title: Ethyl acetate fraction of the root of Rubia cordifolia L. inhibits keratinocyte proliferation in vitro and promotes keratinocyte differentiation in vivo: potential application for psoriasis treatment.
abstract: Psoriasis is a skin disease associated with hyperproliferation and aberrant differentiation of keratinocytes. Our previous studies have identified the root of Rubia cordifolia L. as a potent antiproliferative and apoptogenic agent in cultured HaCaT cells (IC(50) 1.4 microg/ml). In the present study, ethanolic extract of Radix Rubiae was fractioned sequentially with hexane, ethyl acetate (EA), n-butanol and water. EA fraction was found to possess most potent antiproliferative action on HaCaT cells (IC(50) 0.9 microg/ml). Mechanistic study revealed that EA fraction induced apoptosis on HaCaT cells, as it was capable of inducing apoptotic morphological changes. Annexin V-PI staining assay also demonstrated that EA fraction significantly augmented HaCaT apoptosis. In addition, EA fraction decreased mitochondrial membrane potential in a concentration- and time-dependent manner. The standardized EA fraction was formulated into topical gel and its keratinocyte-modulating action was tested on mouse tail model. EA fraction dose-dependently increased the number and thickness of granular layer and epidermal thickness on mouse tail skin, indicative of the keratinocyte differentiation-inducing activity. Taking the in vitro and in vivo findings together, the present preclinical study confirms that EA fraction is a promising antipsoriatic agent warranting further development for psoriasis treatment.
authors: School of Chinese Medicine, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong, China. linzx@cuhk.edu.hk
authors: Z X
authors: ZX
authors: Lin
authors: B W
authors: BW
authors: Jiao
authors: C T
authors: CT
authors: Che
authors: Z
authors: Z
authors: Zuo
authors: C F
authors: CF
authors: Mok
authors: M
authors: M
authors: Zhao
authors: W K K
authors: WK
authors: Ho
authors: W P
authors: WP
authors: Tse
authors: K Y
authors: KY
authors: Lam
authors: R Q
authors: RQ
authors: Fan
authors: Z J
authors: ZJ
authors: Yang
authors: C H K
authors: CH
authors: Cheng
mesh_terms: D000085:Acetates; D000279:Administration, Cutaneous; D000818:Animals; D002454:Cell Differentiation / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects*; D002478:Cells, Cultured; D003879:Dermatologic Agents / Q000008:administration & dosage / Q000494:pharmacology*; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry; D011565:Psoriasis / Q000188:drug therapy; D045470:Rubia / Q000737:chemistry*
chemical_list: D000085:Acetates; D003879:Dermatologic Agents; D010936:Plant Extracts; C007650:ethyl acetate