scholarly journals (5-Hydroxy-4-oxo-2-styryl-4H-pyridin-1-yl)-acetic Acid Derivatives as Multifunctional Aldose Reductase Inhibitors

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5135
Author(s):  
Huan Chen ◽  
Xin Zhang ◽  
Xiaonan Zhang ◽  
Wenchao Liu ◽  
Yanqi Lei ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Acetic Acid ◽  
Aldose Reductase ◽  
Polyol Pathway ◽  
Binding Mode ◽  
Positive Control ◽  
Reductase Inhibitors ◽  
Ic50 Values ◽  
Antioxidative Action ◽  
Phenyl Vinyl

As rate-limited enzyme of polyol pathway, aldose reductase (ALR2) is one of the key inhibitory targets for alleviating diabetic complications. To reduce the toxic side effects of the inhibitors and to decrease the level of oxidative stress, the inhibitory selectivity towards ALR2 against detoxicating aldehyde reductase (ALR1) and antioxidant activity are included in the design of multifunctional ALR2 inhibitors. Hydroxypyridinone derivatives were designed, synthesized and evaluated their inhibitory behavior and antioxidant activity. Notably, {2-[2-(3,4-dihydroxy-phenyl)-vinyl]-5-hydroxy-4-oxo-4H-pyridin-1-yl}-acetic acid (7l) was the most potent, with IC50 values of 0.789 μM. Moreover, 7l showed excellent selectivity towards ALR2 with selectivity index 25.23, which was much higher than that of eparlestat (17.37), the positive control. More significantly, 7l performed powerful antioxidative action. At a concentration of 1 μM, phenolic compounds 7l scavenged DPPH radical with an inhibitory rate of 41.48%, which was much higher than that of the well-known antioxidant Trolox, at 11.89%. Besides, 7l remarkably suppressed lipid peroxidation with a rate of 88.76% at a concentration of 100 μM. The binding mode derived from molecular docking proved that the derivatives were tightly bound to the activate site, suggesting strongly inhibitory action of derivatives against ALR2. Therefore, these results provided an achievement of multifunctional ALR2 inhibitors capable with potency for both selective ALR2 inhibition and as antioxidants.

scholarly journals Isatin Derivatives as a New Class of Aldose Reductase Inhibitors With Antioxidant Activity

2021 ◽  
Author(s):  
Wenchao Liu ◽  
Huan Chen ◽  
Xiaonan Zhang ◽  
Xin Zhang ◽  
Long Xu ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Acetic Acid ◽  
Aldose Reductase ◽  
Acid Group ◽  
Docking Studies ◽  
Side Chain ◽  
New Class ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors ◽  
Isatin Derivatives

Abstract In this work, isatin was employed as the scaffold to design aldose reductase inhibitors with antioxidant activity. Most of the isatin derivatives were proved to be excellent in the inhibition of aldose reductase (ALR2) with IC 50 values at submicromolar level, and (E)-2-(5-(4-methoxystyryl)-2,3-dioxoindolin-1-yl) acetic acid (9g) was identified as the most effective with an IC 50 value of 0.015 μM. Moreover, compounds 9a-h with styryl side chains at the C5 position of isatin showed potent antioxidant activity. Particularly, the phenolic compound 9h demonstrated similar antioxidant activity with the well-known antioxidant Trolox. Structure-activity relationship and molecular docking studies showed that the acetic acid group at N1 and C5 p-hydroxystyryl side chain were the key structures to increase the aldose reductase inhibitory activity and antioxidant activity.

ChemInform Abstract: Thermorubin and 2-Hydroxyphenyl Acetic Acid, Aldose Reductase Inhibitors.

ChemInform ◽  
2010 ◽  
Vol 27 (17) ◽  
pp. no-no
Author(s):  
K. HAYASHI ◽  
M. DOMBOU ◽  
M. SEKIYA ◽  
H. NAKAJIMA ◽  
T. FUJITA ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

scholarly journals Pyridothiadiazine derivatives as aldose reductase inhibitors having antioxidant activity

2016 ◽  
Vol 31 (sup1) ◽  
pp. 126-130 ◽  
Author(s):  
Shaojuan Zhu ◽  
Shuzhen Zhang ◽  
Xin Hao ◽  
Xiangyu Qin ◽  
Shagufta Parveen ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

scholarly journals Antioxidant and Hypoglycemic Properties of Seeds of Cucurbitaceae Family from Western Nepal

2019 ◽  
Vol 9 (2) ◽  
pp. 1-5
Author(s):  
Atisammodavardhana Kaundinnyayana ◽  
Anita G.C ◽  
Asmita Banstola ◽  
Kishwor Poudel ◽  
Nirmal Acharya ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Positive Control ◽  
Lagenaria Siceraria ◽  
Benincasa Hispida ◽  
Ic50 Values ◽  
In Vitro Antioxidant Activity

Introduction: Diabetes mellitus is an endocrine and metabolic disorder characterized by the defect in insulin secretion or insulin action or both. The association between diabetes mellitus and oxidative stress is well established. Cucurbitaceae is the largest family containing 120 genera mostly grown for its sweet and juicy fruit in warm climates all over the world. In the present work ethanolic extracts of the seeds of Trichosanthes cucumerina Linn (Chichinno), Lagenaria siceraria (Lauka), Cucurbita pepo (Pharsi), Luffa aegiptiaca (Ghiraula), and Benincasa hispida (Kubindo) collected from Western Nepal has been evaluated for their in vitro antioxidant activity and in vivo hypoglycemic effects. Methods: In vitro antioxidant activity was assessed by using DPPH free radical scavenging activities and their IC50 values were calculated. In vivo hypoglycemic effect was examined on normoglycemic rats. The clinical significance of ethanolic extract at the doses of 250 and 500 mg/kg body weight was investigated in 0, 30, 60, 120 and 180 minutes of oral administration. Metformin treated group was used as the positive control. Results: For DPPH radical scavenging action, the IC50 values of Trichosanthes cucumerina, Luffa aegiptiaca, Benincasa  hispida, Cucurbita pepo, Lagenaria siceraria were found to be 60.72, 127.73, 49.63, 98.16 and 52.46 µg/ml respectively which were compared to the IC50 value of ascorbic acid (Positive control) which was found to be 38.11 µg/ml. The extracts of Benincasa hispida, and were having higher antioxidant activity and tested for in vivo hypoglycemic activity.In vivo administration of two doses of ethanolic extract of Lagenaria siceraria reduced the level of blood glucose while the best result was obtained at 250 mg/kg. Conclusions: Present study revealed promising antioxidant and hypoglycemic activity of ethanolic extract of Lagenaria siceraria. The further exploration of Lagenaria siceraria for its effective use in the traditional medicinal system is essential.

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 Uji Aktivitas Antioksidan Ekstrak Buah Semangka (Citrullus lanatus)

2018 ◽  
Vol 7 (2) ◽  
pp. 96
Author(s):  
Sri Mariani ◽  
Nurdin Rahman ◽  
Supriadi Supriadi
Keyword(s):  
Antioxidant Activity ◽  
Vitamin C ◽  
Antioxidant Activities ◽  
Citrullus Lanatus ◽  
Natural Antioxidants ◽  
Positive Control ◽  
Control Measurement ◽  
Ic50 Value ◽  
Ic50 Values

The aim of this study is determine the IC50 extracts values of white peel and flesh of red watermelon, white peel and flesh of yellow watermelon as antioxidants. To determine antioxidant activities DPPH reagent was used as well as UV-Vis Spectrophotometry was used to measure vitamin C as a positive control measurement. The samples mixed with ethanol in various concentration of 5, 15, 25 and 35 mg/L. The results showed that the IC50 values for each extract of red watermelon flesh, yellow watermelon flesh, white peel of red watermelon, and white peel of yellow watermelon were 16.619 mg/L, 16.575 mg/L, 14.729 mg/L, and 16.782 mg/L, respectively. Vitamin C as the positive control has IC50 value of 9.526 mg/L. These IC50 values showed that vitamin C had higher antioxidant activity than watermelon extracts, but the extracts of watermelon still categorized in strong natural antioxidants. This study concluded that watermelon is good to be consumed because it is a very strong antioxidant.

Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity

2020 ◽  
Vol 28 (20) ◽  
pp. 115699
Author(s):  
Huan Chen ◽  
Xin Zhang ◽  
Xiaonan Zhang ◽  
Zhenya Fan ◽  
Wenchao Liu ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Aldose Reductase ◽  
Aldose Reductase Inhibitors ◽  
Reductase Inhibitors

scholarly journals OPTIMASI WAKTU PENGERINGAN TERHADAP AKTIVITAS ANTIOKSIDAN EKSTRAK ETANOL RIMPANG TEMU PUTIH (Curcuma aromatica Salisb)

2017 ◽  
Vol 4 (2) ◽  
pp. 143
Author(s):  
Nia Yuliani ◽  
Mamay Maslahat ◽  
Puji Lestari
Keyword(s):  
Antioxidant Activity ◽  
Ethanol Extract ◽  
Positive Control ◽  
Drying Process ◽  
Tropical Country ◽  
Drying Time ◽  
Dpph Method ◽  
Ic50 Values ◽  
Herbal Plants ◽  
Anti Oxidant

Optimization of The Drying Time of The Anti-Oxidant Activity of The Ethanol Extract of The Rhizomes of Temu Putih (Curcuma aromatica Salisb)Indonesia is a tropical country that has many varieties of medicinal herbal plants. One of them is Curcuma aromatica Salisb. It has a secondary metabolite that acts as an antioxidant. The metabolite will degrade if it goes through a long drying process. The Curcuma aromatica Salisb rhizome is dried at a temperature of 65oC with variant time durations : 22, 23, 24, 25 and 26 hours. The dried rhizome is extracted with ethanol as the solvent and the results are 14.16%, 11,89%, 15,95%, 12,10% dan 11,97% respectively. Phytochemical test shows the existence of alkaloids and flavonoids in the extract. The measurement of antioxidant activity is done using the DPPH method with a spectrophotometer at 517 nm wavelength. The result is then compared to Quercetin as the positive control. The IC50  values of Quercetin, extracts of Curcuma after 22, 23, 24, 25 and 26 hours after drying respectively are 6,47µ g/ml , 160,54µ g/ml, 133,17µ g/ml, 117,81µ g/ml, 144,69 µ g/ml, dan 157,7 µ g/ml. The extracts after 23-25 hours of drying have medium antioxidant levels, while the ones with 22 and 26 hours of drying have low antioxidant levels. The duration of drying affects the antioxidant activity of Curcuma aromatica salisb extract. The highest value of IC50 is achieved on the positive control of Quercetin and followed by the Curcuma extract with 24 hours of drying.Key words : ethanol, Curcuma aromatica salisb, drying duration, antioxidant activity ABSTRAKIndonesia merupakan negara tropis yang memiliki berbagai macam tanaman obat. Salah satunya adalah temu putih (Curcuma aromatica Salisb). Temu putih mengandung senyawa metabolit sekunder yang bermanfaat sebagai antioksidan. Senyawa metabolit sekunder akan rusak bila dikeringkan dengan waktu yang lama.Rimpang temu putih dikeringkan pada suhu 65oC dengan variasi waktu 22, 23, 24, 25 dan 26 jam. Simplisia temu putih diekstrak dengan pelarut etanol diperoleh rendemen berturut-turut, 14,16%, 11,89%, 15,95%, 12,10% dan 11,97%. Uji Fitokimia menunjukkan adanya alkaloid dan flavonoid pada ekstrak etanol rimpang temu putih. Penentuan aktivitas antioksidan dilakukan dengan metode DPPH menggunakan spektrofotometer pada panjang gelomban g 517 nm. Hasilnya dibandingkan dengan Kuersetin sebagai kontrol positif. Nilai IC50 Kuersetin, ekstrak etanol rimpang temu putih 22, 23 24, 25 dan 26 jam berturut-turut adalah 6,47μg/ml , 160,54μg/ml, 133,17μg/ml, 117,81μg/ml, 144,69 μg/ml, dan 157,7 μg/ml. Ekstrak etanol rimpang temu putih pengeringan 23-25 jam memiliki aktivitas antioksidan sedang, sedangkan pengeringan 22 dan 26 jam memiliki aktivitas antioksidan lemah. Lama proses pengeringan mempengaruhi aktivitas antioksidan ekstrak etanol rimpang temu putih. IC50 terbaik diperoleh pada standar positif Kuersetin kemudian pada ekstrak etanol rimpang temu putih pengeringan 24 jam.Kata Kunci : etanol, Curcuma aromatica Salisb, lama pengeringan, aktivitas antioksidan

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