Peringatan Keamanan

In an acute oral toxicity study, the LD50-value for ?-arbutin is 9804 mg/kg bw for the mouse and 8715 mg/kg bw for the rat F44. Dermal LD50 value in rat and mouse was reported to be greater than 928 mg/kg bw, according to an acute dermal toxicity study F44. Extremely high doses may cause ringing in the ears, shortness of breath, convulsions, collapse, vomiting and delirium F43. Nausea and vomiting were seen individuals with sensitive stomachs following oral ingestion of 15 g of dried uva ursi leaves that contain arbutin F43.

Arbutin

DB11217

small molecule approved

Deskripsi

Extracted from the dried leaves of bearberry plant in the genus Arctostaphylos and other plants commonly in the Ericaceae family, arbutin is a beta-D-glucopyranoside of DB09526. It is found in foods, over-the-counter drugs, and herbal dietary supplements F43. Most commonly, it is an active ingredient in skincare and cosmetic products as a skin-lightening agent for the prevention of melanin formation in various skin conditions that involve cutaneous hyperpigmentation or hyperactive melanocyte function A27248. It has also been used as an anti-infective for the urinary system as well as a diuretic F43. Arbutin is available in both natural and synthetic forms; it can be synthesized from acetobromglucose and DB09526 F43. Arbutin is a competitive inhibitor of tyrosinase (E.C.1.14.18.1) in melanocytes A27248, and the inhibition of melanin synthesis at non-toxic concentrations was observed in vitro. Arbutin was shown to be less cytotoxic to melanocytes in culture compared to DB09526 A32942.

Struktur Molekul 2D

Berat 272.2512
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) No pharmacokinetic data available.
Volume Distribusi No pharmacokinetic data available.
Klirens (Clearance) No pharmacokinetic data available.

Absorpsi

Arbutin was found to be extensively absorbed from the gastrointestinal tract where it is primarily converted to hydroquinone F43.

Metabolisme

Arbutin is readily susceptible to hydrolysis in dilute acids to yield D-glucose and hydroquinone. It is expected that orally administered arbutin is easily hydrolyzed to free hydroquinone molecules by stomach acid F43. Hydroquinone is further metabolized into the main metabolites, hydroquinone glucuronide and hydroquinone sulfate F43.

Rute Eliminasi

During the first 4 hours following ingestion of a single dose of 210 mg arbutin in healthy volunteers, 224.5 ?mol/L hydroquinone glucuronide and 182 ?mol/L of hydroquinone sulfate were recovered in the urine F43.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Tyrosinase TYR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 8632348
    Maeda K, Fukuda M: Arbutin: mechanism of its depigmenting action in human melanocyte culture. J Pharmacol Exp Ther. 1996 Feb;276(2):765-9.
  • PMID: 24189417
    Inoue Y, Hasegawa S, Yamada T, Date Y, Mizutani H, Nakata S, Matsunaga K, Akamatsu H: Analysis of the effects of hydroquinone and arbutin on the differentiation of melanocytes. Biol Pharm Bull. 2013;36(11):1722-30.
  • PMID: 15056856
    Sugimoto K, Nishimura T, Nomura K, Sugimoto K, Kuriki T: Inhibitory effects of alpha-arbutin on melanin synthesis in cultured human melanoma cells and a three-dimensional human skin model. Biol Pharm Bull. 2004 Apr;27(4):510-4.
  • PMID: 19387580
    Lim YJ, Lee EH, Kang TH, Ha SK, Oh MS, Kim SM, Yoon TJ, Kang C, Park JH, Kim SY: Inhibitory effects of arbutin on melanin biosynthesis of alpha-melanocyte stimulating hormone-induced hyperpigmentation in cultured brownish guinea pig skin tissues. Arch Pharm Res. 2009 Mar;32(3):367-73. doi: 10.1007/s12272-009-1309-8. Epub 2009 Apr 23.
  • PMID: 9711535
    Chakraborty AK, Funasaka Y, Komoto M, Ichihashi M: Effect of arbutin on melanogenic proteins in human melanocytes. Pigment Cell Res. 1998 Aug;11(4):206-12.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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