Synthesis and Antioxidant Activity of Novel Series of Naphthoquinone Derivatives Attached to Benzothiophene Moiety

Gouda, Moustafa A.

doi:10.4172/2161-0444.1000143

Cited by 29 publications

(7 citation statements)

References 18 publications

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“…It was inferred that the structural variations bring about change in bioactivity e.g., if halogens (Cl or Br) were substituted in the aromatic ring, it sharply enhanced the antioxidant potency of the compound (Hossain et al, 2009). The radical scavenging activity of naphthoquinones has also been studied and it was found that the antioxidant potential of 2-aminothiophene compounds has increased by introducing the naphthoquinones moiety to the compounds (Gouda et al, 2013). In the present study, among four PAN derivatives tested, the nitro and bromo derivatives have shown the better radical scavenging activity as compared to the chloro derivative, however, the methyl derivative has shown no activity at all.…”

Section: Biology: Antioxidant and Hypoglycaemic Potentialmentioning

confidence: 99%

Synthesis and evaluation of 2-phenylamino-1,4-naphthoquinones derivatives as potential hypoglycaemic agents

et al. 2024

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Due to the severe side effects revealed by most of the currently used antidiabetic medicines, search for finding new and safe drugs to manage diabetes is continued. Naphthoquinones possessing strong antioxidant properties have been employed as candidates for diabetes therapy. Present study is aimed at finding the antioxidant and hypoglycaemic potential of some novel derivatives of 2-phenylamino-1,4-naphthoquinones (PAN) including chloro, nitro, methyl and bromo (5a-d) derivatives synthesized by single pot experiment. Product crystals were purified by TLC and characterized by FT-IR. The antioxidant potential of the compounds was assayed through DPPH radical scavenging and reducing power activities noted as UV-vis. absorbance. The DPPH assay has showed the powerful antioxidant activity of nitro and bromo derivatives, while the nitro derivative showed the significant reduction potential towards FRAP assay. Hypoglycaemic potential of the compounds was studied in rat animal model. All synthesized compounds revealed better hypoglycaemic activity; however, the chloro-derivative exhibited the more potent hypoglycaemic activity showing about 43% reduction in the mean blood glucose levels of the treated animals. As the bioreduction of naphthoquinones may be influenced by changing its redox properties, it has been noticed that the e-donating resonance effect (+R) of ‘chloro’ group has shown the significant effects on biological activity through stabalization of its imine form which limits the potential of generation of free radicals during bioreduction of quinones and thus has been proposed as the reason of its hypoglycaemic activity. Future studies employing the properties of e-donating groups of PAN may optimize the drug-receptor interaction for better drug designing and drug development strategies against diabetes and also for the clinical trials.

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Section: Biology: Antioxidant and Hypoglycaemic Potentialmentioning

confidence: 99%

Synthesis and evaluation of 2-phenylamino-1,4-naphthoquinones derivatives as potential hypoglycaemic agents

et al. 2024

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“…2016). Fenol (C 6 H 5 OH) atau asam karbolat, merupakan kandungan lain dari tomat, yang terdiri dari asam aromatic dan flavonoid berperan sebagai radical scavenging dengan bertindak sebagai nitrogen untuk mencegah dan memecah siklus pembentukan radikal bebas sehingga mencegah kematian sel (Gouda et al,. 2013).…”

Section: Hasil Dan Pembahasan Pengaruh Pemberian Ekstrak Tomat (unclassified

Pengaruh Pemberian Ekstrak Tomat (Lycopersicon esculentum) Terhadap Gambaran HistopatologiI Hepar Tikus Putih (Rattus norvegicus) Jantan Galur Wistar Yang Diinduksi Monosodium Glutamat (MSG)

Vidiyanti

2020

mul. AGRI-TEK. mul. ind. ilmu. ilmu. ind

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ABSTRAKPENGARUH PEMBERIAN EKSTRAK TOMAT (Lycopersicon esculentum) TERHADAP GAMBARAN HISTOPATOLOGI HEPAR TIKUS PUTIH (Rattus norvegicus) JANTAN GALUR WISTAR YANG DIINDUKSI MONOSODIUM GLUTAMAT (MSG)Regga Arma VidiyantiMonosodium glutamat (MSG) adalah penambah rasa makanan yang telah banyak dikonsumsi masyarakat di seluruh dunia, tetapi bila dikonsumsi secara berlebih dapat menimbulkan kerusakan berbagai organ, diantaranya adalah hepar dikarenakan didalam hepar terjadi metabolisme obat dan toksikasi. Efek MSG dilaporkan dapat menyebabkan stress oksidatif. Efek toksik terhadap hepar dapat mengakibatkan terjadinya peroksidase lipid, serta perubahan morfologi jaringan hati yang ditandai dengan gangguan arsitektur hati, vakuolisasi, degenerasi, dan atrofi sel hati. Untuk mengantisipasi kerusakan hepar, diperlukan antioksidan. Salah satu sumber antioksidan adalah tomat.Penelitian ini bertujuan untuk mengetahui efek ekstrak tomat (Lycopersicon esculentum) terhadap gambaran histopatologi hepar tikus putih (Rattus norvegicus) jantan galur Wistar yang diinduksi MSG. Sampel yang digunakan sebanyak 24 ekor tikus putih (Rattus norvegicus) jantan galur Wistar yang dibagi menjadi 3 kelompok: (1) kelompok hewan coba yang diberi pakan standar; (2) kelompok hewan coba yang diberi MSG 5 mg/gBB/hari pada hari ke-1 s/d hari ke-14; dan (3) kelompok hewan coba yang diberi ekstrak tomat dosis 40 mg/kgBB dan MSG 5 mg/gBB/hari pada hari ke-1 s/d hari ke-14. Pada hari ke-15, hewan coba dikorbankan dan dilakukan pembuatan preparat hepar dan pemeriksaan gambaran mikroskopis. Uji analisis menggunakan Kruskal-Wallis dan Mann Whitney.Hasil uji Mann-Whitney menunjukkan perbedaan bermakna derajat kerusakan hepar pada kelompok hewan coba yang diberi pakan standar (rerata=1) dengan kelompok hewan coba yang diberi MSG (rerata=3,5) (p=0,001). Hasil uji Mann-Whitney menunjukkan perbedaan tidak bermakna derajat kerusakan hepar pada kelompok hewan coba yang diberi MSG (rerata=3,5) dengan kelompok hewan coba yang diberi MSG dan ekstrak tomat (rerata=3,125) (p=0,344).Kesimpulan dari hasil penelitian menunjukan bahwa MSG meningkatkan secara bermakna derajat kerusakan hepar yang digambarkan melalui gambaran histopatologi hepar dan ekstrak tomat (Lycopersicon esculentum) dapat menurunkan secara tidak bermakna derajat kerusakan hepar yang digambarkan melalui gambaran histopatologi hepar karena tomat memiliki flavonoid, vitamin C, fenol, likopen yang berfungsi sebagai antioksidan.Kata kunci : Monosodium glutamat, tomat (Lycopersicon esculentum), gambaran histopatologi hepar. ABSTRACTTHE EFFECT OF TOMATO EXTRACT (Lycopersicon esculentum) IN LIVER HISTOPATHOLOGICAL APPEARANCE ON WHITE RATS (Rattus norvegicus) WISTAR STRAIN MALE INDUCED BY MONOSODIUM GLUTAMAT (MSG)Regga Arma Vidiyanti Monosodium glutamate (MSG) is a food flavor enhancer that has been consumed by people all over the world, but if consumed excessively it can cause damage to various organs, including liver because drug metabolism and toxicity occur in the liver. The effect of MSG is reported to cause oxidative stress. Toxic effects on the liver can result in lipid peroxidase, as well as morphological changes in liver tissue characterized by impaired liver architecture, vacuolization, degeneration, and liver cell atrophy. To anticipate liver damage, antioxidants are needed. One of the source of antioxidants is tomatoes. This study aims to determine the effect of tomato extract (Lycopersicon esculentum) on the liver histopathology on white rats (Rattus norvegicus) Wistar strain male induced by MSG. The samples used were 24 white rats (Rattus norvegicus) Wistar strain male which were divided into 3 groups: (1) the experimental group of animals fed standard feed; (2) the experimental groups given MSG 5 mg / gBB / day on day 1 to day 14; and (3) the experimental group given a tomato extract dose of 40 mg / kgBB and MSG 5 mg / gBB / day on day 1 to day 14. On the 15th day, experimental animals were sacrificed and liver preparations were made and microscopic images were examined. The Test analysis of this study using Kruskal-Wallis and Mann Whitney. The results of the Mann-Whitney test showed that there is significant differences in the degree of liver damage in the experimental group given standard feed (mean = 1) with the experimental group given MSG (mean = 3.5) (p = 0.001). The Mann-Whitney test results showed there is no significant difference in the degree of liver damage in the experimental group given MSG (mean = 3.5) with the experimental group given MSG and tomato extract (mean = 3.125) (p = 0.344). The Conclusions of the results showed that MSG significantly increased the degree of liver damage described by liver histopathology and tomato extract (Lycopersicon esculentum) it can significantly reduce the degree of liver damage described by liver histopathology because tomatoes have flavonoids, vitamin C, phenol, Lycopene as an antioxidant. Keywords: Monosodium glutamate, tomatoes (Lycopersicon esculentum), liver histopathological appearance.

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“…A great deal of attention has been paid to 2-amino-thiophenes recently, owing to improvements in their synthetic methods, stability, availability, and structural simplicity, which makes them an important moiety in pharmaceuticals [18,19]. Furthermore, antifungal [20], antibacterial [21,22], antileishmanial [23], anxiolytic [24], anti-inflammatory [25], antiplatelet [26], antioxidant [27], antiandrogenic [28], and anti-diabetes [29] actions have been revealed for thiophene and its analogues.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Pharmacological Evaluation, and In-Silico Studies of Thiophene Derivatives

Mishra¹,

Kumar²,

Sachan³

2021

Oncologie

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Synthesis and Antioxidant Activity of Novel Series of Naphthoquinone Derivatives Attached to Benzothiophene Moiety

Cited by 29 publications

References 18 publications

Synthesis and evaluation of 2-phenylamino-1,4-naphthoquinones derivatives as potential hypoglycaemic agents

Synthesis and evaluation of 2-phenylamino-1,4-naphthoquinones derivatives as potential hypoglycaemic agents

Pengaruh Pemberian Ekstrak Tomat (Lycopersicon esculentum) Terhadap Gambaran HistopatologiI Hepar Tikus Putih (Rattus norvegicus) Jantan Galur Wistar Yang Diinduksi Monosodium Glutamat (MSG)

Synthesis, Pharmacological Evaluation, and In-Silico Studies of Thiophene Derivatives

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