์—ฐ๊ตฌ์šฉ

Fisetin Natural Flavonoid

์ œํ’ˆ ๋ฒˆํ˜ธS2298

Fisetin (Fustel) is a potent sirtuin activating compound (STAC) and an agent that modulates sirtuins.
Fisetin Sirtuin modulator Chemical Structure

ํ™”ํ•™ ๊ตฌ์กฐ

๋ถ„์ž๋Ÿ‰: 286.24

๋ฐ”๋กœ๊ฐ€๊ธฐ

ํ’ˆ์งˆ ๊ด€๋ฆฌ (Quality Control)

๋ฐฐ์น˜: ์ˆœ๋„: 99.91%
99.91

์„ธํฌ ๋ฐฐ์–‘, ์ฒ˜๋ฆฌ ๋ฐ ์ž‘์—… ๋†๋„
(Cell Culture, Treatment & Working Concentration)

์„ธํฌ์ฃผ ๋ถ„์„ ์œ ํ˜• ๋†๋„ ๋ฐฐ์–‘ ์‹œ๊ฐ„ ์ œํ˜• ํ™œ์„ฑ ์„ค๋ช… PMID
MDA-MB-453 Cell viability assay 0, 20, 40, 60, 80, and 100 ยตM 24, 48, and 72 hours With increasing concentrations of fisetin (0, 20, 40, 60, 80, and 100 ยตM), there was a decrease observed in cell number in different time intervals (24, 48, and 72 hours).
SGC7901 Proliferation assay 0, 1, 5, 10, 15 or 20 ยตM 48 h inhibits proliferation
A549 Cell viability assay 0, 10, 20, 30 or 40 ยตM 24, 48 or 72 h fisetin was effective in inhibiting the growth of A549 cells in a dose- and time-dependent manner
ARPE-19 Cell migration assay 5 or 10 ฮผM 24 h pretreatment with fisetin markedly reduced cell migration in EGF-treated ARPE-19 cells
SCC-23 Cell viability assay 0-100 ฮผM 24 h fisetin significantly inhibited cell viability in a dose-dependent manner (significantly when the concentration is higher than 20 ฮผM)
Tca-8113 Cell viability assay 0-100 ฮผM 24 h fisetin significantly inhibited cell viability in a dose-dependent manner (significantly when the concentration is higher than 20 ฮผM)
ํด๋ฆญํ•˜์—ฌ ๋” ๋งŽ์€ ์„ธํฌ์ฃผ ์‹คํ—˜ ๋ฐ์ดํ„ฐ ๋ณด๊ธฐ

ํ™”ํ•™ ์ •๋ณด, ๋ณด๊ด€ ๋ฐ ์•ˆ์ •์„ฑ (Chemical Information, Storage & Stability)

๋ถ„์ž๋Ÿ‰ 286.24 ํ™”ํ•™์‹

C15H10O6

๋ณด๊ด€ (์ˆ˜๋ น์ผ๋กœ๋ถ€ํ„ฐ)
CAS ๋ฒˆํ˜ธ 528-48-3 SDF ๋‹ค์šด๋กœ๋“œ ์›์•ก ๋ณด๊ด€

์šฉํ•ด๋„ (Solubility)

In vitro
๋ฐฐ์น˜:

DMSO : 57 mg/mL (199.13 mM)
(์ˆ˜๋ถ„์œผ๋กœ ์˜ค์—ผ๋œ DMSO๋Š” ์šฉํ•ด๋„๋ฅผ ๊ฐ์†Œ์‹œํ‚ฌ ์ˆ˜ ์žˆ์Šต๋‹ˆ๋‹ค. ์‹ ์„ ํ•˜๊ณ  ๋ฌด์ˆ˜ DMSO๋ฅผ ์‚ฌ์šฉํ•˜์‹ญ์‹œ์˜ค.)

Ethanol : 9 mg/mL

Water : Insoluble

๋ชฐ๋†๋„ ๊ณ„์‚ฐ๊ธฐ

์งˆ๋Ÿ‰ ๋†๋„ ๋ถ€ํ”ผ ๋ถ„์ž๋Ÿ‰
ํฌ์„ ๊ณ„์‚ฐ๊ธฐ ๋ถ„์ž๋Ÿ‰ ๊ณ„์‚ฐ๊ธฐ

In vivo
๋ฐฐ์น˜:

์ƒ์ฒด ๋‚ด ์ œํ˜• ๊ณ„์‚ฐ๊ธฐ (ํˆฌ๋ช…ํ•œ ์šฉ์•ก)

1๋‹จ๊ณ„: ์•„๋ž˜ ์ •๋ณด ์ž…๋ ฅ (๊ถŒ์žฅ: ์‹คํ—˜ ์ค‘ ์†์‹ค์„ ๊ณ ๋ คํ•˜์—ฌ ์ถ”๊ฐ€ ๋™๋ฌผ ํฌํ•จ)

mg/kg g ฮผL

2๋‹จ๊ณ„: ์ƒ์ฒด ๋‚ด ์ œํ˜• ์ž…๋ ฅ (์ด๊ฒƒ์€ ๊ณ„์‚ฐ๊ธฐ์ผ ๋ฟ ์ œํ˜•์ด ์•„๋‹™๋‹ˆ๋‹ค. ์šฉํ•ด๋„ ์„น์…˜์— ์ƒ์ฒด ๋‚ด ์ œํ˜•์ด ์—†๋Š” ๊ฒฝ์šฐ ๋จผ์ € ๋‹น์‚ฌ์— ๋ฌธ์˜ํ•˜์‹ญ์‹œ์˜ค.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

๊ณ„์‚ฐ ๊ฒฐ๊ณผ:

์ž‘์—… ๋†๋„: mg/ml;

DMSO ์›์•ก ์ค€๋น„ ๋ฐฉ๋ฒ•: mg ์•ฝ๋ฌผ ์‚ฌ์ „ ์šฉํ•ด ฮผL DMSO ( ์›์•ก ๋†๋„ mg/mL, ๋†๋„๊ฐ€ ํ•ด๋‹น ์•ฝ๋ฌผ ๋ฐฐ์น˜์˜ DMSO ์šฉํ•ด๋„๋ฅผ ์ดˆ๊ณผํ•˜๋Š” ๊ฒฝ์šฐ ๋จผ์ € ๋‹น์‚ฌ์— ๋ฌธ์˜ํ•˜์‹ญ์‹œ์˜ค. )

์ƒ์ฒด ๋‚ด ์ œํ˜• ์ค€๋น„ ๋ฐฉ๋ฒ•: ์ทจํ•˜๋‹ค ฮผL DMSO ์›์•ก, ๋‹ค์Œ ์ถ”๊ฐ€ฮผL PEG300, ํ˜ผํ•ฉํ•˜๊ณ  ํˆฌ๋ช…ํ•˜๊ฒŒ ํ•œ ๋‹ค์Œ ์ถ”๊ฐ€ฮผL Tween 80, ํ˜ผํ•ฉํ•˜๊ณ  ํˆฌ๋ช…ํ•˜๊ฒŒ ํ•œ ๋‹ค์Œ ์ถ”๊ฐ€ ฮผL ddH2O, ํ˜ผํ•ฉํ•˜๊ณ  ํˆฌ๋ช…ํ•˜๊ฒŒ ํ•ฉ๋‹ˆ๋‹ค.

์ƒ์ฒด ๋‚ด ์ œํ˜• ์ค€๋น„ ๋ฐฉ๋ฒ•: ์ทจํ•˜๋‹ค ฮผL DMSO ์›์•ก, ๋‹ค์Œ ์ถ”๊ฐ€ ฮผL ์˜ฅ์ˆ˜์ˆ˜ ๊ธฐ๋ฆ„, ํ˜ผํ•ฉํ•˜๊ณ  ํˆฌ๋ช…ํ•˜๊ฒŒ ํ•ฉ๋‹ˆ๋‹ค.

์ฐธ๊ณ : 1. ๋‹ค์Œ ์šฉ๋งค๋ฅผ ์ถ”๊ฐ€ํ•˜๊ธฐ ์ „์— ์•ก์ฒด๊ฐ€ ํˆฌ๋ช…ํ•œ์ง€ ํ™•์ธํ•˜์‹ญ์‹œ์˜ค.
2. ์šฉ๋งค๋ฅผ ์ˆœ์„œ๋Œ€๋กœ ์ถ”๊ฐ€ํ•ด์•ผ ํ•ฉ๋‹ˆ๋‹ค. ๋‹ค์Œ ์šฉ๋งค๋ฅผ ์ถ”๊ฐ€ํ•˜๊ธฐ ์ „์— ์ด์ „ ์ถ”๊ฐ€์—์„œ ์–ป์€ ์šฉ์•ก์ด ํˆฌ๋ช…ํ•œ ์šฉ์•ก์ธ์ง€ ํ™•์ธํ•ด์•ผ ํ•ฉ๋‹ˆ๋‹ค. ์™€๋™, ์ดˆ์ŒํŒŒ ๋˜๋Š” ๋œจ๊ฑฐ์šด ๋ฌผ ์ค‘ํƒ•๊ณผ ๊ฐ™์€ ๋ฌผ๋ฆฌ์  ๋ฐฉ๋ฒ•์„ ์‚ฌ์šฉํ•˜์—ฌ ์šฉํ•ด๋ฅผ ๋„์šธ ์ˆ˜ ์žˆ์Šต๋‹ˆ๋‹ค.

์ž‘์šฉ ๋ฉ”์ปค๋‹ˆ์ฆ˜ (Mechanism of Action)

Targets/IC50/Ki
Sirtuin
์‹œํ—˜๊ด€ ๋‚ด(In vitro)

Fisetin selectively kills SPiDER-β-Gal positive senescence neural cells in vitro.

์ƒ์ฒด ๋‚ด(In vivo)

Oral administration of fisetin, a senolytic drug, reduces the number of senescent neural cells observed, the SASP expression level, and depressive behavior in MRL/lpr mice.

์ฐธ์กฐ

์ ์šฉ ๋ถ„์•ผ (Applications)

๋ฐฉ๋ฒ• ๋ฐ”์ด์˜ค๋งˆ์ปค ์ด๋ฏธ์ง€ PMID
Western blot p-IKKฮฑ/ฮฒ / IKKฮฒ / IKKฮฑ / p-IฮบBฮฑ / IฮบBฮฑ / p-p65 / p65 XBP1s / ATF6 / CHOP / ATF4 / PERK DR3 / pNF-ฮบB / NF-ฮบB p-mTOR / mTOR / Raptor / Rictor
S2298-WB1
23861901
Immunofluorescence p-4EBP1 / p-eIF4B / p-rpS6 uPA
S2298-IF1
20530556
Growth inhibition assay Cell viability
S2298-viability1
19670328

์ž„์ƒ์‹œํ—˜ ์ •๋ณด (Clinical Trial Information)

(๋ฐ์ดํ„ฐ ์ถœ์ฒ˜ https://clinicaltrials.gov, ์—…๋ฐ์ดํŠธ ๋‚ ์งœ 2024-05-22)

NCT ๋ฒˆํ˜ธ ๋ชจ์ง‘ ์กฐ๊ฑด ์Šคํฐ์„œ/ํ˜‘๋ ฅ์ž ์‹œ์ž‘์ผ ๋‹จ๊ณ„
NCT05758246 Recruiting
Sepsis|Acute Infection|Organ Failure
University of Minnesota
August 23 2023 Phase 2