scholarly journals Inhibition Kinetics of Sida rhombifolia L. Extract Toward Xanthine Oxidase by Electrochemical Method

2014 ◽  
Vol 14 (1) ◽  
pp. 71-77 ◽  
Author(s):  
Dyah Iswantini ◽  
Muammar Yulian ◽  
Sri Mulijani ◽  
Trivadila Trivadila
Keyword(s):  
Xanthine Oxidase ◽  
Crude Extract ◽  
Inhibitory Activity ◽  
Electrochemical Method ◽  
Competitive Inhibition ◽  
Ethanol Extract ◽  
Inhibition Kinetics ◽  
Ic50 Value ◽  
Kinetics Of ◽  
Sida Rhombifolia

Sida rhombifolia L. is a traditional medicinal plant that has been known with potential as antigout. The previous research suggested that flavonoids crude extract of S. rhombifolia had an inhibitory activity toward xanthine oxidase by 71% and a spectrophotometric measurement showed that the type of flavonoids crude extract inhibition was a competitive inhibition. The purpose of the research was to investigate the type of inhibition kinetic of S. Rhombifolia’s ethanol extract by electrochemical method and to compare the measurements of linearity and sensitivity between spectrophotometric and electrochemical methods. The results showed that the yield of S. Rhombifolia’s ethanol extract was 9.82% with the inhibitory activity ranging from 13.64% to 82.69% (5.00-200 mg L-1) and IC50 value was 91.15±5.74 mg L-1. Allopurinol as a control showed the inhibitory activity of 15.26-70.95% (0.10-4.00 mg L-1) and IC50 value was 2.45±2.21 mg L-1. Inhibition kinetics of the ethanol extract caused a KM increase and unchange of VMAX. Based on the data, the type of inhibition kinetics was a competitive inhibition, with an inhibitor affinity (α) value of 3.18. Linearity of xanthine oxidase activity assay by electrochemical and spectrophotometric methods showed the range of 0.01-1.00 mM (R2 = 0.978) and 0.05-0.70 mM (R2 = 0.977) respectively. The sensitivity of electrochemical method was reported higher (0.95 μA mM-1) than the spectrophotometric method (0.007 min-1).

scholarly journals Aktivitas Penghambatan Xantin Oksidase pada Ekstrak Daun Sirih Hitam (Piper sp)

2016 ◽  
Vol 3 ◽  
pp. 160-163
Author(s):  
Muhammad Amir Masruhim ◽  
Wisnu Cahyo Prabowo ◽  
Dita Paramitha
Keyword(s):  
Uric Acid ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Ethanol Extract ◽  
Betel Leaf ◽  
Activity Test ◽  
Ic50 Values ◽  
One Way Anova

Hyperuricemia is a condition in which increased levels of uric acid in the blood. Xanthine oxidase role in the oxidation of hypoxanthine and xanthine to uric acid. One treatment of hyperuricemia is inhibiting xanthine oxidase in the process of formation of uric acid. The purpose of this study to determine the inhibitory activity of xanthine oxidase in the ethanol extract of black betel leaf (Piper sp). Xanthine oxidase inhibitory activity test using UV-Vis spectrophotometry in vitro with a concentration of 5 ppm, 10 ppm and 20 ppm. The data obtained were analyzed using one-way ANOVA. The result is the ethanol extract of black betel leaf has a different activity significantly and IC50 values obtained is 65.96 ppm.

scholarly journals POTENSI BIODIVERSITAS INDONESIA SEBAGAI INHIBITOR XANTINA OKSIDASE DAN ANTIGOUT

2014 ◽  
Vol 2 (1) ◽  
pp. 80
Author(s):  
Muammar Yulian
Keyword(s):  
Medicinal Plants ◽  
Xanthine Oxidase ◽  
Ethanol Extract ◽  
Andrographis Paniculata ◽  
Apium Graveolens ◽  
Degenerative Diseases ◽  
Potential Inhibitor ◽  
Ic50 Values ◽  
Sida Rhombifolia

Tendency for people to go back to nature and the government's policy to "Saintifikasi Jamu" prioritizing in degenerative diseases such as hyperglycemia, hypertension, hypercholesterolemia and hyperuricemia / gout is a condition that is highly prospective and has pushed for the development of research on medicinal plants-based biodiversity Indonesiasebagai state megabiodiversity. Results of research have shown that among the diversity of Indonesia's biodiversity as a potential inhibitor of xanthine oxidase (XO) and antigot is sidaguri (Sida rhombifolia L), celery (Apium graveolens L), fruits (Salacca R. edulis) varieties of Bangkok, ear- earrings (Acalypha indicaL.), and Bitter (Andrographis paniculata, Ness.). Ethanol extract of the herb sidaguri XO inhibitor has potential as indicated by the ability to dampen the activity of XO with IC50 values

scholarly journals Xanthine Oxidase Inhibitory Activity, Chemical Composition, Antioxidant Properties and GC-MS Analysis of Keladi Candik (Alocasia longiloba Miq)

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2658 ◽  
Author(s):  
Ferid Abdulhafiz ◽  
Arifullah Mohammed ◽  
Fatimah Kayat ◽  
Matcha Bhaskar ◽  
Zulhazman Hamzah ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Side Effects ◽  
Herbal Medicine ◽  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Total Phenolic ◽  
Phytochemical Analysis ◽  
Fruit Extracts ◽  
Ms Analysis ◽  
Ic50 Value

Alocasia longiloba, locally known as ‘Keladi Candik’, has been used traditionally to treat wounds, furuncle and joint inflammations. A. longiloba can be a new source of herbal medicine against hyperuricemia by inhibiting the activity of xanthine oxidase enzyme, the enzyme which is responsible for the development of hyperuricemia in human. Existing xanthine oxidase inhibitors (XOI drugs) show several side effects on gout patients. Therefore, an alternative herbal medicine from plants, with high therapeutic property and free of side effects, are greatly needed. This study was conducted to evaluate XO inhibitory activity, chemical composition, antioxidant activity and GC-MS profile of A. longiloba. Our results showed that ethanolic petiole extract exhibited the highest XO inhibitory activity (70.40 ± 0.05%) with IC50 value of 42.71 μg/mL, followed by ethanolic fruit extracts (61.44 ± 1.24%) with the IC50 value of 51.32 μg/mL. In a parallel study, the phytochemical analysis showed the presence of alkaloid, flavonoid, terpenoids, glycoside and saponin in petiole and fruit extracts, as well as higher total phenolic and flavonoid contents and strong scavenging activity on DPPH and ABTS antioxidant assay. The GC-MS analysis of fruit and petiole extracts revealed the presence of various compounds belonging to different chemical nature, among them are limonen-6-ol, α-DGlucopyranoside, paromomycin, aziridine, phenol, Heptatriacotanol, Phen-1,2,3-dimethyl and Betulin found in ethanolic fruit extract, and Phen-1,4-diol,2,3-dimethyl-, 1-Ethynyl-3,trans(1,1-dimethylethyl), Phenol,2,6-dimethoxy-4-(2-propenyl)- and 7-Methyl-Z-tetradecen-1-olacetate found in ethanolic petiole extract. Some compounds were documented as potent anti-inflammatory and arthritis related diseases by other researchers. In this study, the efficiency of solvents to extract bioactives was found to be ethanol > water, methanol > hexane > chloroform. Together, our results suggest the prospective utilization of fruit and petiole of A. longiloba to inhibit the activity of XO enzyme.

Phenylpropanoid and Iridoid Glucosides from the Whole Plant of Hemiphragma heterophyllum and Their alpha-Glucosidase Inhibitory Activities

Planta Medica ◽  
2020 ◽  
Vol 86 (03) ◽  
pp. 205-211
Author(s):  
Yan-Hong Li ◽  
Jia-Meng Dai ◽  
Cui Yang ◽  
Meng-Yuan Jiang ◽  
Yong Xiong ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Ethanol Extract ◽  
2D Nmr ◽  
Positive Control ◽  
Iridoid Glucoside ◽  
2D Nmr Spectroscopy ◽  
Whole Plant ◽  
Ic50 Value ◽  
Iridoid Glucosides ◽  
Alpha Glucosidase

AbstractThree phenylpropanoid glucosides (1 – 3) and one iridoid glucoside (11), together with eleven known glucosides, were isolated from the ethanol extract of the whole plant of Hemiphragma heterophyllum. Their structures were elucidated by means of 1D and 2D NMR spectroscopy, HRMS, and chemical methods. All compounds except 11 and 13 – 15 showed varying degrees of α-glucosidase inhibitory activity. Compounds 5, 9, and 12 were marginally active in the bioassay, while compounds 1 – 4, 6 – 8, and 10 exhibited appreciable inhibitory activity with an IC50 value of 33.6 ~ 83.1 µM, which was much lower than that of the positive control acarbose (IC50 = 310.8 µM).

scholarly journals Halogen-Substituted Triazolethioacetamides as a Potent Skeleton for the Development of Metallo-β-Lactamase Inhibitors

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1174 ◽  
Author(s):  
Yilin Zhang ◽  
Yong Yan ◽  
Lufan Liang ◽  
Jie Feng ◽  
Xuejun Wang ◽  
...  
Keyword(s):  
Antibiotic Resistance ◽  
Inhibitory Activity ◽  
Docking Studies ◽  
Hydroxyl Group ◽  
Inhibition Kinetics ◽  
Ic50 Value ◽  
Lactam Antibiotic ◽  
Value Range ◽  
Ic50 Values ◽  
Enzyme Inhibition Kinetics

Metallo-β-lactamases (MβLs) are the target enzymes of β-lactam antibiotic resistance, and there are no effective inhibitors against MβLs available for clinic so far. In this study, thirteen halogen-substituted triazolethioacetamides were designed and synthesized as a potent skeleton of MβLs inhibitors. All the compounds displayed inhibitory activity against ImiS with an IC50 value range of 0.032–15.64 μM except 7. The chlorine substituted compounds (1, 2 and 3) inhibited NDM-1 with an IC50 value of less than 0.96 μM, and the fluorine substituted 12 and 13 inhibited VIM-2 with IC50 values of 38.9 and 2.8 μM, respectively. However, none of the triazolethioacetamides exhibited activity against L1 at inhibitor concentrations of up to 1 mM. Enzyme inhibition kinetics revealed that 9 and 13 are mixed inhibitors for ImiS with Ki values of 0.074 and 0.27μM using imipenem as the substrate. Docking studies showed that 1 and 9, which have the highest inhibitory activity against ImiS, fit the binding site of CphA as a replacement of ImiS via stable interactions between the triazole group bridging ASP120 and hydroxyl group bridging ASN233.

Phosphodiesterase 5 Inhibitors from Derris scandens

Planta Medica ◽  
2018 ◽  
Vol 84 (15) ◽  
pp. 1134-1140 ◽  
Author(s):  
Nattiya Chaichamnong ◽  
Prapapan Temkitthawon ◽  
Nantaka Khorana ◽  
Prompan Pitpakdeeanan ◽  
Pornnarin Taepavarapruk ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Ethanol Extract ◽  
Bioactive Constituents ◽  
First Line ◽  
Phosphodiesterase 5 Inhibitors ◽  
Ic50 Value ◽  
Limit Of Quantitation ◽  
Satisfactory Precision ◽  
Ic50 Values ◽  
Phosphodiesterase 5

AbstractPhosphodiesterase 5 inhibitors have been used as a first-line medicine for the treatment of erectile dysfunction. In the search for new phosphodiesterase 5 inhibitors from natural sources, we found that the 95% ethanol extract of Derris scandens stem showed phosphodiesterase 5 inhibitory activity with an IC50 value of about 7 µg/mL. Seven isoflavones and a coumarin constituent isolated from this plant were investigated for phosphodiesterase 5 inhibitory activity. The results showed that osajin (8), 4′,5,7-trihydroxybiprenylisoflavone (4), and derrisisoflavone A (2) had the ability to inhibit phosphodiesterase 5 with IC50 values of 4, 8, and 9 µM, respectively. These compounds exhibited selectivity on phosphodiesterase 5 over phosphodiesterase 1, however, the selectivity on phosphodiesterase 5 over phosphodiesterase 6 was low. In order to quantitatively determine these bioactive constituents in D. scandens extract, LC-QTOF-MS method has been developed and validated. The limit of quantitation values in the range of 0.1 – 5 µg/mL were obtained. The assay showed satisfactory precision and accuracy. The results from our method showed that the 95% ethanol extract of D. scandens stem was comprised of all eight compounds, with derrisisoflavone A (2) and lupalbigenin (3) presenting as the major constituents.

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 ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Kinetic Study ◽  
Inhibitory Activity ◽  
Methanolic Extract ◽  
Competitive Inhibition ◽  
Spectroscopic Methods ◽  
First Report ◽  
Ic50 Value ◽  
Phytochemical Constituents

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.

scholarly journals Sambiloto (Andrographis paniculata Nees.) leaf extract activity as an α-Amylase enzyme inhibitor

2021 ◽  
pp. 305-308
Author(s):  
Yustina Sri Hartini ◽  
Dewi Setyaningsih ◽  
Maria Josephine Vivian Chang ◽  
Maria Cyrilla Iglesia Adi Nugrahanti
Keyword(s):  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Enzyme Inhibitor ◽  
Statistical Tests ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
Andrographis Paniculata ◽  
Activity Test ◽  
Ic50 Value

Introduction: Sambiloto (Andrographis paniculata) is an antidiabetic medicinal plant that acts by inhibiting the α-amylase enzyme. Andrographolide, the active compound of sambiloto leaf, is insoluble in water but dissolves in ethanol. Aim: This study compared the in vitro activity of aqueous extract and ethanolic extract of sambiloto leaf with the α-amylase enzyme. Methods: The inhibitory activity test of the α-amylase enzyme was carried out using the ultraviolet-visible spectrophotometric method by measuring the absorbance of the remaining starch, which forms a blue complex with iodine-iodide. Results: The inhibitory activity of the α-amylase enzyme of the aqueous extract of sambiloto leaf (with the IC50 value of 14.203 ± 0.112 mg/mL) was lower than that of the ethanol extract (with the IC50 value of 9.253 ± 0.116 mg/mL). The results of the statistical tests showed significant differences (p <0.05) between the inhibitory activity of the α-amylase enzyme acarbose and the activity of both extracts.

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