Helichrysetin

SKU: orb1940921

Description

Helichrysetin has mild anti-HIV-1 PR activity. Helichrysetin has great potentials for development as an anticancer agent, it has cytotoxic effect on four selected cancer cell lines, A549, MCF-7, Ca Ski, and HT-29.Searching for anti-HIV-1 protease (PR) inhibitors of Thai medicinal plants led to the isolation of a new cyclohexenyl chalcone named panduratin C and chalcone derivatives from the methanol extract of Boesenbergia pandurata rhizomes. The known compounds were identified to be panduratin A, hydroxypanduratin A, Helichrysetin, 2',4',6'-trihydroxyhydrochalcone, and uvangoletin . The structures of all compounds were elucidated on the basis of chemical and spectroscopic methods.

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Key Properties

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CAS Number	62014-87-3
MW	286.3
Purity	>98% (HPLC)
Formula	C₁₆H₁₄O₅
SMILES	O=C(C1=C(OC)C=C(O)C=C1O)/C=C/C2=CC=C(O)C=C2
Target	HIV
Solubility	In Vitro: DMSO : 50 mg/mL (174.65 mM)

Bioactivity

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In Vivo

Animal model: MGC803 cell-xenografted mouse model. Dosage: 3, 10, 30 mg/kg. Administration: i.p. Result: Decreased the tumor size and weight without an obvious effect on body weight in nude mice. Reduced the expression of Ki67 and increased the number of apoptotic cells in tumor tissues.

In Vitro

Cell Viability Assay Cell line: HT-29, A549, MCF-7, and Ca Ski. Concentration: 1.56, 3.13, 6.25, 12.5, 25, 50, 100 μg/mL Incubation time: 72 h. Result: Inhibited cell growth in a dose-dependent manner. IC50 for A549, Ca Ski, HT29, MCF-7 was 50.72 ± 1.26 μM (14.52 ± 0.36 μg/mL), 31.02 ± 0.45 μM (8.88 ± 0.13 μg/mL), 102.94 ± 2.20 μM (29.47 ± 0.63 μg/mL) and 97.35 ± 1.71 μM (27.87 ± 0.49 μg/mL). Apoptosis Analysis Cell line: A549. Concentration: 5, 15, 20 μg/mL. Incubation time: 24-72 h. Result: The population of early apoptotic cells increased from 2.65 ± 0.31% (control) to 2.78 ± 0.21%, 14.98 ± 0.79%, and 28.55 ±1.19%. Caused accumulation of cells in S phase, occurring simultaneously with the significant reduction of cell percentage in G0/G1 phase with 15 and 20 μg/mL. Western blot analysis. Cell line: MGC803. Concentration: 10, 20 40 μM. Incubation time: 24 h. Result: Increased the protein expression of cleaved caspase 3 (20 and 40 μM) and reduced protein expression of Bcl-2 (40 μM), but had no significant effect on the protein expression of Bax. RT-PCR Cell line: MGC803. Concentration: 10, 20 40 μM. Incubation time: 24 h. Result: Reduced the mRNA and protein expression of PDHK1 and LDHA but only decreased the mRNA level of LDHB.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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Helichrysetin (orb1940921)

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Purity:	98.38%
CAS Number:	62014-87-3
MW:	286.28
Formula:	C₁₆H₁₄O₅

Helichrysetin

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Bioactivity

Storage & Handling

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