Pegylated azelaic acid: Synthesis, tyrosinase inhibitory activity, antibacterial activity and cytotoxic studies

Abstract Background Dental caries and periodontal disease are the most common chronic infectious oral diseases in the world. Acacia nilotica was commonly known in Sudan as Garad or Sunt has a wide range of medicinal uses. In the present study, antibacterial activity of oral bacteria (Streptococcus sobrinus and Porphyromonas gingivalis), inhibitory activity against glucosyltransferase (GTF) enzyme and antioxidant activity were assayed for methanolic crude extract of A. nilotica bark and its fractions. Methods Methanoilc crude extract of A. nilotica bark was applied to a Sephadex LH-20 column and eluted with methanol, aqueous methanol, and finally aqueous acetone to obtain four fractions (Fr1- Fr4). Furthermore, the crude extract and fractions were subjected to analytical high performance liquid chromatography (HPLC). The crude extract and its fractions were assayed for antibacterial activity against S. sobrinus and P. gingivalis using a microplate dilution assay method to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC), as well as GTF inhibition and antioxidant activity using ABTS radical scavenging method. Results Fractions (Fr1 and Fr2) exhibited MIC values of 0.3 mg/ml against the P. gingivalis. Additionally, Fr2 displayed MBC value of 1 mg/ml against two types of bacteria. Fr4 showed an especially potent GTF inhibitory activity with IC50 value of 3.9 μg/ml. Fr1 displayed the best antioxidant activity with IC50 value of 1.8 μg/ml. The main compound in Fr1 was identified as gallic acid, and Fr2 was mostly a mixture of gallic acid and methyl gallate. Conclusions The results obtained in this study provide some scientific rationale and justify the use of this plant for the treatment of dental diseases in traditional medicine. A. nilotica bark, besides their antibacterial potentiality and GTF inhibitory activity, it may be used as adjuvant antioxidants in mouthwashes. Further studies in the future are required to identify the rest of the active compounds.

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The C‐terminally shortened analogs of a hexapeptide derived from Lingzhi hydrolysate with enhanced tyrosinase‐inhibitory activity

Archiv der Pharmazie ◽

10.1002/ardp.202100204 ◽

2021 ◽

Author(s):

Sucheewin Krobthong ◽

Yodying Yingchutrakul ◽

Pawitrabhorn Samutrtai ◽

Kiattawee Choowongkomon

Keyword(s):

Inhibitory Activity ◽

Tyrosinase Inhibitory Activity

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Insecticidal activity of forty-seven marine algae species from the Mediterranean, Aegean, and Sea of Marmara in connection with their cholinesterase and tyrosinase inhibitory activity

South African Journal of Botany ◽

10.1016/j.sajb.2021.06.038 ◽

2021 ◽

Author(s):

Mehtap Kilic ◽

Ilkay Erdogan Orhan ◽

Gokcen Eren ◽

Emine Sukran Okudan ◽

Alden S. Estep ◽

...

Keyword(s):

Insecticidal Activity ◽

Inhibitory Activity ◽

Marine Algae ◽

Sea Of Marmara ◽

Tyrosinase Inhibitory Activity ◽

The Mediterranean

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Essential oils bearing specialized metabolites with potential tyrosinase inhibitory activity

10.1055/s-0041-1736962 ◽

2021 ◽

Author(s):

Francesca Capetti ◽

Cecilia Cagliero ◽

Arianna Marengo ◽

Giulia Mastellone ◽

Carlo Bicchi ◽

...

Keyword(s):

Essential Oils ◽

Inhibitory Activity ◽

Tyrosinase Inhibitory Activity ◽

Specialized Metabolites

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Tyrosinase Inhibitory Activity of Flavonoids from Artocarpus Lowii King

Jurnal Teknologi ◽

10.11113/jt.v71.2711 ◽

2014 ◽

Vol 71 (1) ◽

Author(s):

Shajarahtunnur Jamil ◽

Siti Awanis Abdullah ◽

Siti Mariam Abdul Lathiff ◽

Hasnah Mohd Sirat

Keyword(s):

Inhibitory Activity ◽

Kojic Acid ◽

Mushroom Tyrosinase ◽

Tyrosinase Inhibitory Activity ◽

Crude Extracts ◽

Ic50 Value ◽

Microplate Reader

Tyrosinase inhibitory activity was studied on the crude extracts and flavonoids successfully isolated from the leaves and heartwoods of Artocarpus lowii King. The flavonoids were fully characterized spectroscopically as isobavachalcone (1), 4-hydroxyonchocarpin (2), 2',4'-dihydroxy-4-methoxy-3'-prenyldihydrochalcone (3), 2',4'-dihydroxy-3,4-(2",2"-dimethylchromeno)-3'-prenyldihydrochalcone (4), artocarpin (5), cycloheterophyllin (6) and 4',5-dihydroxy-6,7-(2,2-dimethylpyrano)-2'-methoxy-8-γ,γ-dimethyl allylflavone (7). Tyrosinase inhibitory activity of the samples was determined against mushroom tyrosinase using ELISA microplate reader. Cycloheterophyllin (6) exhibited an excellent inhibitory activity against mushroom tyrosinase comparable to the standard kojic acid with the IC50 value of 52.5 µg/mL (88.3%).

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