scholarly journals Four Novel Phenanthrene Derivatives with α-Glucosidase Inhibitory Activity from Gastrochilus bellinus

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 418
Author(s):  
Htoo Tint San ◽  
Nutputsorn Chatsumpun ◽  
Thaweesak Juengwatanatrakul ◽  
Natapol Pornputtapong ◽  
Kittisak Likhitwitayawuid ◽  
...  

Four new phenanthrene derivatives, gastrobellinols A-D (1–4), were isolated from the methanolic extract of Gastrochilus bellinus (Rchb.f.) Kuntze, along with eleven known phenolic compounds including agrostophyllin (5), agrostophyllidin (6), coniferyl aldehyde (7), 4-hydroxybenzaldehyde (8), agrostophyllone (9), gigantol (10), 4-(methoxylmethyl)phenol (11), syringaldehyde (12), 1-(4′-hydroxybenzyl)-imbricartin (13), 6-methoxycoelonin (14), and imbricatin (15). Their structures were determined by spectroscopic methods. Each isolate was evaluated for α-glucosidase inhibitory activity. Compounds 1, 2, 3, 7, 9, 13, and 15 showed higher activity than the drug acarbose. Gastrobellinol C (3) exhibited the strongest α-glucosidase inhibition with an IC50 value of 45.92 μM. A kinetic study of 3 showed competitive inhibition on the α-glucosidase enzyme. This is the first report on the phytochemical constituents and α-glucosidase inhibitory activity of G. bellinus.

2021 ◽  
Vol 25 (11) ◽  
pp. 11-19
Author(s):  
Chaitanya Darapureddy ◽  
K.R.S. Prasad ◽  
R.S. Ch Phani

The study is intended to evaluate the pharmacological activities, isolation and characterization of the bioactive phytochemical constituents from the crude leaf extract of Sterculia urens Roxb. The extraction of the phytochemicals from the leaves was carried on Soxhlet extraction apparatus using solvents like hexane, ethyl acetate, methanol and water. Pharmacological activities such as DPPH free radical scavenging assay (antioxidant), α-amylase inhibition assay (antidiabetic), albumin denaturation assay (antiinflammatory), blood clot lysis method (thrombolytic) and well diffusion method (antibacterial) of the crude extracts were evaluated and then the semi-preparative HPLC analysis followed by spectral studies was carried for the purification and identification of bioactive compounds. The methanolic extract showed high DPPH radical scavenging activity, α-amylase inhibition activity and albumin denaturation inhibition activity with IC50 values of 29.51±0.11, 146.85±0.18 and 149.91±0.19 μg/mL respectively. The % clot lysis of the methanolic extract was found higher than the other extracts and all the extracts have potential inhibition on the growth of the bacterial studied. From the leaf methanolic extract, 4 phenolic compounds (2,4-dihydroxybenzoic acid, methyl 4- hydroxycinnamate, p-coumaric acid and stercurensin) and 3 phenolic compounds (gossypetin, farrerol and quercetin 5,7,3',4'-tetramethyl ether) were isolated and characterised. Based on the results observed, it can be concluded that the leaf extracts of Sterculia urens Roxb are having rich phytochemical constituents with prominent pharmacological activities.


2018 ◽  
Vol 10 (1) ◽  
pp. 384
Author(s):  
Caroline Wijaya ◽  
Berna Elya ◽  
Arry Yanuar

Objective: This study was carried out to evaluate the phytochemical constituents and tyrosinase inhibitory activity of Cassia fistula leaves.Methods: A tyrosinase inhibitory activity assay was performed by measuring the decrease in the intensity of color suggestive of the inhibition ofdopachrome formation resulting from the L-DOPA-tyrosinase reaction.Results: The test results showed that the tyrosinase inhibitory activity of the water fraction of C. fistula leaf extract had the highest IC50 value(152.031 μg/mL) among other fractions (n-hexane, ethyl acetate, and n-butanol). An enzyme kinetic assay showed that the water fraction of C. fistulaleaf extract inhibited tyrosinase with mixed-type inhibition. Phytochemical screening showed that the water fraction of C. fistula leaf extract containedalkaloids, flavonoids, glycosides, phenols, and tannins.Conclusion: The current study indicated that C. fistula leaves possess significant tyrosinase inhibitory activity.


Author(s):  
SUJATHA ILANGOVAN ◽  
THAVASUMANI P

Objective: The objective of the study was the preliminary screening of the methanolic leaf extract of Couroupita guianensis for various phytochemical constituents, its antioxidant, antibacterial, and antifungal activities. Methods: Phytochemical screening of 18 qualitative, 6 quantitative constituents, antioxidant activity, alpha-amylase inhibitory activity, and alpha-glucosidase inhibitory activity of the methanolic extract of the leaf of C. guianensis was performed adopting the standard protocols. The disk diffusion methods were used for assessing the antibacterial and antifungal activities of the extract. Results: The preliminary studies revealed the presence of alkaloids, saponin, flavonoids, phenol, tannin, and terpenoids in the methanolic extract of the leaf of C. guianensis. Potent antioxidant, free radical scavenging activity, and inhibitory activity against α-amylase and α-glucosidase activity of the methanolic extract were also evident. Conclusions: The preliminary studies in the methanolic extract of the leaf of C. guianensis are suggestive of the therapeutic potentials of the methanolic extract of leaves of C. guianensis.


2021 ◽  
Vol 8 (3) ◽  
pp. 1-9
Author(s):  
Fahima Talhi ◽  
Noureddine Gherraf ◽  
Amar Zellagui ◽  
Awatif Boumaza ◽  
Amira Meghlaoui

Abstract Medicinal plants have several therapeutic properties; they have been used for a long time to treat different diseases. Lantana camara L. has been widely used by man for healing these diseases. In this study, four leaves extracts of L. camara were subjected to preliminary phytochemical screening to determine the presence and/or the absence of phytochemical constituents; In addition, they were tested for hemolytic activity on human erythrocytes. This activity is performed using the UV-Vis spectrophotometer method at 520 nm and at five different concentrations (125 µg/ml, 250 µg/ml, 500 µg/ml, 750 µg/ml, and 1000 µg/ml). The phytochemical screening showed the presence of various phytochemical groups such as phenolic compounds, saponins, sterols, tannins, flavonoids, reducing compounds and the absence of alkaloids in the four extracts. These same extracts showed average hemolytic activity sequentially: chloroformic extract, petroleum ether extract, aqueous extract and then methanolic extract. This activity is dependent on the concentration of the extract.


2020 ◽  
Vol 11 (4) ◽  
pp. 6707-6714
Author(s):  
Sneha Bhatt ◽  
Gletta Anjaly C.T ◽  
Shlini P

Histamine release is involved in developing wakefulness and activation of cortex. The purpose of the study was to find an alternative to these antihistamines by inhibiting the enzyme histidine decarboxylase which is responsible for the production of histamine. Histamine brings about the allergic response due to mast cell degranulation. It is also necessary that the enzyme is not completely inhibited as it plays a role as a neurotransmitter and also regulates gastric acid secretion. In the present study, the methanolic extract of commercially available fennel seeds were examined for its inhibitory activity on the purified extract of bacterial histidine decarboxylase. The methanolic extract of fennel was analyzed to check the presence of various phytochemical constituents. The spice extract was quantified to estimate the presence of flavonoids. The extract was subjected to purification by thin layer chromatography and HPLC in order to isolate and identify the flavonoids present in spice extract. The HPLC results with reference to the standard indicated the presence of ellagic acid and quercetin. The spice extracts were subjected to inhibitory studies at increasing concentrations. The fennel extract at concentration of 0.625 moles was found to be inhibiting histidine decarboxylase which was determined using the Dixon plot. The identified flavonoids were then subjected to software’s like Molinspiration and Swiss ADME in order to study the molecular properties, drug likeliness and pharmacokinetics.


2020 ◽  
Vol 10 (1) ◽  
pp. 77-81
Author(s):  
Rajendra Gyawali ◽  
Bijay Bhattarai ◽  
Susan Bajracharya ◽  
Surakshya Bhandari ◽  
Puja Bhetwal ◽  
...  

Introduction: Antioxidant and α-Amylase inhibitory activity of methanolic extract of Calotropis gigantea (L.) Dryand leaves were evaluated. Methods: The antioxidant activity was evaluated by DPPH assay. The extract was fractionated in Silica gel loaded column chromatography (CC). All fractions were evaluated for their purity by TLC. Out of 11 fractions from CC, one fraction was analyzed by Gas Chromatography-Mass Spectrometry (GC-MS). Results: The antioxidant activity of methanolic extract was found satisfactory (IC50268.80 µg/ml) as compared with ascorbic acid (141.82 µg/ml). TLC of a fractions showed a compound at Rf value at 0.45 in toluene: chloroform: methanol with mobile phase ratio 7:2:1 respectively. Conclusions: Total 17 compounds were identified by GC-MS of ethyl acetate fraction and 5-hydroxyl methyl furfural was major furan compound (59.49%). α-Amylase inhibitory activity of the same fraction showed IC50 value of 0.94 mg/ ml. The Nepalese originated C. gigentea (L.) Dryand possesses antioxidant and α-Amylase inhibitory property.


2020 ◽  
Vol 15 (3) ◽  
pp. 1934578X2091345 ◽  
Author(s):  
Htoo Tint San ◽  
Panitch Boonsnongcheep ◽  
Waraporn Putalun ◽  
Wanwimon Mekboonsonglarp ◽  
Boonchoo Sritularak ◽  
...  

A methanolic extract from the dried root of Dendrobium christyanum Rchb.f. (Orchidaceae) exhibited α-glucosidase inhibitory activity and glucose uptake stimulatory effect. Chromatographic separation of the extract led to the isolation of 13 phenolic compounds (1-13). Their structures were determined by spectroscopic analysis. The isolates were then evaluated for in vitro α-glucosidase inhibitory and glucose uptake stimulatory activities. Methyl haematommate (1), methyl 2,4-dihydroxy-3,6-dimethylbenzoate (3), n-docosyl 4-hydroxy- trans-cinnamate (4), coniferyl aldehyde (6), 4,5-dihydroxy-2-methoxy-9,10-dihydrophenanthrene (7), gigantol (10), and diorcinolic acid (13) showed higher α-glucosidase inhibitory activity than the drug acarbose. Moreover, n-docosyl 4-hydroxyl- trans-cinnamate (4), vanillin (5), and coniferyl aldehyde (6) could enhance glucose uptake by L6 myotubes. Compounds 4 and 6 appear to be potential hypoglycemic agents since they possess both α-glucosidase inhibitory and glucose uptake stimulatory activities. This study is the first report on the chemical constituents and antidiabetic activity of D. christyanum.


2017 ◽  
Vol 12 (6) ◽  
pp. 1934578X1701200
Author(s):  
Tho Huu Le ◽  
Hai Xuan Nguyen ◽  
Truong Van Nhat Do ◽  
Phu Hoang Dang ◽  
Nhan Trung Nguyen ◽  
...  

Bioactivity-guided fractionation of the woods extract of Artocarpus heterophyllus collected in Vietnam revealed that a new 2-arylbenzofuran, moracin VN (1) together with two known compounds were isolated. Compound 1 possessed the inhibitory activity on tyrosinase with IC50 value of 0.82 μM, more potent than the positive control kojic acid (IC50, 44.6 μM). Compound 1 also showed moderate inhibitory activity on xanthine oxidase with IC50 value of 22.8 μM. The kinetic study of tyrosinase was performed on moracin VN (1) showed non-competitive inhibition with Ki value of 2.40 μM.


2016 ◽  
Vol 15 (1) ◽  
Author(s):  
Norsyuhada Alias ◽  
Adam Leow Thean Chor ◽  
Mohd. Shukuri Mohamad Ali ◽  
Abu Bakar Salleh ◽  
Asilah Ahmad Tajudin ◽  
...  

Introduction: Antilipase from natural resources are a potential tool for the treatment of obesity while antioxidant-rich plants are essential in combating degenerative diseases. The aim of this study is to determine the antilipase and antioxidant activity of Orthosiphon stamineus methanolic extract. Methods: The inhibitory activity against pancreatic lipase was determined by measuring the hydrolysis of p-nitrophenyl butyrate to p-nitrophenol at 405 nm. Antioxidant activity of O. stamineus extract was measured by 2, 2, diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity assay. Results: The O. stamineus crude extract exhibited strong lipase inhibitory activity with an IC50 value of 34.7 µg/ml. The inhibition mode study disclosed that O. stamineus could act as uncompetitive inhibitor. O. stamineus showed high antioxidant activity with an EC50 value of 26.3 µg/ml. Conclusions: The results suggest that O. stamineus has shown potential as a source of natural antilipase and antioxidant.


2019 ◽  
Vol 35 (3) ◽  
pp. 982-986 ◽  
Author(s):  
Ekbal Hasan Al-Khateeb ◽  
Ghada Ahmad Al-Assi ◽  
Ashok K. Shakya ◽  
Naseer Al-Rawi ◽  
Naeem Shalan

The macerated methanolic extract of P. vera L., A. strigosa and I. paraguariensis A. St.-Hil. were used for evaluating their antioxidant. The results of present study showed that the IC50 value for Pistacia vera L., Anchusa strigosa and Ilex paraguariensis A. St.-Hil. extracts were 5.85 ± 0.11, 43.75 ± 1.05 and 8.98 ± 0.65µg/ml respectively compared to 1.48 ± 0.05 µg/ml of ascorbic acid against DPPH radical. The IC50 values for β-carotene bleaching (BCB) assay for P. vera L., A. strigosa and I. paraguariensis A. St.-Hil. extracts were 390.1 ± 7.5, 425.8 ± 6.5 and 410.2 ± 9.0 µg/ml respectively compared to 9.5 ± 0.4 µg/ml of rutin. The results of β-carotene bleaching (BCB) assay showed that the plant extract exhibits weak activity compared to rutin. In conclusion, the present study indicates that these plants and their phytochemical constituents can be exploited in future extensively for controlling oxidative stress and ailments.


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