• 생명과학회지
• /
• 제8권2호
• /
• pp.158-161
• /
• 1998

Farmesy-Protein Transferase의 저해제는 Ras단백질의 발암활성을 차잔하는 항암제의 후보로서 알려져있다. 우리는 최근에 topoisomerase I에 대하여 저해활성을 갖는 dihydrotanshinone I을 약용식물인 Salvia miltorhiza Bunge(Danshen)으로부터 분리하였다. Dihydrotanshinone Iml 작용기작의 해석을 위한 시도에서 farmesy-Protein Transferase에 대한 저해능($IC_{50}$치= 15ug/ml)을 관찰하였으며, 이것은 유용한 항암제로서의 가능성을 제시한 결과로 본다.

• 대한임상약리학회:학술대회논문집
• /
• 대한임상약리학회 2006년도 제15차 추계학술대회
• /
• pp.103-103
• /
• 2006

• 한국약용작물학회지
• /
• 제12권3호
• /
• pp.179-182
• /
• 2004

단삼(丹蔘)을 bioassay-directed fractionation에 의한 에탄올 추출물의 클로로포롬 분획물을 silica gel column chromatography, recycling preparative-HPLC 등을 실시하여 항균활성을 나타내는 2개의 화합물을 분리하여 이화학적 성상 및 spectra data (IR,$^1H-NMR,\;^{13}C-NMR$ 및 Mass)에 의해 각각 Cryptotanshinone과 dihydrotanshinone I으로 동정하였으며, 이들 화합물의 항균성 (MIC)은 각각 S. epidermidis에 대하며 $6.3,\;3.1\;{\mu}g/ml$와 S. pyogenes에 대해 $6.3\;{\mu}g/ml$로 비교적 높은 활성을 나타내어 항생제로서 개발 가능성을 보여주었다.

• Archives of Pharmacal Research
• /
• 제28권8호
• /
• pp.909-913
• /
• 2005

We screened natural products to find compounds with anti-osteoporotic potential using a coculture-based system by which osteoclast differentiation is effectively achieved. We found that methylene chloride soluble fraction of the root of Salvia miltiorrhiza Bunge (Labiatae) suppressed osteoclast differentiation. Five tanshinones, tanshinone IIA (1), tanshinone I (2), cryptotanshinone (3), 15,16-dihydrotanshinone I (4), and ferruginol (5) were subsequently isolated from fraction. Among the five compounds, compounds 1-4 reduced the formation of TRAP­positive multinuclear osteoclasts. These results suggest that the identified tanshinones may be useful candidates for development of therapeutic agents to treat osteoporosis and other bone-resorptive diseases.

• Archives of Pharmacal Research
• /
• 제25권4호
• /
• pp.446-448
• /
• 2002

The inhibitory activity of tanshinones from Salvia miltiorrhiza was tested on rat liver diacylglycerol acyltransferase (DGAT). Cryptotanshinone (1) and 15,16-dihydrotanshinone I (3) exhibited potent DGAT inhibitory activities dose-dependently with $IC_{50}$ values of $10.5 {\;}{\mu\textrm{g}}/ml{\;}and{\;}11.1{\;}{\mu\textrm{g}}/ml$. However, tanshinone IIA (2) and tanshinone I (4) showed very weak inhibition ($IC_{50}{\;}value:{\;}>{\;}250{\;}{\mu\textrm{g}}/ml$). A dihydrofuran moiety was seemed to be responsible for the stronger inhibitory activity

• Archives of Pharmacal Research
• /
• 제27권12호
• /
• pp.1233-1237
• /
• 2004

The effects of four tanshinones isolated from Tanshen (the root of Salvia miltiorrhiza Bunge, Labiatae) were tested for their inhibition of nitric oxide production in macrophage cells, and the underlying molecular mechanisms studied. Of the four tanshinones used, 15, 16-dihydrotanshinone- I, tanshinone-IIA and cryptotanshinone, but not tanshinone I, demonstrated significant inhibition of the LPS-induced nitric oxide production in RAW 264.7 cells, with calculated $IC_{50}$ values of 5, 8, and 1.5 ${\mu}M$ , respectively. Tanshinones exerted inhibitory activities on the LPS-induced nitric oxide production only when applied concurrently with LPS, and tanshinone- IIA and cryptotanshinone were found to inhibit LPS-induced NF-$_KB$ mobilization and extracellular- regulated kinase (ERK) activation, respectively. These results suggest that tanshinones inhibit LPS-induced nitric oxide generation by interfering with the initial stage of LPS-induced expression of certain genes. NF-$_KB$ and ERK could be the molecular targets for tanshinones for the inhibition of LPS-induced nitric oxide production in macrophage cells.

• 약학회지
• /
• 제57권2호
• /
• pp.119-124
• /
• 2013

The aim of this present study was to investigate the antifungal effect of tanshinones isolated from Salvia miltiorrhiza against Candida ablicans, a polymorphic fungus. For the work, tanshinone IIA (TSN), cryptotanshinone (CTS), and dihydrotanshinone I (DTS) were chosen. Initially, their antifungal effect was analyzed by in-vitro susceptibility test. Data from the susceptibility test showed that while all of these three compounds had antifungal activity, DTS was the most potent. At $100{\mu}g$ DTS/ml, there was about 80% CFU (colony forming unit) reduction as compared to DTS-untreated C. albicans yeast cells (P<0.05). Thus, DTS was selected to determine its antifungal activity in a murine model of disseminated candidiasis due to C. albicans. Results showed that DTS enhanced resistance of mice against disseminated candidiasis. During the entire period of 30-day observation, 60% of DTS-given mice groups survived whereas control animals all died within 14 days (P<0.05). Moreover, DTS inhibited the hyphal production, one of the virulence factors of this fungus, from the blastoconidial form of the fungus. Therefore, the tanshinone appears to have antifungal activity specific for C. albicans infection, which could possibly be mediated by the blockage of hyphal production.