์ฐ๊ตฌ์ฉ
์ ํ ๋ฒํธS3800
| ๊ด๋ จ ํ๊ฒ | HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase DPP HIV Protease |
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| ๊ธฐํ ADC Cytotoxin ์ต์ ์ | Triptolide SN-38 Luteolin (+)-Bicuculline Rutin Artemisinin BHQ Pinocembrin Luteoloside Sacituzumab-govitecan |
| ๋ถ์๋ | 323.77 | ํํ์ | C16H17NO4.HCl |
๋ณด๊ด (์๋ น์ผ๋ก๋ถํฐ) | |
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| CAS ๋ฒํธ | 2188-68-3 | SDF ๋ค์ด๋ก๋ | ์์ก ๋ณด๊ด |
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| ๋์์ด | Galanthidine hydrochloride, Amarylline hydrochloride, Narcissine hydrochloride, Licorine hydrochloride | Smiles | C1CN2CC3=CC4=C(C=C3C5C2C1=CC(C5O)O)OCO4.Cl | ||
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In vitro |
DMSO
: 65 mg/mL
(200.75 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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1๋จ๊ณ: ์๋ ์ ๋ณด ์ ๋ ฅ (๊ถ์ฅ: ์คํ ์ค ์์ค์ ๊ณ ๋ คํ์ฌ ์ถ๊ฐ ๋๋ฌผ ํฌํจ)
2๋จ๊ณ: ์์ฒด ๋ด ์ ํ ์ ๋ ฅ (์ด๊ฒ์ ๊ณ์ฐ๊ธฐ์ผ ๋ฟ ์ ํ์ด ์๋๋๋ค. ์ฉํด๋ ์น์ ์ ์์ฒด ๋ด ์ ํ์ด ์๋ ๊ฒฝ์ฐ ๋จผ์ ๋น์ฌ์ ๋ฌธ์ํ์ญ์์ค.)
๊ณ์ฐ ๊ฒฐ๊ณผ:
์์ ๋๋: mg/ml;
DMSO ์์ก ์ค๋น ๋ฐฉ๋ฒ: mg ์ฝ๋ฌผ ์ฌ์ ์ฉํด ฮผL DMSO ( ์์ก ๋๋ mg/mL, ๋๋๊ฐ ํด๋น ์ฝ๋ฌผ ๋ฐฐ์น์ DMSO ์ฉํด๋๋ฅผ ์ด๊ณผํ๋ ๊ฒฝ์ฐ ๋จผ์ ๋น์ฌ์ ๋ฌธ์ํ์ญ์์ค. )
์์ฒด ๋ด ์ ํ ์ค๋น ๋ฐฉ๋ฒ: ์ทจํ๋ค ฮผL DMSO ์์ก, ๋ค์ ์ถ๊ฐฮผL PEG300, ํผํฉํ๊ณ ํฌ๋ช ํ๊ฒ ํ ๋ค์ ์ถ๊ฐฮผL Tween 80, ํผํฉํ๊ณ ํฌ๋ช ํ๊ฒ ํ ๋ค์ ์ถ๊ฐ ฮผL ddH2O, ํผํฉํ๊ณ ํฌ๋ช ํ๊ฒ ํฉ๋๋ค.
์์ฒด ๋ด ์ ํ ์ค๋น ๋ฐฉ๋ฒ: ์ทจํ๋ค ฮผL DMSO ์์ก, ๋ค์ ์ถ๊ฐ ฮผL ์ฅ์์ ๊ธฐ๋ฆ, ํผํฉํ๊ณ ํฌ๋ช ํ๊ฒ ํฉ๋๋ค.
์ฐธ๊ณ : 1. ๋ค์ ์ฉ๋งค๋ฅผ ์ถ๊ฐํ๊ธฐ ์ ์ ์ก์ฒด๊ฐ ํฌ๋ช
ํ์ง ํ์ธํ์ญ์์ค.
2. ์ฉ๋งค๋ฅผ ์์๋๋ก ์ถ๊ฐํด์ผ ํฉ๋๋ค. ๋ค์ ์ฉ๋งค๋ฅผ ์ถ๊ฐํ๊ธฐ ์ ์ ์ด์ ์ถ๊ฐ์์ ์ป์ ์ฉ์ก์ด ํฌ๋ช
ํ ์ฉ์ก์ธ์ง ํ์ธํด์ผ ํฉ๋๋ค. ์๋, ์ด์ํ ๋๋ ๋จ๊ฑฐ์ด ๋ฌผ ์คํ๊ณผ ๊ฐ์ ๋ฌผ๋ฆฌ์ ๋ฐฉ๋ฒ์ ์ฌ์ฉํ์ฌ ์ฉํด๋ฅผ ๋์ธ ์ ์์ต๋๋ค.
| ์ํ๊ด ๋ด(In vitro) |
Lycorine not only possesses strong pharmacological effects on many diseases, including anti-leukemia, anti-tumor, anti-angiogenesis, anti-virus, anti-bacteria, anti-inflammation, and anti-malaria, but also exerts many other biological functions, such as inhibition of acetylcholinesterase and topoisomerase, suppression of ascorbic acid biosynthesis, and control of circadian period length. Lycorine inhibits cell proliferation and induces cell apoptosis in acute myeloid leukemia (AML) cell line HL-60, monocyte leukemia cell line U937, and T-cell leukemia cell line Jurkat. Lycorine also blocks multiple myeloma KM3 cell cycle, induces K562 cell-cycle arrest at the G0/G1 phase and suppresses tumorigenesis and the growth of various tumor cells, including melanoma C8161, ovarian cancer Hey1B, lung cancer A549, glioblatatoma U373, and esophageal cancer OE21. Lycorine can inhibit protein synthesis in eukaryotic cells, and acetylcholinesterase activity.
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| ์์ฒด ๋ด(In vivo) |
Lycorine exhibits its numerous pharmacological effects on various diseases with very low toxicity and mild side effects. In vivo studies, lycorine effectively inhibits tumor growth in several mouse xenograft models. It effectively inhibits tumor neovascularization. Lycorine has trivial toxicity to normal cells and normal bodies. The animal toxicological experiments show that the 50% lethal death rate (LD50) of lycorine in mice is 112.2ยฑ0.024 mg/kg via intraperitoneal injection. The LD50 of lycorine in mice is 344 mg/kg via gastric lavage injection, suggesting that lycorine is very low toxicity in gastrointestinal administration. In vivo studies show that lycorine has linear plasma kinetics with a mean elimination half-life of 0.67 and 0.3 h after single s.c. and i.v. administration, respectively. The mean oral bioavailability is calculated to be about 40%. Biochemical and hematological parameters of safety studies indicate no pathological signs.
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์ฐธ์กฐ |
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