scholarly journals A New Macrolactone, Racemolide Along With Seven Known Compounds With Biological Activities From Mangrove Plant,Lumnitzera racemosa

2019 ◽  
Vol 14 (6) ◽  
pp. 1934578X1986125
Author(s):  
Ahmed Gomaa Gomaa Darwish ◽  
Mamdouh Nabil Samy ◽  
Sachiko Sugimoto ◽  
Hideaki Otsuka ◽  
Katsuyoshi Matsunami

One new macrolide, racemolide (1), was isolated from an MeOH extract of the leaves of Lumnitzera racemosa with 7 known compounds (2-8) by various chromatographic techniques via silica gel, octadecylsilyl column chromatography and high-performance liquid chromatography. The structure of the new compound was determined through a combination of spectroscopic and chemical analyses. The isolated compounds were evaluated for their antileishmanial, hepatoprotective, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities. Compound 1 showed potent antileishmanial activity at inhibition % value of 67.6 ± 1.24% compared with the clinical drug miltefosine (93.3 ± 4.39%). Compounds 1 and 5 possessed moderate hepatoprotective activity against acetaminophen (APAP)-induced hepatotoxicity using human HepG2 cells at protection % value of 21.70 ± 1.97% and 27.5 ± 1.41%, respectively, compared with the standard glycyrrhizin (69.50 ± 3.53%). Compounds 4, 6, 7, and 8 had high DPPH radical scavenging activity (91.10 ± 4.25, 91.53 ± 0.05, 91.91 ± 0.09, and 86.48 ± 2.87%, respectively), while compounds 3 and 5 showed moderate (45.38 ± 3.62% and 62.20 ± 1.47%, respectively), comparable with the standard trolox (89.21 ± 5.88%). These results suggest that the new compound, racemolide (1), and known compounds (3-8) are valuable as promising antileishmanial, hepatoprotective, and anti-oxidant agents.

2021 ◽  
Vol 51 (5) ◽  
Author(s):  
Lucas Dutra Zani da Silva Souza ◽  
Stéphane Raquel Almeida Velande da Fonseca ◽  
Ariana Ferrari ◽  
Daniele Fernanda Felipe

ABSTRACT: Plants that contain antioxidant compounds have attracted increasing interest for their vital role in the attenuation of oxidative damage caused by free radicals and in the treatment of various diseases. The present study investigated the β-ecdysone content and the antioxidant activity of Brazilian ginseng (Pfaffia glomerata) extracts obtained from inflorescences, stems, and roots. The P. glomerata extracts were tested for antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method, β-carotene bleaching test, and phosphomolybdenum method. The β-ecdysone content of P. glomerata extracts was measured by high-performance liquid chromatography (HPLC). The P. glomerata inflorescences showed the strongest DPPH radical scavenging activity and the strongest antioxidant activity in the β-carotene bleaching assay and phosphomolybdenum test. The roots showed the lowest antioxidant capacity in all of the assays. The concentration of β-ecdysone in the plant organs followed the following decreasing order: inflorescences > stems > roots. The present study showed that P. glomerata inflorescence extract had high antioxidant capacity that could be attributed to the presence of β-ecdysone.


Marine Drugs ◽  
2020 ◽  
Vol 18 (11) ◽  
pp. 574
Author(s):  
Chien Thang Doan ◽  
Thi Ngoc Tran ◽  
Van Bon Nguyen ◽  
Anh Dzung Nguyen ◽  
San-Lang Wang

Microbial fermentation of by-products is a renewable and efficient technique in the development of a range of useful products. In this study, protease synthesis by Paenibacillus sp. TKU052 was carried out on culture media containing some common seafood processing by-products (SPBPs) as the sole source of carbon and nitrogen (C/N). The most suitable C/N nutrition source for the production of proteases was found to be 3.0% (w/v) demineralized crab shells powder (deCSP) and maximal enzyme activity of 4.41 ± 0.16 U/mL was detected on the third day of the culture. Two proteases (P1 and P2) with a similar molecular weight of 31 kDa were successfully isolated and purified from the 3-day deCSP-containing medium. Both P1 and P2 exhibited the highest activity of gelatin hydrolysis at pH 6 and 60 °C. The gelatin hydrolysates catalyzed by Paenibacillus TKU052 proteases were evaluated for biological activities, including 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, angiotensin-I converting enzyme (ACE) inhibition, and prebiotic activities. The gelatin hydrolysates expressed 31.76–43.95% DPPH radical scavenging activity and 31.58–36.84% ACE inhibitory activity, which was higher than those from gelatin. Gelatin hydrolysates also showed the growth-enhancing effect on Bifidobacterium bifidum BCRC 14615 with an increase to 135.70–147.81%. In short, Paenibacillus sp. TKU052 could be a potential strain to utilize crab shell wastes to produce proteases for bio-active peptides’ preparation.


2014 ◽  
Vol 79 (5) ◽  
pp. 517-526
Author(s):  
Maya Chochkova ◽  
Assya Georgieva ◽  
Galya Ivanova ◽  
Nadya Nikolova ◽  
Luchia Mukova ◽  
...  

Seven N-hydroxycinnamoyl amides were synthesized by EDC/HOBt coupling of the corresponding substituted cinnamic acids (p-coumaric-, ferulic-, sinapic- and caffeic acids) with influenza antivirals (amantadine, rimantadine and oseltamivir). DPPH (1,1-diphenyl-2-picrylhydrazyl) scavenging abilities and the inhibitory effect on mushroom tyrosinase activity (using L-tyrosine as the substrate) were investigated in vitro. Amongst the synthesized compounds, N-[(E)-3-(3?,4?-dihydroxyphenyl)-2-propenoyl]oseltamivir (1) and N-[(E)-3-(3?,4?-dihydroxyphenyl)-2-propenoyl]rimantadine (4), containing catechol moiety, exhibited the most potent DPPH radical-scavenging activity. Amide (1) displayed also tyrosinase inhibitory effect toward L-tyrosine as the substrate (~50%). Due to its biological activities revealed so far compound (1) can be considered as a promising candidate for a cosmetic ingredient. The synthesized compounds were also investigated for their in vitro inhibitory activity against the replication of influenza virus A (H3N2).


2018 ◽  
Vol 44 (4) ◽  
pp. 515-520
Author(s):  
M Kazemi

Carum copticum L. comprises several relevant species for food, cosmetic, perfumery and pharmaceutical industries. GC/MS analysis of the enential oil of C. copticum revealed γ- terpinene as a major component of C. copticum, with its contribution of 33.85%. Essential oils (EOs) exhibited a significant antimicrobial activity against all tested microbial strains. In addition, the C. copticum oil demonstrated the highest DPPH radical scavenging activity. These results clearly show the antimicrobial and antioxidant effects of the plant essential oil.


2018 ◽  
Vol 15 (2) ◽  
pp. 127-135 ◽  
Author(s):  
Parvesh Singh ◽  
Nomandla Ngcoya ◽  
Ramgopal Mopuri ◽  
Nagaraju Kerru ◽  
Neha Manhas ◽  
...  

Background: Diabetes Mellitus (DM) is a complex metabolic disease illustrated by abnormally high levels of plasma glucose or hyperglycaemia. Accordingly, several α-glucosidase inhibitors have been developed for the treatment of diabetes and other degenerative disorders. While, a coumarin ring has the privilege to represent numerous natural and synthetic compounds with a wide spectrum of biological activities e.g. anti-cancer, anti-HIV, anti-viral, anti-malarial, anti-microbial, anti-convulsant, anti-hypertensive properties. Besides this, coumarins have also shown potential to inhibit α-glucosidase leading to a generation of new promising antidiabetic agents. However, the testing of O-substituted coumarins for α-glucosidase inhibition has evaded the attention of medicinal chemists. Methods: For O-alkylation/acetylation reactions, the hydroxyl coumarins (A-B) initially activated by K2CO3 in dry DMF were reacted with variedly substituted haloalkanes at room temperature under nitrogen. The synthesized compounds were tested for their α-glucosidase (from Saccharomyces cerevisiae) inhibitory activity and anti-oxidant activity using DPPH radical scavenging activity. In silico docking simulations were conducted using CDocker module in DS (Accelrys) to explore the binding modes of the representative compounds in the catalytic site of α-glucosidase. Results: All the coumarin analogues (A1, B1, A2-A10, B2-B8) including their precursors (A-B) were evaluated for their in vitro α-glucosidase inhibition using acarbose as a standard inhibitor. All the mono O-alkylated coumarins (except A1) showed significant (p <0.05) α-glucosidase inhibition relative to the hydroxyl coumarin (A) with IC50 values ranging between 11.084±0.117 to 145.24± 29.22 µg/mL. Compound 7-(benzyloxy)-4, 5-dimethyl-2H-chromen-2-one (A9) bearing a benzyl group (Ph-CH2-) at position 7 showed a remarkable (p <0.05) increase in the activity (IC50 = 11.084±0.117 µg/mL), almost four-fold more than acarbose (IC50 = 40.578±5.999 µg/mL). The introduction of –NO2 group dramatically improved the anti-oxidant activity of coumarin, while the O-alkylation/acetylation decreased the activity. Conclusion: The present study describes the synthesis of functionalized coumarins and their evaluation for α-glucosidase inhibition and antioxidant activity under in vitro conditions. Based on IC50 data, the mono O-alkylated coumarins were observed to be stronger inhibitors of α-glucosidase with respect to their bis O-alkylated analogues. Coumarin (A9) bearing O-benzyloxy group displayed the strongest α-glucosidase inhibition, even higher than the standard inhibitor acarbose. The coumarin (A10) bearing –NO2 group showed the highest anti-oxidant activity amongst the synthesized compounds, almost comparable to the ascorbic acid. Finally, in silico docking simulations revealed the role of hydrogen bonding and hydrophobic forces in locking the compounds in catalytic site of α-glucosidase.


2020 ◽  
Vol 2020 ◽  
pp. 1-16
Author(s):  
Nur Sumirah Mohd Dom ◽  
Nurshieren Yahaya ◽  
Zainah Adam ◽  
Nik Mohd Afizan Nik Abd. Rahman ◽  
Muhajir Hamid

The present study aimed to evaluate the potential of standardized methanolic extracts from seven Ficus deltoidea varieties in inhibiting the formation of AGEs, protein oxidation, and their antioxidant effects. The antiglycation activity was analyzed based on the inhibition of AGEs, fructosamine, and thiol groups level followed by the inhibition of protein carbonyl formation. The antioxidant activity (DPPH radical scavenging activity and reducing power assay) and total phenolic contents were evaluated. After 28 days of induction, all varieties of Ficus deltoidea extracts significantly restrained the formation of fluorescence AGEs by 4.55–5.14 fold. The extracts also reduced the fructosamine levels by 47.0–86.5%, increased the thiol group levels by 64.3–83.7%, and inhibited the formation of protein carbonyl by 1.36–1.76 fold. DPPH radical scavenging activity showed an IC50 value of 66.81–288.04 μg/ml and reducing power activity depicted at 0.02–0.24 μg/ml. The extent of phenolic compounds present in the extracts ranged from 70.90 to 299.78 mg·GAE/g. Apart from that, correlation studies between the activities were observed. This study revealed that seven varieties of Ficus deltoidea have the potential to inhibit AGEs formation and possess antioxidant activity that might be attributed to the presence of phenolic compounds.


2013 ◽  
Vol 781-784 ◽  
pp. 1294-1297 ◽  
Author(s):  
Ping Liu ◽  
Yun Tao Gao ◽  
Jiao Jiao Yu ◽  
Jia Wei Cha ◽  
Dong Mei Zhao ◽  
...  

The UV-Vis absorption spectrum of kaempferol and DPPH was investigated, the optimum determination wavelength and reaction time for determining the DPPH radical scavenging activity of kaempferol was 517 nm and 30 min, respectively. Kaempferol exhibited strong DPPH radical scavenging activity with a IC50 value of 0.004349 mg·mL-1, which is smaller than that of rutin, indicating that kaempferol has a stronger antioxidant activity than rutin.


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