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Objective: To investigate the chemical constituents of the leaves of Phyllanthus acidus. Methods: All compounds were isolated by silica gel and Sephadex LH-20 gel column chromatographies as well as semi-preparative HPLC, and their structures were elucidated on the basis of physicochemical properties and spectral data. Results: Ten compounds were isolated and identified as 3α-cinnamoyloxyurs-20(29)-en-18β-ol (1), phyllanthol (2), maslinic acid (3), ovoideal E (4), quercetin-3-rhamnoside (5), 4-hydroxybenzoic acid (6), methyl 4-hydroxyphenylacetate (7), 4-O-(β-glucopyranosyloxy)-benzoic acid (8), thioacetic anhydride (9), L-pyroglutamic acid (10). Conclusion: Compound 1 is a new compound named as phyllanacidol B, and compounds 3-10 are obtained from P. acidus for the first time.
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Objective: To determine the effect of extracts from Phyllanthus acidus (P. acidus) (L.) Skeels and Rhinacanthus nasutus (R. nasutus) (L.) Kurz leaves on melanogenesis and the underlying mechanism in normal human epidermal melanocytes (NHEM) and a reconstitutive skin model. Methods: NHEM and a reconstitutive skin model were stimulated with ethanol extracts of P. acidus (L.) Skeels and R. nasutus (L.) Kurz leaves. mRNA expression of microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), tyrosinase-related protein 1 (TYRP1) and dopachrome tautomerase (DCT) were examined by real-time PCR. The melanin content in NHEM was also measured. Moreover, protein levels of tyrosinase were determined using western blot analysis. Results: In NHEM and the reconstitutive skin model, ethanol extracts from P. acidus (at 12.5 and 25.0 μg/mL) and R. nasutus (at 6.25 and 12.50 μg/mL) significantly diminished mRNA expression of MITF, TYR, TYRP1 and DCT in a concentration-dependent manner. P. acidus and R. nasutus extracts also reduced the amount of melanin in α-MSH-stimulated NHEM. Moreover, P. acidus and R. nasutus extracts markedly suppressed tyrosinase at the translational level in the reconstitutive skin model. Conclusions: P. acidus and R. nasutus extracts significantly reduced melanogenesis in NHEM and the reconstitutive skin model, suggesting that P. acidus and R. nasutus extracts can inhibit melanin synthesis through downregulation of MITF, TYR, TYRP1 and DCT. Therefore, the ethanol extracts of P. acidus and R. nasutus contain compounds that have the potential for development as a skin lightening agent for the treatment of hyperpigmentation disorder or melasma.
RESUMEN
Objective: To determine the effect of extracts from Phyllanthus acidus (P. acidus) (L.) Skeels and Rhinacanthus nasutus (R. nasutus) (L.) Kurz leaves on melanogenesis and the underlying mechanism in normal human epidermal melanocytes (NHEM) and a reconstitutive skin model. Methods: NHEM and a reconstitutive skin model were stimulated with ethanol extracts of P. acidus (L.) Skeels and R. nasutus (L.) Kurz leaves. mRNA expression of microphthalmia-associated transcription factor (MITF), tyrosinase (TYR), tyrosinase-related protein 1 (TYRP1) and dopachrome tautomerase (DCT) were examined by real-time PCR. The melanin content in NHEM was also measured. Moreover, protein levels of tyrosinase were determined using western blot analysis. Results: In NHEM and the reconstitutive skin model, ethanol extracts from P. acidus (at 12.5 and 25.0 μg/mL) and R. nasutus (at 6.25 and 12.50 μg/mL) significantly diminished mRNA expression of MITF, TYR, TYRP1 and DCT in a concentration-dependent manner. P. acidus and R. nasutus extracts also reduced the amount of melanin in α-MSH-stimulated NHEM. Moreover, P. acidus and R. nasutus extracts markedly suppressed tyrosinase at the translational level in the reconstitutive skin model. Conclusions: P. acidus and R. nasutus extracts significantly reduced melanogenesis in NHEM and the reconstitutive skin model, suggesting that P. acidus and R. nasutus extracts can inhibit melanin synthesis through downregulation of MITF, TYR, TYRP1 and DCT. Therefore, the ethanol extracts of P. acidus and R. nasutus contain compounds that have the potential for development as a skin lightening agent for the treatment of hyperpigmentation disorder or melasma.
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Objective: To evaluate analgesic, anti-inflammatory and in vitro antioxidant potential and determine total phenolic, total flavonoid content of leaves extracts of Phyllanthus acidus, a folk medicinal plant of India. Methods: Anti-inflammatory activity was evaluated using carrageenan induced paw oedema, cotton pellet induced granuloma, membrane stabilizing activity method. Analgesic activity of the extracts was estimated against acetic acid induced writhing, tail immersion method, formalin test. Free radical scavenging and antioxidant potential of the extracts of Phyllanthus acidus leaves was performed using several in vitro and ex vivo assay models. Total phenolic and total flavonoid contents of the extracts were determined using standard chemical methods. Results: The extracts exhibited significant anti-inflammatory and analgesic activities at dose dependent manner. Methanol extract at a dose of 500 mg/kg showed superior activity which was comparable with the standard drugs. Ethyl acetate extract showed moderate activity while petroleum ether extract showed least activity. Total phenolic and total flavonoid content in methanol extract were 73.08±0.682 mg GAE/g and 61.28±0.062 mg QE/g respectively. The extracts possess significant antioxidant activity, methanol extract showed highest IC50 value. The contents of flavonoids and phenolic compounds could be correlated with the antioxidant, analgesic and anti-inflammatory activities observed for Phyllanthus acidus leaves. Conclusion:Our findings suggest that Phyllanthus acidus contains potential antioxidant, analgesic and anti-inflammatory compounds which could be tested as drug candidates against oxidative stress, pain and inflammation related pathological diseases.
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In the present work, the ethanol extract of the barks of Phyllanthus acidus L. (Family: Euphorbiaceae) were investigated for preliminary phytochemical screening, cytotoxicity and antibacterial activities. The presence of phytochemical constituents was identified by characteristic changes using standard procedure. Brine shrimp lethality (BSL) bioassay was used to investigate the cytotoxic effects and the agar disc diffusion method was used for antimicrobial assay of the plant extract. The phytochemical screening of ethanol extract of the plant showed the presence of alkaloids, glycosides and steroids. The ethanol extracts of Phyllanthus acidus L. bark showed cytotoxicity with LC50 and LC90 values of 501.19μg/mL and LC90: 794.33μg/mL, respectively. The extract of Phyllanthus acidus L. bark showed significant antibacterial activity against gram negative bacteria only such as such as E. coli (19.25 ± 0.54mm), S. typhi (32.08 ± 0.51mm) and Vibrio cholerae (16.42 ± 0.42mm). The obtained results showed a potential source of biologically active compounds which can be used as antibacterial agents.
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The present study was carried out to evaluate the phytochemical properties, antimicrobial and cytotoxic as well as antioxidant activities of the chloroform extract.of Phyllanthus acidus fruit. Phytochemical screening showed confirmation of saponin, alkaloid, tannin and flavanoid. Antioxidant activity of PACF (Phyllanthus acidus chloroform extract) was assessed by using 1,1-diphenyl-2- picrylhydrazyl radical(DPPH),reducing power, cupric reducing antioxidant capacity and antioxidant activity increased in a concentration dependent manner. In DPPH radical scavenging assay IC50 value found 2745.86 μg mL−1 and compared to ascorbic acid with 13.37 μg mL−1. In brine shrimp lethality bioassay it showed good result with LC50 value 4.46 μg/ml. Antibacterial activity of plant extract was carried out using disc diffusion method with eleven pathogenic bacteria. This extract showed narrow spectrum activity aligned with Shigella dysenteriae, Escherichia coli, Staphylococcus aureus and Sarcina lutea at concentration of 500 μg/disc in comparison with standard kanamycin. The range of zone of inhibition of chloroform extract was 0.5 to 2.5 mm.