Costunolide

製品コードS1319 バッチS131904

化学情報

	Synonyms	NSC 106404	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₅H₂₀O₂
	分子量	232.32	CAS No.	553-21-9
Solubility (25°C)*	体外	DMSO	47 mg/mL (202.3 mM)
		Ethanol	47 mg/mL (202.3 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Costunolide (NSC 106404), a natural sesquiterpene compound with multiple biological activities; inhibits FPTase with IC50 of 20 μM, also inhibits telomerase with IC50 of 65-90 μM.
in vitro	Costunolide inhibits the growth and telomerase activity of MCF-7 and MDA-MB-231 cells in a concentration- and time-dependent manner. ^[1] Costunolide also inhibits the farnesylation process of human lamin-B by farnesyl–proteinttransferase (FPTase), in a dose dependent manner. Continuously treatment of Costunolide for 48 hours will significantly decrease proliferation of human tumor cells (A549, SK-OV-3, SK-MEL-2, XF498 and HCT-1) in a dose-dependent manner. ^[2] Costunolide induces apoptosis by ROS-mediated mitochondrial permeability transition and cytochrome C release to the cytosol in HL-60 human leukemia cells. ^[3] A recent study indicates that Costunolide shows significant antifungal activity, including Trichophyton mentagrophytes, T.simlii, T.rubrum, and so on. ^[4]
in vivo	Costunolide inhibits angiogenic response by blocking the angiogenic factor signaling pathway. In a mouse corneal micropocket assay, Costunolide reduces VEGF-stimulated neovascularization in mice. ^[5]

プロトコル(参考用のみ)

キナーゼアッセイ	Telomerase activity assay
キナーゼアッセイ	The telomerase activity is measured by the TRAP assay using the TRAPez Telomerase Detection Kit, which includes primers of a 36-bp internal control (IC) for quantifying the amplification of telomerase activity within a linear range close to 2.5 logs. For RNase treatment, 10μL of extract are incubated with 1μg of RNase at 37 °C for 20 minutes. The products of the TRAP assay are resolved by electrophoresis in a nondenaturing12% PAGE in a buffer containing 0.5 × Tris–borate EDTA and detected by autoradiograph. For quantification of TRAP products, the dried gels are exposed to Fuji Imaging Plate at room temperature. Results are corrected for background, and a standard value of 100 is given to the untreated control cell signal. Signal intensities of Costunolide-treated cells are compared to the standard and are expressed as a fraction of the maximum value of 100. ^[1]
細胞アッセイ	細胞株	MCF-7 and MDA-MB-231 cells
	濃度	0-100 μM
	反応時間	48 hours
	実験の流れ	1) Plate 500-10,000 cells in 200 μL media per well in a 96 well plate. Leave 8 wells empty for blank controls. 2) Incubate (37 °C, 5% CO₂) overnight to allow the cells to attach to the wells. 3) Add 2 μL of Costunolide dissolved in DMSO to each well. Place on a shaking table, 150 rpm for 5 minutes, to thoroughly mix the samples into the media. 5) Incubate (37 °C, 5% CO₂) for 48 hours to allow Costunolide to take effect. 6) Make 2 mL or more of MTT solution per 96 well plate at 5 mg/mL in PBS. Do not make a stock as MTT in solution is not stable long-term. 7) Add 20 μL MTT solution to each well. Place on a shaking table, 150 rpm for 5 minutes, to thoroughly mix the MTT into the media. 8) Incubate (37 °C, 5% CO₂) for 1-5 hours to allow the MTT to be metabolized. 9) Dump off the media. (Dry plate on paper towels to remove residue if necessary. 10) Resuspend formazan (MTT metabolic product) in 200 μL DMSO. Place on a shaking table, 150 rpm for 5 minutes, to thoroughly mix the formazan into the solvent. 11) Read optical density at 560 nm and subtract background at 670 nm. Optical density should be directly correlated with cell quantity.
動物実験	動物モデル	Hydron N containing VEGF are implanted into mouse cornea.
	投薬量	100 mg/kg
	投与方法	Intraperitoneal injection once daily.

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Costunolide alleviated DDC induced ductular reaction and inflammatory response in murine model of cholestatic liver disease [ J Tradit Complement Med, 2023, 13(4):345-357]	PubMed: 37396159
Costunolide enhances cisplatin-induced cytotoxicity in hypopharyngeal SCC FaDu cells by increasing the production of reactive oxygen species [ Pathol Res Pract, 2022, 236:153966]	PubMed: 35679753
Costunolide Influences Germ Tube Orientation in Sunflower Broomrape - A First Step Toward Understanding Chemotropism [ Front Plant Sci, 2021, 12:699068]	PubMed: 34484263
A Patient-Derived Cell Atlas Informs Precision Targeting of Glioblastoma [ Cell Rep, 2020, 32(2):107897]	PubMed: 32668248
The TERT copy number gain is sensitive to telomerase inhibitors in human melanoma. [ Clin Sci (Lond), 2020, 10.1042/CS20190890]	PubMed: 31919521
Costunolide Induces Autophagy and Apoptosis by Activating ROS/MAPK Signaling Pathways in Renal Cell Carcinoma [ Front Oncol, 2020, 10:582273]	PubMed: 33194716
Amelioration of Benign Prostatic Hyperplasia by Costunolide and Dehydrocostus Lactone in Wistar Rats. [ World J Mens Health, 2019, 10.5534/wjmh.190053]	PubMed: 31749336
Characterization of CYP71AX36 from Sunflower (Helianthus annuus L., Asteraceae). [ Sci Rep, 2019, 9(1):14295]	PubMed: 31586110
New sesquiterpene lactones from sunflower root exudate as germination stimulants for Orobanche cumana. [Raupp FM, et al. J Agric Food Chem, 2013, 61(44):10481-7]	PubMed: 24117219

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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