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Metal Chelating, Inhibitory DNA Damage, and Anti-Inflammatory Activities of Phenolics from Rambutan (Nephelium lappaceum) Peel and the Quantifications of Geraniin and Corilagin.

Whereas the preparation and biological properties of rambutan peel phenolics (RPP) were explored in our previous studies, the metal chelating, inhibitory DNA damage, and anti-inflammatory activities of RPP were evaluated and the important phenolics of RPP quantified in this study. Results showed that RPP had high Fe2+ and Cu2+-chelating activities with EC50 of 0.80 mg/mL and 0.13 mg/mL, respectively. RPP effectively decreased the production of hydroxyl radical with IC50 of 62.4 µg/mL. The protective effects of RPP against AAPH-induced DNA damage were also explored. RPP efficiently inhibited peroxyl radical-induced plasmid DNA strand breakage. The anti-inflammatory effects of RPP were determined using a lipopolysaccharide (LPS)-induced RAW 264.7 cell model. RPP significantly inhibited the production of nitric oxide (NO) and controlled the levels of inducible NO synthase mRNA in LPS-induced RAW 264.7 cells. The inhibitory activity increased in a dose-dependent manner. The above bioactivity of RPP was associated with its phenolic content and phenolic profiles. Furthermore, the contents of geraniin and corilagin in RPP were determined by an ultra-high performance liquid chromatography coupled with triple quadruple mass spectrometry (UPLC-QQQ-MS), showing 140.02 and 7.87 mg/g extract dry weight. Thus, RPP has potential applications as a novel nutraceutical and functional food in health promotion.

Protective Effects of Rambutan (Nephelium Lappaceum) Peel Phenolics on H O -induced Oxidative Damages in HepG2 Cells and D-Galactose-Induced Aging Mice.

Rambutan peel phenolic (RPP) extracts were prepared via dynamic separation with macroporous resin. The total phenolic content and individual phenolics in RPP were determined. Results showed that the total phenolic content of RPP was 877.11 mg gallic acid equivalents (GAE)/g extract. The content of geranin (122.18 mg/g extract) was the highest among those of the 39 identified phenolic compounds. RPP protected against oxidative stress in H O -induced HepG2 cells in a dose-response manner. The inhibitory effects of RPP on cell apoptosis might be related to its inhibitory effects on the generation of intracellular reactive oxygen species and increased effects on superoxide dismutase activity. The in vivo anti-aging activity of RPP was evaluated using an aging mice model that was induced by dgalactose (d-gal). The results showed that RPP enhanced the antioxidative status of experimental mice. Moreover, histological analysis indicated that RPP effectively reduced d-gal-induced liver and kidney tissue damage in a dose-dependent manner. Therefore, RPP can be used as a natural antioxidant and anti-aging agent in the pharmaceutical and food industries.

Geraniin extracted from the rind of Nephelium lappaceum binds to dengue virus type-2 envelope protein and inhibits early stage of virus replication.

Abstract Background The rapid rise and spread in dengue cases, together with the unavailability of safe vaccines and effective antiviral drugs, warrant the need to discover and develop novel anti-dengue treatments. In this study the antiviral activity of geraniin, extracted from the rind of Nephelium lappaceum, against dengue virus type-2 (DENV-2) was investigated. Methods Geraniin was prepared from Nephelium lappaceum rind by reverse phase C-18 column chromatography. Cytotoxicity of geraniin towards Vero cells was evaluated using MTT assay while IC50 value was determined by plaque reduction assay. The mode-of-action of geraniin was characterized using the virucidal, attachment, penetration and the time-of-addition assays’. Docking experiments with geraniin molecule and the DENV envelope (E) protein was also performed. Finally, recombinant E Domain III (rE-DIII) protein was produced to physiologically test the binding of geraniin to DENV-2 E-DIII protein, through ELISA competitive binding assay. Results Cytotoxicity assay confirmed that geraniin was not toxic to Vero cells, even at the highest concentration tested. The compound exhibited DENV-2 plaque formation inhibition, with an IC50 of 1.75 μM. We further revealed that geraniin reduced viral infectivity and inhibited DENV-2 from attaching to the cells but had little effect on its penetration. Geraniin was observed to be most effective when added at the early stage of DENV-2 infection. Docking experiments showed that geraniin binds to DENV E protein, specifically at the DIII region, while the ELISA competitive binding assay confirmed geraniin’s interaction with rE-DIII with high affinity. Conclusions Geraniin from the rind of Nephelium lappaceum has antiviral activity against DENV-2. It is postulated that the compound inhibits viral attachment by binding to the E-DIII protein and interferes with the initial cell-virus interaction. Our results demonstrate that geraniin has the potential to be developed into an effective antiviral treatment, particularly for early phase dengue viral infection.

Antioxidant and antibacterial activities of Nephelium lappaceum L. Extracts.

Ether, methanolic and aqueous extracts of lyophilized rambutan (Nephelium lappaceum L.) peels and seeds were evaluated for phenolic contents, antioxidant and antibacterial activities. High amounts of phenolic compounds were found in the peel extracts and the highest content was in the methanolic fraction (542.2 mg/g dry extract). Several potential antioxidant activities, including reducing power, β-carotene bleaching, linoleic peroxidation and free radical scavenging activity, were evaluated. The peel extracts exhibited higher antioxidant activity than the seed extracts in all methods determined (P < 0.05). The methanolic fraction was found to be the most active antioxidant as shown by their 50% DPPHradical dot inhibition concentration, 4.94 μg/mL. The results indicated this fraction exhibited greater DPPHradical dot radical scavenging activity than BHT and ascorbic acid (0.32 g dry extract/g BHT or ascorbic acid). Antibacterial activity against eight bacterial strains was assessed by disc diffusion and broth macrodilution methods. All peel extracts exhibited antibacterial activity against five pathogenic bacteria. The most sensitive strain, Staphylococcus epidermidis, was inhibited by the methanolic extract (MIC 2.0 mg/mL).

A Review on Nephelium lappaceum L.

Nephelium lappaceum L. (Family- Sapindaceae), popularly known as ‘Rambutan’, is an evergreen tree, native to Malaysia but grown in other parts of the world. The plant has been used as traditional medicine for centuries especially as a remedy for diabetes and high blood pressure. Further, the fruits always remained as a potential source of minerals and other nutrients. A thorough literature survey revealed that the plant possesses several
biological activities such as antidiabetic, analgesic, antiinflammatory, immunomodulatory, antioxidant, anticancer, antimicrobial and antiviral activities against dengue virus. This paper outlines an updated review on this important plant focusing on the traditional uses, phytochemistry and pharmacological aspects that would assist researchers to search scientific information in the future.

Pharmacological effects of gallic acid in health and diseases: A mechanistic review.

Objective(s): Gallic acid is a natural phenolic compound found in several fruits and medicinal plants. It is reported to have several health-promoting effects. This review aims to summarize the pharmacological and biological activities of gallic acid in vitro and animal models to depict the pharmacological status of this compound for future studies. Materials and Methods: All relevant papers in the English language were collected up to June 2018. The keywords of gallic acid, antioxidant, anticancer, antimicrobial, gastrointestinal-, cardiovascular-, metabolic-, neuropsychological-, and miscellaneous- diseases were searched in Google Scholar, PubMed, and Scopus. Results: Several beneficial effects are reported for gallic acid, including antioxidant, anti-inflammatory, and antineoplastic properties. This compound has been reported to have therapeutic activities in gastrointestinal, neuropsychological, metabolic, and cardiovascular disorders. Conclusion: Current evidence confirms the pharmacological and therapeutic interventions of gallic acid in multiple health complications; however, available data are limited to just cellular and animal studies. Future investigations are essential to further define the safety and therapeutic efficacy of gallic acid in humans.