scholarly journals IN-VITRO HYPOGLYCEMIC EVALUATION OF FRACTIONS OF HYDRO-ACOHOLIC EXTRACT OF HEARTWOOD OF TECOMELLA UNDULATA LINN.

2017 ◽  
Vol 10 (2) ◽  
pp. 266
Author(s):  
Munish Garg ◽  
Ruby Rohilla ◽  
Chanchal Garg
Keyword(s):  
Postprandial Hyperglycemia ◽  
Alcoholic Extract ◽  
Phytochemical Screening ◽  
Bioactive Components ◽  
Standard Drug ◽  
Minimal Inhibitory Concentrations ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Tecomella Undulata

Objective: To screen α-amylase and α-glucosidase inhibitors from the different fractions of crude hydro-alcoholic extract of heartwood of Tecomella undulata Linn.Methods: Four fractions of crude hydro-alcoholic extract of heartwood of plant were used for in-vitro inhibitory assays against digestive enzymes: α-amylase and α-glucosidase. For assay, different concentrations (20, 40, 60, 80, 100 µg/ml) were used for all fractions. Standard protocol was used for preliminary phytochemical screening of different bioactive components present in all fractions.Results: The fractions have shown moderate to highest inhibitory activity against both enzymes. But, the strong inhibition was revealed by acetone fraction against α-amylase with very minimal inhibitory concentrations at IC50 values when compared with a standard drug acarbose. Several medicinally active phytocomponents such as flavanoids, saponin, anthraquinones, tannins, triterpenoids and phenols were observed in all studied fractions.Conclusion: The different fractions prepared from crude hydro-alcoholic extract of heartwood of plant are capable of inhibiting α-amylase and α-glucosidase and it can be concluded that heartwood of Tecomella undulata Linn. is partially active against postprandial hyperglycemia, thus diabetes mellitus.Keywords: Tecomella undulata Linn., Diabetes mellitus, α-Amylase, α-Glucosidase. 

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). 

Study on the interaction of 1,5-diaryl pyrrole derivatives with α-glucosidase; synthesis, molecular docking, and kinetic study

2019 ◽  
Vol 15 ◽  
Author(s):  
Tadesse Bekele Tafesse ◽  
Ebrahim Saeedian Moghadam ◽  
Mohammed Hussen Bule ◽  
Mohammad Ali Faramarzi ◽  
Mohammad Abdollahi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Kinetic Studies ◽  
Postprandial Hyperglycemia ◽  
Binding Energies ◽  
Potential Candidate ◽  
Pyrrole Derivatives ◽  
Standard Drug ◽  
Glucosidase Inhibitors ◽  
Inhibitory Activities

Background: The delaying of absorption of glucose is one of the principal therapeutic approaches of type 2 diabetes. α-glucosidase inhibitors compete with the α-glucosidase enzyme activity, which helps to reduce the conversion of carbohydrates into glucose and thereby control the postprandial hyperglycemia incidence. Objective: The aim of this study was to synthesize a series of novel 1,5-diphenyl pyrrole derivatives and evaluate their in vitro α-glucosidase inhibitory activities. Methods: Compounds were synthesized through a multistep reaction and were evaluated for α-glucosidase inhibitory activities. Molecular docking and kinetic studies were carried out to predict the mode of binding and mechanism of inhibition for the most active compounds, 5g and 5b, against α-glucosidase. Results: Synthesized compounds showed good in vitro α-glucosidase inhibitory activity with IC50 values in the range of (117.5 ± 3.8 to 426.0 ± 10.2 µM) as compared to acarbose, the standard drug, (750 ± 8.7 µM). Compound 5g (117.5 ± 3.8 µM) ascertained as the most potent inhibitor of α-glucosidase in a competitive mode. The binding energies of compounds 5g and 5b (119.0 ± 7.5 µM), as observed from the best docking conformations, indicates that they have a lower free binding energy (-3.26 kcal/mol and -3.0 kcal/mol, respectively) than acarbose (2.47 kcal/mol). Conclusion: The results of our study reveal that the synthesized compounds are a potential candidate for α-glucosidase inhibitors for the management of postprandial hyperglycemia for further investigation.

GC-MS Characterization of Phyto-Components in the Ethanolic and Hydroalcoholic Extracts of Cocos nucifera Endocarp and Evaluation of their Antimalarial Potential

2019 ◽  
Vol 9 (4) ◽  
pp. 289-294
Author(s):  
Babita Aggarwal ◽  
Pankaj Sharma ◽  
Hardarshan Singh Lamba
Keyword(s):  
Antimalarial Activity ◽  
Cocos Nucifera ◽  
Antiplasmodial Activity ◽  
Bioactive Components ◽  
Traditional Use ◽  
Standard Drug ◽  
Ic50 Values

Background: Plants are rich and cheap source of active phytoconstituents. Present study was performed in order to authenticate the traditional use of Cocos nucifera in malaria treatment as well as to search an alternative for drug resistant parasites. Objective: In the present investigation, ethanolic (ACN) and hydroalcoholic (HACN) extracts of Cocos nucifera endocarp were evaluated for antimalarial potential as well as subjected to GC-MS analysis to characterize the bioactive components. Methods: In vitro antiplasmodial activity of ACN and HACN was assessed against P. falciparum strains MRC-02 (CQ sensitive) and RKL-09 (CQ resistant) and percentage schizont maturation inhibition was determined. To confirm the antimalarial potential, in vivo Peter’s 4-Day suppressive test using P. berghei strain was performed at a dose of 25 and 50 mg/kg/day for 4 consecutive days. Bioactive components were characterized by the application of Gas chromatography and Mass spectrometric technique to the extracts. Results: Promising in vitro antiplasmodial activity was exhibited by both alcoholic (ACN) and hydroalcoholic (HACN) extracts against P. falciparum strains MRC-02 (CQ sensitive) with IC50 values < 5 µg/mL. HACN (% Suppression = 75.43 ± 0.18; MST=19.21 days) and ACN (% Suppression = 34.65 ± 0.11; MST=10.11 days) showed moderate in vivo antimalarial activity (p < 0.05) at dose 50 mg/Kg while standard drug chloroquine (8mg/kg) suppressed 100% parasitaemia. Twenty compounds have been identified and characterized by GC-MS studies.

scholarly journals Inhibition of Heme Polymerization Invitro Assay Of Extract of Sirih Leaf (Piper betle Linn.) and Sun Flower Leaves (Helianthus annuus L.)

2020 ◽  
Vol 7 (1) ◽  
pp. 22 ◽  
Author(s):  
Ami Tjitraresmi ◽  
Moelyono Moektiwardoyo ◽  
Yasmiwar Susilawati
Keyword(s):  
Helianthus Annuus ◽  
Antimalarial Activity ◽  
Antimalarial Drugs ◽  
Piper Betle ◽  
Phytochemical Screening ◽  
Helianthus Annuus L ◽  
Betel Leaf ◽  
The People ◽  
Ic50 Values

Malaria is a disease that occurs in tropical countries like Indonesia. The incidence of malaria in the world is still quite high and the occurrence of cases of Plasmodium resistance to antimalarial drugs and the widespread of resistance have prompted researchers to look for new antimalarial drugs, especially from natural materials. Betel leaf (Piper betle Linn.) And sunflower leaf (Helianthus annuus L.) have long been used by the people of Indonesia as an antimalarial drug. The purpose of this study was to determine antimalarial activity through inhibition of heme polymerization and determine secondary metabolite compounds by phytochemical screening from betel leaves and sunflower leaves. The heme polymerization inhibition activity assay was carried out by the in-vitro method using a microplate reader at 415 nm and 630 nm wavelengths. IC50 values of betel leaf extract and sunflower leaf were 178.67 μg/ml and 160.10 μg/ml, respectively. Phytochemical screening results from betel leaf showed the presence of flavonoids, polyphenols, tannins, quinones, saponins, and monoterpenoids-sesquiterpenoids, while sunflower leaves contain alkaloids, polyphenols, flavonoids, steroids and monoterpenoids-sesquiterpenoids.Keywords: Piper betle Linn., Helianthus annuus L., Malaria, Heme Polymerization

scholarly journals In Vitro and In Vivo Effectiveness of Carvacrol, Thymol and Linalool against Leishmania infantum

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2072 ◽  
Author(s):  
Mohammad Reza Youssefi ◽  
Elham Moghaddas ◽  
Mohaddeseh Abouhosseini Tabari ◽  
Ali Akbar Moghadamnia ◽  
Seyed Mohammad Hosseini ◽  
...  
Keyword(s):  
Mtt Assay ◽  
Leishmania Infantum ◽  
Standard Drug ◽  
In Vivo Test ◽  
Causative Agents ◽  
Ic50 Values ◽  
Vector Borne ◽  
Effective Drugs

Background: One of the most important causative agents of visceral leishmaniasis (VL) is Leishmania infantum, which is mainly spread by Phlebotomus and Lutzomyia sandflies in the Old and New World, respectively. Novel and effective drugs to manage this neglected vector-borne disease are urgently required. In this study, we evaluated the toxicity of carvacrol, thymol and linalool, three common essential oil constituents, on amastigotes and promastigotes of L. infantum. Methods: in vitro experiments were performed by 24 h MTT assay. Carvacrol, thymol and linalool at concentrations ranging from 1.3 to 10 μg/mL were tested on promastigotes of L. infantum. For in vivo test, two groups of hamsters (Mesocricetus auratus) received 100 mg/kg of body weight/day of carvacrol and thymol as intraperitoneal injection on day 7 post-infection, followed by a 48 h later injection. The third group was treated with the glucantime as standard drug (500 mg/kg) and the last group (control) just received normal saline. On the 16th day, the number of parasites and histopathological changes in liver and spleen were investigated. Results: 24 h MTT assay showed promising antileishmanial activity of thymol and carvacrol, with IC50 values of 7.2 (48 μM) and 9.8 μg/mL (65 μM), respectively. Linalool at all concentrations did not affect L. infantum promastigote viability. In vivo toxicity data of carvacrol and thymol showed that the former at 100 mg/kg was the safest and most effective treatment with little side effects on the liver. Conclusions: Overall, thymol and carvacrol are highly promising candidates for the development of effective and safe drugs in the fight against VL.

scholarly journals Aktivitas Antioksidan Ekstrak Metanol Daun Alpukat Menggunakan Metode DPPH

2021 ◽  
Vol 11 (2) ◽  
pp. 104-110
Author(s):  
Alfin Surya ◽  
Zaiyar Nazir ◽  
Anggun Syazulfa
Keyword(s):  
Antioxidant Activity ◽  
Ascorbic Acid ◽  
Free Radicals ◽  
Methanol Extract ◽  
Natural Antioxidants ◽  
Positive Control ◽  
Phytochemical Screening ◽  
Bioactive Components ◽  
Ic50 Value ◽  
Ic50 Values

Free radicals are molecules that lose electrons in their outer orbitals so that the number of electrons becomes odd and unstable. Free radicals can damage various macromolecule cells including proteins, carbohydrates, fats. Antioxidants are compounds that can donate one or more electrons to free radicals. Avocado leaves contain high bioactive components that can be used as a source of natural antioxidants. Avocado leaves that have been dried, mashed and then shifted with methanol. The extracts were tested by phytochemical screening, including flavonpoid, phenolic, tannin and antioxidant activity using the DPPH (2,2-diphenyl-1-picrylhidrazyl) method. This method is based on the reduction of 2,2-diphenyl-1-picrylhydrazyl (DPPH) against free radicals which causes a change from purple to yellow 2,2-diphenyl-1-picrylhydrazyl) (DPPH). From the research, the IC50 values ​​in avocado leaves were 118.8056 µg / mL and 7,276 µg / mL on ascorbic acid as a positive control. From the IC50 value obtained, it is known that the methanol extract of avocado leaves has strong antioxidant activity to fight free radicals.

scholarly journals Synthesis and Evaluation of Triazolyl Dihydropyrimidines as Potential Anticancer Agents

2018 ◽  
Vol 10 (4) ◽  
pp. 18
Author(s):  
Rajanna Ajumeera ◽  
Ganapathi Thipparapu ◽  
Shireesha Boyapati ◽  
Bharath Singh Padya ◽  
Vijayalaxmi Venkatesan
Keyword(s):  
Anticancer Agents ◽  
Human Breast Cancer Cell ◽  
S Phase ◽  
Human Breast ◽  
Standard Drug ◽  
M Phase ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Mcf 7

Novel N &ndash; triazolyl 3(a-f) and O-triazolyl (4a-f) derivatives of 4, 6-diaryl-1, 4-dihydropyrimidines were synthesized through mannich reaction. All compounds were characterized by physical and spectral data. These compounds were screened for in vitro efficiency in human breast cancer cell (MCF-7&amp;MDA-MB-231) lines and found to have very good anti-proliferative activity.&nbsp; Among all compounds of 4b, 3e, 4e endowed with lesser respective IC50 values of 31.94, 55.73, 55.03 &micro;M in MCF-7 cells and 41.50, 35.28, 32.06 &micro;M in MDA-MB 231 cells by MTT assay. In further studies, Compounds 4b, 3e, 4e were found to arrest cell growth at S phase in MCF-7 cells. In MDA-MB 231 cells, 4b, 4e were found to arrest the cells in S phase, and compound 3e found to arrest G2/M phase when compared to the standard drug tamoxifen, arrested S phase in MCF-7 cells and G0/G1 phase in MDA-MB 231 cells.

Evaluation of in-vitro antidiabetic activity of leaf juice of Plectranthus amboinicus (lour.)

2020 ◽  
Vol 10 (1) ◽  
pp. 9-17
Author(s):  
Pavan Kumar Kurakula ◽  
Tharun D ◽  
Mahantesh S ◽  
Krishna O ◽  
Sudheer A ◽  
...  
Keyword(s):  
Side Effects ◽  
Enzyme Inhibitors ◽  
Antidiabetic Activity ◽  
Albino Rat ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Gastrointestinal Side Effects ◽  
Plectranthus Amboinicus ◽  
Leaf Juice

Diabetes mellitus ‘the disease of modern civilization’ is characterized by chronic hyperglycaemia. The management of elevated post prandial glucose is critical to control the sequale of complications and α-amylase, α-glucosidases are responsible for elevated plasma glucose. Enzyme inhibitors in current clinical practice like acarbose, voglibose etc. are known to cause various gastrointestinal side effects. The present study was aimed to screen for potential α-amylase and α-glucosidase inhibitors from natural sources by in–vitro antidiabetic assays to overcome the side effects and toxicity. Different concentrations of leaf juice of Plectranthus amboinicus Lour. (20, 40, 60, 80 &amp;100 μg/ml) were tested against fungal α-amylase and α-glucosidases isolated from albino rat small intestine and a prominent dose dependent inhibition of the enzymes was observed comparable with the marketed product, Acarbose. The IC50 values of LJPA and acarbose on fungal α-amylase was found to be 83.15 &amp;52.15 μg/ml respectively. The IC50 values of LJPA and acarbose on α-glucosidase was found to be 92.44 &amp;54.84 μg/ml respectively. The protein concentration of leaf juice was found to be 10.6 mg/ml.

2-Mercapto Benzothiazole Derivatives: As Potential Leads for the Diabetic Management

2020 ◽  
Vol 16 (6) ◽  
pp. 826-840
Author(s):  
Saeed Ullah ◽  
Salma Mirza ◽  
Uzma Salar ◽  
Shafqat Hussain ◽  
Kulsoom Javaid ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Inhibitory Activity ◽  
Kinetic Studies ◽  
Binding Pocket ◽  
Docking Studies ◽  
Standard Drug ◽  
Dual Nature ◽  
Benzothiazole Derivatives ◽  
Glucosidase Inhibitors

Background: Results of our previous studies on antiglycation activity, and the noncytotoxicity of 2-mercapto benzothiazoles, encouraged us to further widen our investigation towards the identification of leads against diabetes mellitus. Methods: 33 derivatives of 2-mercapto benzothiazoles 1-33 were evaluated for in vitro α- glucosidase inhibitory activity. Mode of inhibition was deduced by kinetic studies. To predict the interactions of 2-mercapto benzothiazole derivatives 1-33 with the binding pocket of α-glucosidase enzyme, molecular docking studies were performed on the selected inhibitors. Results: Compounds 2-4, 6-7, 9-26, 28 and 30 showed many folds potent α-glucosidase inhibitory activity in the range of IC50 = 31.21-208.63 μM, as compared to the standard drug acarbose (IC50 = 875.75 ± 2.08 μM). It was important to note that except derivative 28, all other derivatives were also found previously to have antiglycating potential in the range of IC50 = 187.12-707.21 μM. Conclusion: A number of compounds were identified as dual nature as antiglycating agent and α- glucosidase inhibitors. These compounds may serve as potential lead candidates for the management of diabetes mellitus.

Antisickling Activity of the Fresh and Dried Roots of Cissus populnea Guill. Et Perr (Vitaceae)

2015 ◽  
Vol 19 ◽  
pp. 134-138
Author(s):  
EM Adebayo ◽  
AA Adeyemi ◽  
OO Omotade ◽  
FA Fasola ◽  
TO Ajayi ◽  
...  
Keyword(s):  
Sickle Cell Disease ◽  
Sickle Cell ◽  
Maximum Activity ◽  
Research Strategy ◽  
Powdered Sample ◽  
Phytochemical Screening ◽  
Cell Disease ◽  
Traditional Use ◽  
Standard Drug

Research into plants with claimed traditional use in the management of sickle cell anaemia constitutes a useful research strategy in the search for new antisickling drugs and templates. The root of Cissus populnea has been used traditionally in the management of sickle cell disease (SCD). Phytochemical screening of the fresh and powdered sample of the root of C. populnea (CP) was done using standard methods followed by in vitro antisickling evaluation of extracts, solvent-partitioned fraction (ethylacetate) and the vacuum liquid chromatographic fractions (VLC) of the fresh and dried roots of C. populnea with sodium metabisulphite induced sickling of HbSS erythrocytes. p-hydroxybenzoic acid and normal saline were used as positive and negative controls respectively. Phytochemical screening revealed the presence of tannins, saponins and cardiac glycosides. The result of this study showed that the extracts and solvent partitioned fraction (ethylacetate) from the root of CP have antisickling property with a higher activity for the ethylacetate partitioned fraction of the dried roots compared to that of the fresh roots. The VLC fractions exhibited higher activity than the crude extracts; fraction 3 (FR3) had the maximum activity of 96.4% while 88.6% activity was demonstrated for the standard drug (PABA) at an incubation time of 45 min. This study has thus provided scientific evidence for the traditional use of CP in the management of SCD.Keywords: Sickle Cell Disease, Cissus populnea, Antisickling Activity

Sign in / Sign up

Export Citation Format

Share Document