• Title/Summary/Keyword: asiatic acid

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Advanced Formulation and Pharmacological Activity of Hydrogel of the Titrated Extract of C. Asiatica

  • Hong Soon-Sun;Kim Jong-Ho;Li Hong;Shim Chang-Koo
    • Archives of Pharmacal Research
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    • v.28 no.4
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    • pp.502-508
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    • 2005
  • Titrated extract of Centella asiatica (TECA) contains three principal ingredients, asiaticoside (AS), asiatic acid (AA), and madecassic acid (MA). These components are known to be clinically effective on systemic scleroderma, abnormal scar formation, and keloids. However, one problem associated with administration of TECA is its low solubility in aqueous as well as oil medium. In this study, various nonionic surfactants and bile salts as anionic surfactant were tested and screened for solubilizing TECA with a view to developing topical hydrogel type of ointment which is stable physicochemically, and has better pharmacological effects. When TECA was incorporated into various nonionic surfactant systems, labrasol had the most potent capacity for solubilizing TECA. In cases of bile salt systems, Na-deoxycholate (Na-DOC) had foremost solubilizing capacity, even more than labrasol. In differential scanning calorimetric study, the peaks of AA, MA, AS and Na-DOC disappeared at the coprecipitate of $1\%$ TECA and $1\%$ Na-DOC, suggesting the optimum condition of Na-DOC for solubilizing TECA. When the physicochemical stability of hydrogel containing this mixture was assessed, it was stable at room temperature for at least one month. Pharmacologically it significantly decreased the size of wound area at the $9^{th}$ day when applied to the wound area of rat dorsal skin. Taken together, solubility of TECA was dramatically improved by using non ionic and anionic surfactant systems, and Na-DOC was found to be the most effective solubilizer of TECA in formulating a TECA-containing hydrogel typed ointment. Moreover this gel was considered to be applicable to clinical use for wound healing effect.

Anti-oxidative and Anti-bacterial Constituents from the Extracts of Rhododendron weyrichii Leaves (참꽃나무 잎 추출물 유래 항산화 및 항균 활성 성분)

  • Kim, Jung Eun;Jo, Seong Mi;Lee, Nam Ho
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.45 no.4
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    • pp.341-351
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    • 2019
  • In this study, we investigated anti-oxidative and anti-bacterial constituents from Rhododendron weyrichii leaves. DPPH and ABTS+ radical scavenging activities were screened for the ethanol extract and solvent fractions. Potent scavenging activities were appeared from the extract, ethyl acetate (EtOAc) and n-butanol (BuOH) fractions. Upon the anti-bacterial tests using Staphylococcus epidermidis and Propionibacterium acnes, extract, n-hexane (Hex) and EtOAc fractions showed strong activities. To isolate the active constituents, the EtOAc fraction was further purified to afford five phytochemicals; ursolic acid (1), corosolic acid (2), asiatic acid (3), astragalin (4) and isoquercetin (5). All of the compounds 1-5 were isolated for the first time from this plant. Among the isolates, the compound 4 and 5 showed strong DPPH and ABTS+ radical scavenging activities. Also, compound 3 exhibited the most potent anti-bacterial activity. In addition, the content of astragalin isolated from this plant was determined by UPLC and the quantity was about 8.1 mg/g for the 70% ethanol extract and 34.8 mg/g for the EtOAc fraction. Based on these results, it is concluded that R. weyrichii extract could be potentially applicable as anti-oxidative and anti-bacterial ingredients in cosmetic formulations.

Inhibitory Effect on TNF-${\alpha}$-Induced IL-8 Production in the HT29 Cell of Constituents from the Leaf and Stem of Weigela subsessilis

  • Thuong Phuong Thien;Jin WenYi;Lee JongPill;Seong RackSeon;Lee Young-Mi;Seong YeonHee;Song KyungSik;Bae KiHwan
    • Archives of Pharmacal Research
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    • v.28 no.10
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    • pp.1135-1141
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    • 2005
  • Twelve compounds were isolated from the MeOH extract of the leaf and stem of the Korean endemic plant Weigela subsessilis L. H. Bailey. Their chemical structures were elucidated on the basis of physicochemical and spectroscopic data and by comparison with those of published literatures. These compounds were identified as three sterols, ${\beta}$-sitosterol acetate (2), ${\beta}$-sitosterol (3), daucosterol (11), eight triterpenoids, squalene (1), ursolic acid (4), ilekudinol A (5), corosolic acid (6), ilekudinol B (7), esculentic acid (8), pomolic acid (9), asiatic acid (10), and one iridoid glycoside, alboside I (12). This is the first report pertaining to the isolation of these compounds from Weigela subsessilis L. H. Bailey. In addition, three compounds 7, 9, and 12 were found to display a strong inhibitory effect on the production of IL-8 in the HT29 cells stimulated by TNF-${\alpha}$.

A New Flavonol Glycoside from Tristemma hirtum (Melastomataceae)

  • Kenfack, Joseph Nandjou;Ponou, Beaudelaire Kemvoufo;Kuhlborn, Jonas;Teponno, Remy Bertrand;Nono, Raymond Ngansop;Fouedjou, Romuald Tematio;Opatz, Till;Park, Hee Juhn;Tapondjou, Leon Azefack
    • Natural Product Sciences
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    • v.24 no.3
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    • pp.213-218
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    • 2018
  • Chemical investigation of the plant Tristemma hirtum P. Beauv (Melastomataceae) resulted to the isolation of a new flavonol glycoside named quercetin-7-O-${\alpha}$-D-arabinofuranoside (1), together with nine known compounds including 3'-hexadecanoyl-2'-(9aZ)-tetradecanoyl-glycerol 1'-O-[${\beta}$-D-galactopyranosyl-(1'' ${\rightarrow}$ 6'')-${\alpha}$-D-galactopyranoside] (2), arjunolic acid (3), ${\beta}$-sitosterol-3-O-${\beta}$-D-glucopyranoside (4), terminolic acid (5), quercetin (6), asiatic acid (7), maslinic acid (8), $1{\beta}$-O-galloylpedunculagin (9) and 6-hydroxyapigenin 7-O-${\beta}$-D-glucopyranoside (10) from the methanol extract using normal and reversed phase column chromatography. The structures of these compounds were determined by comprehensive interpretation of their spectral data mainly including 1D- 2D-NMR ($^1H-^1H$ COSY, HSQC, and HMBC) spectroscopic and ESI-TOF-MS mass spectrometric analysis.

Anti-inflammatory and Anti-bacterial Active Ingredients Derived from the Extract of the Leaves of Hydrangea Petiolaris (등수국 잎 추출물 유래 항염 및 항균 활성 성분)

  • Jo, Seong Mi;Kim, Jung Eun;Lee, Nam Ho
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.46 no.3
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    • pp.207-218
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    • 2020
  • In this study, the anti-inflammatory and anti-bacterial activities of the extracts from the leaves of the Hydrangea petiolaris were identified, and the chemical structure was identified by separating the active ingredient. As the result of the anti-inflammatory activity experiment using RAW 264.7 cells, it was confirmed that the n-hexane (Hex) and ethyl acetate (EtOAc) fractions inhibited the production of nitric oxide (NO) and the expression of iNOS protein in a concentration-dependent manner without cytotoxicity. In addition, the n-Hex and EtOAc fractions reduced the production of pro-inflammatory cytokines (TNF-α, IL-1β and IL-6). Upon the anti-bacterial tests using Staphylococcus epidermidis and Cutibacterium acnes, the extract, n-Hex, EtOAc and n-butanol (BuOH) fractions showed potent activities. In order to isolate the active constituents, the n-Hex and EtOAc fractions were further purified to afford four phytochemicals; phytol (1), corosolic acid (2), asiatic acid (3) and 1-O-p-coumaroyl-β-D-glucopyranoside (4). All of the compounds 1 - 4 were isolated for the first time from this plant. In addition, the contents of isolated compounds were determined by HPLC and the quantity of phytol (1) was 27.8 mg/g for the 70% EtOH extract. Based on the above research results, it is believed that it will be possible to develop a natural cosmetic material that has anti-inflammatory and anti-bacterial effects using the extract of H. petiolaris leaves.

Structure-Related Cytotoxicity and Anti-Heaptofibric Effect of Asiaticoside Derivatives in Rat Hepatic Stellate Cell Line, Hsc-T6

  • Kim, Jeong-Ran;Jung, Seung-Hyun;Lee, Eung-Seok;Lee, Eun-Joo;Yi, Jung-Bum;Lee, Namkyu;Cho, Yong-Baik;Kwak, Wie-Jong;Park, Young-In
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2003.10b
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    • pp.171-171
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    • 2003
  • Asiaticoside, a biologically active triterpenoid present in Centella asicatica, has been known to exert a variety of biological effect such as wound-healing, hepatoprotective, anti-inflammatory. In this study, we observed the effect of asiatic acid asiaticoside and its 16 derivatives on the cytotoxicity and the content of hydroxyproline in rat hepatic stellate cell line, HSC-T6 cell as a preliminary study for screening the anti-hepatofibrotic effect.(omitted)

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Biological Activities and Stability of a Standardized Pentacyclic Triterpene Enriched Centella asiatica Extract

  • Puttarak, Panupong;Brantner, Adelheid;Panichayupakaranant, Pharkphoom
    • Natural Product Sciences
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    • v.22 no.1
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    • pp.20-24
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    • 2016
  • Pentacyclic triterpenes, mainly, asiatic acid, madecassic acid, asiaticoside, and madecassoside are the active constituents of Centella asiatica. A pentacyclic triterpene enriched C. asiatica extract (PRE) was prepared and standardized to contain a total pentacyclic triterpenes not less than 65% w/w. This work was focused on determination of antiinflammatory, antioxidant, and tyrosinase inhibitory activities of PRE and its stability. The PRE exhibited a satisfactory nitric oxide inhibitory effect, with an $IC_{50}$ value of $64.6{\mu}g/mL$. In addition, the PRE inhibited tyrosinase enzyme activity with an $IC_{50}$ value of $104.8{\mu}g/mL$. In contrast, the PRE possessed only weak antioxidant activity. The PRE was stable over a period of four months when stored as a dried powder but only in a well-closed container protected from light at $4^{\circ}C$. An aqueous alcoholic solution of the PRE was stable at pH values of 5.8 and 7.0, but was not stable at a pH of 8.2. Preparations of the PRE in an aqueous solution should be performed in acidic or neutral conditions.