANOLIC EXTRACT OF TERMINALIA ARJUNA BARK ON ALPHA-AMYLASE ENZYMEINHIBITORY EFFECT OF A STANDARDIZED HYDROETHANOLIC EXTRACT OF TERMINALIA ARJUNA BARK ON ALPHA-AMYLASE ENZYME

2018 ◽  
Vol 11 (4) ◽  
pp. 366 ◽  
Author(s):  
Sushant A Shengule ◽  
Sanjay Mishra ◽  
Shweta Bodhale
Keyword(s):  
Inhibitory Activity ◽  
High Performance ◽  
Soxhlet Extraction ◽  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Antidiabetic Activity ◽  
Bark Extract ◽  
Terminalia Arjuna ◽  
Hydroethanolic Extract

 Objective: The present study was initiated to screen the hydroethanolic bark extract for α-amylase inhibitory activity and standardization of the Terminalia arjuna for polyphenolic phytochemicals using high-performance liquid chromatography-photo diode array (HPLC-PDA) method.Methods: The T. arjuna bark sample was extracted with ethanol: water (70:30 v/v) using Soxhlet extraction. A Dionex P680 HPLC system was used to acquire chromatograms. The screening of extract of T. arjuna bark has performed for in vitro α-amylase inhibitory assay. Each experiment was repeated 3 times. All values were expressed mean ± standard deviation.Results: The content of arjunetin, arjungenin, gallic acid, ellagic acid, and quercetin was 0.47, 8.22, 2.443, 7.901, and 3.20 mg/g, respectively, in a hydroethanolic extract of T. arjuna. The hydroethanolic extract of T. arjuna bark and acarbose has shown an inhibitory activity with an IC50 value 145.90 and 62.35 μg/mL, respectively.Conclusion: The hydroethanolic extract T. arjuna bark demonstrates α-amylase inhibitory activity due to a synergistic effect of the phytochemical constituents present in it. This study suggests that one of the mechanisms of this plant for antidiabetic activity is through the inhibition of α-amylase enzyme.

scholarly journals Evaluation of cannabidiol’s inhibitory effect on alpha-glucosidase and its stability in simulated gastric and intestinal fluids

2021 ◽  
Vol 3 (1) ◽  
Author(s):  
Hang Ma ◽  
Huifang Li ◽  
Chang Liu ◽  
Navindra P. Seeram
Keyword(s):  
Molecular Docking ◽  
High Performance ◽  
Inhibitory Effect ◽  
In Vitro Assays ◽  
Inhibitory Effects ◽  
In Vivo Models ◽  
Glucosidase Activity ◽  
Intestinal Fluids

Abstract Objective Cannabidiol (CBD) has been reported to have anti-diabetic effects in pre-clinical and clinical studies but its inhibitory effects on α-glucosidase, a carbohydrate hydrolyzing enzyme, remain unknown. Herein, we evaluated CBD’s inhibitory effects on α-glucosidase using in vitro assays and computational studies. Methods CBD’s inhibitory effect on α-glucosidase activity was evaluated in a yeast enzymatic assay and by molecular docking. The stability of CBD in simulated gastric and intestinal fluids was evaluated by high-performance liquid chromatography analyses. Results CBD, at 10, 19, 38, 76, 152, 304, 608, and 1216 μM, inhibited α-glucosidase activity with inhibition of 17.1, 20.4, 48.1, 56.6, 59.1, 63.7, 74.1, and 95.4%, respectively. Acarbose, the positive control, showed a comparable inhibitory activity (with 85.1% inhibition at 608 μM). CBD’s inhibitory effect on α-glucosidase was supported by molecular docking showing binding energy (-6.39 kcal/mol) and interactions between CBD and the α-glucosidase protein. CBD was stable in simulated gastric and intestinal fluids for two hours (maintained ≥ 90.0%). Conclusions CBD showed moderate inhibitory effect against yeast α-glucosidase activity and was stable in gastric and intestinal fluids. However, further studies on CBD’s anti-α-glucosidase effects using cellular and in vivo models are warranted to support its potential application for the management of type II diabetes mellitus.

EVALUATION OF IN VITRO ALPHA-AMYLASE AND ALPHA-GLUCOSIDASE INHIBITORY POTENTIAL OF ROOTS OF EUPHORBIA HIRTA LINN.

2020 ◽  
Vol 7 (8) ◽  
pp. 18-23
Keyword(s):  
Inhibitory Effect ◽  
Alpha Amylase ◽  
Root Extract ◽  
Alcoholic Extract ◽  
Traditional Use ◽  
Euphorbia Hirta ◽  
Vitro Model ◽  
Inhibitory Potential ◽  
Alpha Glucosidase

Aim: The present study was designed to investigate the in vitro inhibitory potential of Euphorbia hirta root extract on alpha-amylase and alpha glucosidase enzymes. Materials and Methods: Alcoholic extract of Euphorbia hirta was subjected to inhibitory effect of alpha-amylase and alpha-glucosidase using specific standard in vitro procedure. Results: The results revealed that extract successfully inhibited the activity of both enzymes in an in vitro model. The alcoholic root extract of Euphorbia hirta inhibited the alpha amylase and alpha glucosidase enzymes as 79.73 ± 0.18% and 81.35 ± 0.12% respectively. Conclusion: The present study showed that, the alcoholic extract showed a significant inhibitory effect on alpha amylase and alpha glucosidase enzymes, thus validating the traditional use of the plant.

scholarly journals Antimicrobial Activity of Pinus Wallachiana Against Fusarium Oxysporum f. sp. Cubense and Analysis of its Fractions by HPLC

2021 ◽  
Author(s):  
Qurat Ul Ain ◽  
Shahzad Asad ◽  
Karam Ahad ◽  
Muhammad Naeem Safdar ◽  
Atif Jamal
Keyword(s):  
Antimicrobial Activity ◽  
Fusarium Oxysporum ◽  
High Performance ◽  
Leaf Extract ◽  
Ethyl Acetate Fraction ◽  
Severity Index ◽  
Inhibitory Effect ◽  
Butanol Fraction ◽  
Greenhouse Experiments

Abstract Fusarium wilt has ruined banana production and poses a major threat to its industry because of highly virulent Fusarium oxysporum f. sp. cubense (Foc) race 4. The present study focused on the efficacy of Pinus wallachiana and its organic fractions against Foc in in vitro and greenhouse experiments. The presence of polyphenols in the fractions was also investigated using High Performance Liquid Chromatography (HPLC). The in vitro tests carried out for the leaf extract of P. wallachiana showed its inhibitory effect on the mycelial growth and based on this evidence, further characterization of fractions were done. Complete mycelial inhibition and the highest zone of inhibition against Foc was observed for the n-butanol fraction in vitro, while the n-hexane and dichloromethane fractions showed lower disease severity index (DSI) in greenhouse experiments. The fractions were further analysed by HPLC using nine polyphenolic standards, namely quercitin, myrecitin, kaempferol, rutin, gallic acid, trans-ferulic acid, coumeric acid, epicatechin and catechin. The highest content of polyphenols, based on standards used, was quantified in the n-butanol fraction followed by the ethyl acetate fraction of the leaf extract. This is the first report of antimicrobial activity of Pinus wallachiana against Foc to the best of our knowledge.

scholarly journals Delivery of Thyronamines (TAMs) to the Brain: A Preliminary Study

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1616
Author(s):  
Nicoletta di Leo ◽  
Stefania Moscato ◽  
Marco Borso' ◽  
Simona Sestito ◽  
Beatrice Polini ◽  
...  
Keyword(s):  
High Performance ◽  
In Vitro Model ◽  
New Drugs ◽  
Therapeutic Approaches ◽  
Neuroprotective Effects ◽  
Pharmacological Response ◽  
Preliminary Study ◽  
Vitro Model ◽  
The Brain

Recent reports highlighted the significant neuroprotective effects of thyronamines (TAMs), a class of endogenous thyroid hormone derivatives. In particular, 3-iodothyronamine (T1AM) has been shown to play a pleiotropic role in neurodegeneration by modulating energy metabolism and neurological functions in mice. However, the pharmacological response to T1AM might be influenced by tissue metabolism, which is known to convert T1AM into its catabolite 3-iodothyroacetic acid (TA1). Currently, several research groups are investigating the pharmacological effects of T1AM systemic administration in the search of novel therapeutic approaches for the treatment of interlinked pathologies, such as metabolic and neurodegenerative diseases (NDDs). A critical aspect in the development of new drugs for NDDs is to know their distribution in the brain, which is fundamentally related to their ability to cross the blood–brain barrier (BBB). To this end, in the present study we used the immortalized mouse brain endothelial cell line bEnd.3 to develop an in vitro model of BBB and evaluate T1AM and TA1 permeability. Both drugs, administered at 1 µM dose, were assayed by high-performance liquid chromatography coupled to mass spectrometry. Our results indicate that T1AM is able to efficiently cross the BBB, whereas TA1 is almost completely devoid of this property.

Aqueous extracts of avocado pear (Persea americana Mill.) leaves and seeds exhibit anti-cholinesterases and antioxidant activities in vitro

2016 ◽  
Vol 27 (2) ◽  
Author(s):  
Ganiyu Oboh ◽  
Veronica O. Odubanjo ◽  
Fatai Bello ◽  
Ayokunle O. Ademosun ◽  
Sunday I. Oyeleye ◽  
...  
Keyword(s):  
Leaf Extract ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Inhibitory Effect ◽  
Seed Extract ◽  
Persea Americana ◽  
Dependent Manner ◽  
Natural Treatment

AbstractAvocado pear (The inhibitory effects of extracts on AChE and BChE activities and antioxidant potentials (inhibition of FeThe extracts inhibited AChE and BChE activities and prooxidant-induced TBARS production in a dose-dependent manner, with the seed extract having the highest inhibitory effect and the leaf extract exhibiting higher phenolic content and radical scavenging abilities, but lower Fe chelation ability compared with that of the seed. The phytochemical screening revealed the presence of saponins, alkaloids, and terpenoids in both extracts, whereas the total alkaloid profile was higher in the seed extract than in the leaf extract, as revealed by GC-FID.The anti-cholinesterase and antioxidant activities of avocado leaf and seed could be linked to their phytoconstituents and might be the possible mechanisms underlying their use as a cheap and natural treatment/management of AD. However, these extracts should be further investigated in vivo.

scholarly journals Perbandingan Daya Hambat Larutan Antiseptik Povidone iodine dengan Ekstrak Daun Sirih terhadap Candida albicans secara In Vitro

2015 ◽  
Vol 4 (3) ◽  
Author(s):  
Septriana Putri ◽  
Aziz Djamal ◽  
Rahmatini Rahmatini ◽  
Cimi Ilmiawati
Keyword(s):  
Candida Albicans ◽  
Leaf Extract ◽  
Vaginal Discharge ◽  
Povidone Iodine ◽  
Inhibitory Effect ◽  
Iodine Solution ◽  
Betel Leaf ◽  
Post Hoc ◽  
Povidone Iodine Solution

Abstrak Candida albicansb (C. albicans) adalah salah satu mikroorganisme penyebab masalah kesehatan reproduksi wanita, yaitu keputihan (fluor albus). Penggunaan larutan povidone iodine dan bahan alam seperti ekstrak daun sirih menjadi pilihan masyarakat sebagai pembersih alat kewanitaan. Tujuan penelitian ini adalah untuk membandingkandaya hambat larutan antiseptik povidone iodine dan ekstrak daun sirih terhadap jamur C. albicans secara in vitro. Penelitian dilakukan terhadap lima isolat jamur C. albicans dengan larutan kontrol akuades.Perlakuan terdiri dari povidone iodine, ekstrak daun sirih dengan konsentrasi 5%, 10%, dan 20%.Hasil penelitian menunjukkan bahwa povidone iodine memiliki daya hambat terhadap C. albicans. Ekstrak daun sirih dengan konsentrasi 5% dan 10% tidak memiliki daya hambat terhadap C. albicans, namun ekstrak daun sirih konsentrasi 20% memiliki daya hambat terhadap C. albicans. Analisis statistik dengan uji ANOVA yang dilanjutkan dengan uji Post-hoc menunjukkan perbedaan bermakna antara daya hambat larutan povidone iodine dan ekstrak daun sirih 20% terhadap kontrol(p < 0.05).Larutan povidone iodine memiliki daya hambat dua kali lebih besar terhadap pertumbuhan C. albicans dibandingkan ekstrak daun sirih 20%. Dari penelitian ini dapat disimpulkan bahwa larutan povidone iodine dan ekstrak daun sirih 20% dapat menghambat pertumbuhan jamur C. albicans secara in vitro. Kata kunci: povidone iodine, ekstrak daun sirih, Candida albicansAbstract Candida albicans (C. albicans) is one of the frequent causes of  reproductive health problems in women, namely vaginal discharge (fluor albus). The antiseptic solution, povidone iodine, is still an option to overcome vaginal discharge. The use of natural materials such as betel (Piper betle L.) leaves extract also become a popular choice as adouche for women. The objective of this study was to compare the inhibitory activity of povidone iodine solution and betel leaf extract against the growth of C. albicans in vitro. We used five different isolates of C. albicans with distilled water as control. Each isolate was treated with povidone iodine solution, betel leaf extract at concentration of 5%, 10%,and 20%. The results showed that povidone iodine had inhibitory effect on C. albicans. Betel leaf extract at concentration of 5% and 10% did not have inhibitory effectwhile betel leaf extract at concentration of 20% hadinhibitory effect on C. albicans. Analysis by ANOVA followed by Post-hoc tests showed a significant difference in inhibitory activity of povidone iodine and betel leaf extract at 20% concentration compared to control (p < 0,05). Povidone iodine solution showed twice as much as inhibitory effect on C. albicans compared to betel leaf extract (20% concentration). It is concluded that povidone iodine solution and betel leaf extract at 20% concentration can inhibit the growth of C. albicans in vitro.Keywords: povidone iodine, betel leaf extract, Candida albicans

In vitro inhibitory effects of glucosamine, chondroitin and diacerein on human hepatic CYP2D6

2021 ◽  
Vol 36 (4) ◽  
pp. 259-270
Author(s):  
Boon Hooi Tan ◽  
Nafees Ahemad ◽  
Yan Pan ◽  
Uma Devi Palanisamy ◽  
Iekhsan Othman ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
High Performance ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Time Curve ◽  
Clinical Drugs ◽  
Inhibition Potencies ◽  
P450 2D6

Abstract Objectives Glucosamine, chondroitin and diacerein are natural compounds commonly used in treating osteoarthritis. Their concomitant intake may trigger drug–natural product interactions. Cytochrome P450 (CYP) has been implicated in such interactions. Cytochrome P450 2D6 (CYP2D6) is a major hepatic CYP involved in metabolism of 25% of the clinical drugs. This study aimed to investigate the inhibitory effect of these antiarthritic compounds on CYP2D6. Methods CYP2D6 was heterologously expressed in Escherichia coli. CYP2D6–antiarthritic compound interactions were studied using in vitro enzyme kinetics assay and molecular docking. Results The high-performance liquid chromatography (HPLC)-based dextromethorphan O-demethylase assay was established as CYP2D6 marker. All glucosamines and chondroitins weakly inhibited CYP2D6 (IC50 values >300 µM). Diacerein exhibited moderate inhibition with IC50 and K i values of 34.99 and 38.27 µM, respectively. Its major metabolite, rhein displayed stronger inhibition potencies (IC50=26.22 μM and K i =32.27 μM). Both compounds exhibited mixed-mode of inhibition. In silico molecular dockings further supported data from the in vitro study. From in vitro–in vivo extrapolation, rhein presented an area under the plasma concentration-time curve (AUC) ratio of 1.5, indicating low potential to cause in vivo inhibition. Conclusions Glucosamine, chondroitin and diacerein unlikely cause clinical interaction with the drug substrates of CYP2D6. Rhein, exhibits only low potential to cause in vivo inhibition.

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