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 Demonstration of Phytochemicals and In-vitro Antioxidant and Anti-inflammatory activity by methanolic extract of Elettaria cardamomum

2020 ◽  
Vol 3 (3) ◽  
pp. 01-04
Author(s):  
Md. Shahidul Islam
Keyword(s):  
Methanolic Extract ◽  
Research Work ◽  
Inflammatory Activity ◽  
Pharmacological Activities ◽  
Elettaria Cardamomum ◽  
Ic50 Values ◽  
Phytochemical Profile ◽  
Anti Inflammatory ◽  
Dpph Scavenging

The existing research study attempts to untie novel avenues for development of the medicinal exercises of Elettaria cardamomum, fashionable known as the “Queen of Spices” and locally recognized as “elaichi”. Its seeds are utilized as abortifacient, acrid, alexiteric, aromatic, sweet, cardiac tonic, cooling, carminative, digestive, diuretic, expectorant, stimulant and also tonic beneficial in the asthma, haemorrhoids, bronchitis, strangury, renal in addition to vesical calculi, anorexia, halitosis, gastropathy dyspepsia as well as burning sensation. The prime goal of this research work is to evaluate antioxidant as well as anti-inflammatory properties of the traditional Bangladeshi medicinal extracts in addition to examine these activities. The aim in present work was to screen the phytochemical profile as well as pharmacological activities of the methanolic extract of this plant’s leaves. To explore pharmacological actions DPPH scavenging test and the HRBC membrane stabilization techniques were done for the antioxidant and also anti-inflammatory test respectively. The pharmacological works revealed that plant extracts might have noteworthy antioxidant effect which is possibly mediated by the inhibition of DPPH free radical which is accountable for oxidation. The IC50 values by the DPPH scavenging test observed for the standard and the leaves were 106.38µg/ml & 594.47µg/ml respectively. There is also moderate anti-inflammatory activity. The IC50 values for anti-inflammatory activity by standard & leaves were 35.04µg/ml and 944.0 µg/ml respectively.

scholarly journals Phytotherapy: Herbal medicine in the management of Diabetes mellitus

2017 ◽  
Vol 4 (4) ◽  
pp. 161-165
Author(s):  
Twinkle Sunder Bansode ◽  
B K Salalkar
Keyword(s):  
Maximum Effect ◽  
Syzygium Cumini ◽  
Terminalia Chebula ◽  
Salvadora Persica ◽  
Antidiabetic Agents ◽  
Synthetic Drugs ◽  
Wide Range ◽  
Phytochemical Profile

Despite considerable progress in the treatment of the diabetes with synthetic drugs, the search for effective, safe and inexpensive drugs is ongoing from herbs, since they offer a wide range of antidiabetic agents. Antidiabetic studies using in silico, in vitro and in vivo aspect of different medicinal plant products (Trigonella foenum-graecum, seeds; Syzygium cumini, seeds; Salvadora persica, leaves and Terminalia chebula, seeds) were reviewed. The objective of the study was to compare these medicinal plants for their hypoglycemic effect and phytochemical composition in order to find out most feasible and efficient antidiabetic agent. In this regard, the article is going to look at the phytochemical profile and the antihyperglycaemic properties and toxicity studies of the various fractions isolated from these plants. Studies claimed that all crude as well as partially purified fractions showed an antidiabetic effect hence are potent antidiabetic agents, but maximum effect observed in case of fraction isolated from Syzygium cumini and Salvadora persica.

scholarly journals In-Vitro α-Glucosidase Inhibitory Activities of Muntingia Calabura Linn.

2019 ◽  
Vol 7 (4.14) ◽  
pp. 183 ◽  
Author(s):  
N I.I. Nor Azman ◽  
N Hashim ◽  
R Ahmad
Keyword(s):  
Type 2 Diabetes ◽  
Diabetes Type 2 ◽  
Postprandial Hyperglycemia ◽  
Glucosidase Inhibitors ◽  
Biological Studies ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Muntingia Calabura

Muntingia calabura Linn. also known locally as “ceri kampung” is a plant of the family Elaeocarpaceae. The plant has been reported to possess several medicinal properties including reducing high blood pressure, lowering cholesterol level and controlling Type 2 diabetes. Type 2 diabetes is usually related to postprandial hyperglycemia, which is related to the rise of blood sugar level after a meal. This condition can be controlled by α-glucosidase inhibitors which inhibit the enzyme from catalyzing the liberation of glucose from carbohydrates in the digestive tract. Despite many biological studies reported for the plant, its antidiabetic potential has not been widely explored. Thus the aim of this study was to find potential α-glucosidase inhibitors from 16 extracts of M. calabura as a therapeutic approach in decreasing postprandial hyperglycemia. The hexane (Hx), ethyl acetate (Ea), 75% ethanol (Et) and aqueous (Aq) extracts of four parts (fruit, leaf, stem and root) of M. calabura (collected from Bangi, Selangor) were screened for their a-glucosidase inhibitory activities at 50.00, 25.00, 12.50, 6.25, 3.13, 1.56 and 0.78 ppm prepared via two-fold serial dilution against the positive control, acarbose. The aqueous leaf (AqL) and root extracts (AqR) exhibited very strong activities with IC50 values of 0.15 and 0.41 µg/ml  while the other extracts showed strong to moderately strong activities with IC50 values ranging from 1.83-11.66  µg/ml against acarbose (4.3 µg/ml). 

scholarly journals Chemical Group Profiling, In Vitro and In Silico Evaluation of Aristolochia ringens on α-Amylase and α-Glucosidase Activity

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
J. B. Ahmad ◽  
E. O. Ajani ◽  
S. Sabiu
Keyword(s):  
In Silico ◽  
Inhibitory Effect ◽  
Root Extract ◽  
Asiatic Acid ◽  
Standard Drug ◽  
Synthetic Drugs ◽  
Ic50 Values ◽  
Hypoglycaemic Agent

Diabetes mellitus (DM) has become a global scourge, and there is a continuous search for novel compounds as viable alternatives to synthetic drugs which are often accompanied by severe adverse effects. Aristolochia ringens is among the scientifically implicated botanicals effective in the management of several degenerative diseases including DM. The current study evaluated the inhibitory mechanism(s) of root extract of A. ringens on α-amylase and α-glucosidase in vitro and in silico, while its constituents were characterized using liquid chromatography-mass spectrometric technique. The extract had concentration-dependent inhibitory effect on the study enzymes, and the inhibition compared well with that of standard drug (acarbose) with respective IC50 values of 0.67 mg/mL (α-amylase) and 0.57 mg/mL (α-glucosidase) compared with that of the extract (0.63 and 0.54 mg/mL). The extract competitively and uncompetitively inhibited α-amylase and α-glucosidase, respectively. Of the identified compounds, dianoside G (−12.4, −12.5 kcal/mol) and trilobine (−10.0, −10.0 kcal/mol) had significant interactions with α-amylase and α-glucosidase, respectively, while magnoflorine and asiatic acid also interacted keenly with both enzymes, with quercetin 3-O-glucuronide and strictosidine showing better affinity towards α-glucosidase. These observations are suggestive of involvement of these compounds as probable ligands contributing to antidiabetic potential of the extract. While studies are underway to demystify the yet to be identified compounds in the extract, the data presented have lent scientific credence to the acclaimed in vivo antidiabetic potential of the extract and suggested it as a viable source of oral hypoglycaemic agent.

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.

Chickpea (Cicer arietinum L.) Lectin Exhibit Inhibition of ACE-I, α-amylase and α-glucosidase Activity

2019 ◽  
Vol 26 (7) ◽  
pp. 494-501 ◽  
Author(s):  
Sameer Suresh Bhagyawant ◽  
Dakshita Tanaji Narvekar ◽  
Neha Gupta ◽  
Amita Bhadkaria ◽  
Ajay Kumar Gautam ◽  
...  
Keyword(s):  
Biological Effects ◽  
Exchange Chromatography ◽  
Health Concern ◽  
Carbohydrate Binding ◽  
Dependent Manner ◽  
Concentration Dependent Manner ◽  
Ic50 Values ◽  
Chickpea Lectin

Background: Diabetes and hypertension are the major health concern and alleged to be of epidemic proportions. This has made it a numero uno subject at various levels of investigation. Glucosidase inhibitor provides the reasonable option in treatment of Diabetes Mellitus (DM) as it specifically targets post prandial hyperglycemia. The Angiotensin Converting Enzyme (ACE) plays an important role in hypertension. Therefore, inhibition of ACE in treatment of elevated blood pressure attracts special interest of the scientific community. Chickpea is a food legume and seeds contain carbohydrate binding protein- a lectin. Some of the biological properties of this lectin hitherto been elucidated. Methods: Purified by ion exchange chromatography, chickpea lectin was tested for its in vitro antioxidant, ACE-I inhibitory and anti-diabetic characteristic. Results: Lectin shows a characteristic improvement over the synthetic drugs like acarbose (oral anti-diabetic drug) and captopril (standard antihypertensive drug) when, their IC50 values are compared. Lectin significantly inhibited α-glucosidase and α-amylase in a concentration dependent manner with IC50 values of 85.41 ± 1.21 ҝg/ml and 65.05 ± 1.2 µg/ml compared to acarbose having IC50 70.20 ± 0.47 value of µg/ml and 50.52 ± 1.01 µg/ml respectively. β-Carotene bleaching assay showed antioxidant activity of lectin (72.3%) to be as active as Butylated Hydroxylanisole (BHA). In addition, lectin demonstrated inhibition against ACE-I with IC50 value of 57.43 ± 1.20 µg/ml compared to captopril. Conclusion: Lectin demonstrated its antioxidant character, ACE-I inhibition and significantly inhibitory for α-glucosidase and α-amylase seems to qualify as an anti-hyperglycemic therapeutic molecule. The biological effects of chickpea lectin display potential for reducing the parameters of medically debilitating conditions. These characteristics however needs to be established under in vivo systems too viz. animals through to humans.

Synthetic and semi-synthetic drugs as promising therapeutic option for the treatment of COVID-19

2020 ◽  
Vol 20 ◽  
Author(s):  
Ekta Shirbhate ◽  
Preeti Patel ◽  
Vijay K Patel ◽  
Ravichandran Veerasamy ◽  
Prabodh C Sharma ◽  
...  
Keyword(s):  
Therapeutic Option ◽  
Antiviral Treatment ◽  
The Novel ◽  
Clinical Experiences ◽  
Synthetic Compounds ◽  
Synthetic Drugs ◽  
Global Pandemic ◽  
The World ◽  
Novel Coronavirus

: The novel coronavirus disease-19 (COVID-19), a global pandemic that emerged from Wuhan, China has today travelled all around the world, so far 216 countries or territories with 21,732,472 people infected and 770,866 deaths globally (as per WHO COVID-19 update dated August 18, 2020). Continuous efforts are being made to repurpose the existing drugs and develop vaccines for combating this infection. Despite, to date, no certified antiviral treatment or vaccine prevails. Although, few candidates have displayed their efficacy in in vitro studies and are being repurposed for COVID-19 treatment. This article summarizes synthetic and semi-synthetic compounds displaying potent activity in their clinical experiences or studies against COVID-19 and also focuses on mode of action of drugs being repositioned against COVID-19.

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.

Synthesis and Antitumor Activity Evaluation of New Phenanthrene-Based Tylophorine Derivatives

2019 ◽  
Vol 16 (6) ◽  
pp. 462-467
Author(s):  
Songtao Li ◽  
Hongling Zhao ◽  
Zhifeng Yin ◽  
Shuhua Deng ◽  
Yang Gao ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Lines ◽  
Antitumor Activities ◽  
Human Carcinoma ◽  
Carcinoma Cell Lines ◽  
Structure Activity ◽  
Human Carcinoma Cell ◽  
Ic50 Values ◽  
Relationship Of

A series of new phenanthrene-based tylophorine derivatives (PBTs) were synthesized in good yield and their structures were characterized by 1H-NMR spectroscopy and ESI MS. In vitro antitumor activity of these compounds against five human carcinoma cell lines, including HCT116 (colorectal), BGC-823 (gastric), HepG-2 (hepatic), Hela (cervical) and H460 (lung) cells, was evaluated by MTT assay. Among these PBTs, compound 6b showed the highest antitumor activities against HCT116 and HepG-2 cell lines with IC50 values of 6.1 and 6.4 μM, respectively, which were comparable to that of adriamycin hydrochloride. The structure-activity relationship of these compounds was also discussed based on the results of their antitumor activity.

Discovery of 3-Cinnamamido-N-Substituted Benzamides as Potential Antimalarial Agents

2020 ◽  
Vol 16 ◽  
Author(s):  
Haicheng Liu ◽  
Yushi Futamura ◽  
Honghai Wu ◽  
Aki Ishiyama ◽  
Taotao Zhang ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Antimalarial Activity ◽  
In Vitro Assays ◽  
Compound Library ◽  
Antimalarial Agents ◽  
Phenotypic Screen ◽  
Ic50 Values ◽  
Substituted Benzamides

Background: Malaria is one of the most devastating parasitic diseases, yet the discovery of antimalarial agents remains profoundly challenging. Very few new antimalarials have been developed in the past 50 years, while the emergence of drug-resistance continues to appear. Objective: This study focuses on the discovery, design, synthesis, and antimalarial evaluation of 3-cinnamamido-N-substituted benzamides. Method: In this study, a screening of our compound library was carried out against the multidrug-sensitive Plasmodium falciparum 3D7 strain. Derivatives of the hit were designed, synthesized and tested against P. falciparum 3D7 and the in vivo antimalarial activity of the most active compounds was evaluated using the method of Peters’ 4-day suppressive test. Results: The retrieved hit compound 1 containing a 3-cinnamamido-N-substituted benzamide skeleton showed moderate antimalarial activity (IC50 = 1.20 µM) for the first time. A series of derivatives were then synthesized through a simple four-step workflow, and half of them exhibited slightly better antimalarial effect than the precursor 1 during the subsequent in vitro assays. Additionally, compounds 11, 23, 30 and 31 displayed potent activity with IC50 values of approximately 0.1 µM, and weak cytotoxicity against mammalian cells. However, in vivo antimalarial activity is not effective which might be ascribed to the poor solubility of these compounds. Conclusion: In this study, phenotypic screen of our compound library resulted in the first report of 3-cinnamamide framework with antimalarial activity and 40 derivatives were then designed and synthesized. Subsequent structure-activity studies showed that compounds 11, 23, 30 and 31 exhibited the most potent and selective activity against P. falciparum 3D7 strain with IC50 values around 0.1 µM. Our work herein sets another example of phenotypic screen-based drug discovery, leading to potentially promising candidates of novel antimalarial agents once given further optimization.

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