1. Apoptosis
  2. Apoptosis
  3. Helichrysetin

Helichrysetin is isolated from the flower Helichrysum odoratissimum. Helichrysetin is an ID2 (DNA binding inhibitor 2) inhibitor. Helichrysetin induces apoptosis. Helichrysetin has anti-tumor and antioxidant activity.

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Helichrysetin Chemical Structure

Helichrysetin Chemical Structure

CAS No. : 62014-87-3

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Based on 1 publication(s) in Google Scholar

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Description

Helichrysetin is isolated from the flower Helichrysum odoratissimum. Helichrysetin is an ID2 (DNA binding inhibitor 2) inhibitor. Helichrysetin induces apoptosis. Helichrysetin has anti-tumor and antioxidant activity[1][2][3].

In Vitro

Helichrysetin (0-100 μM, 48 h) inhibits the development of ductal carcinoma in situ (DCIS) by targeting DNA inhibitor 2 (ID2) [2].
Helichrysetin (5-20 μg/mL, 48 h) can block the cell cycle and induce apoptosis in A549 human lung cancer cells[2].
Helichrysetin (10-40 μM, 48 h) inhibits the growth of gastric cancer cells by targeting mTOR/p70S6K/c-Myc/ PDHK1-mediated energy metabolic reprogramming of cancer cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[2]

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[3]

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[3]

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.
Decreased the protein expression of pyruvate dehydrogenase phosphatase (PDP) 2 and the ratio of p-PDHA1/PDHA1.
Increased the expression levels of Nrf2, HO-1, and NQO-1 and reduced Keap1.
Inhibited the phosphorylation of PI3K, Akt, mTOR, and P70S6K.
In Vivo

Helichrysetin (10 mg/kg, Intraperitoneal injection) can inhibit DCIS growth in mice with no obvious side effects[1].
Helichrysetin (3, 10, 30 mg/kg, Intraperitoneal injection) can inhibit tumor growth in a mouse model of gastric cancer cell transplantation[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MGC803 cell-xenografted mouse model[3]
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.
Molecular Weight

286.28

Formula

C16H14O5

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=C(OC)C=C(O)C=C1O)/C=C/C2=CC=C(O)C=C2

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (174.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4931 mL 17.4654 mL 34.9308 mL
5 mM 0.6986 mL 3.4931 mL 6.9862 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.92%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4931 mL 17.4654 mL 34.9308 mL 87.3271 mL
5 mM 0.6986 mL 3.4931 mL 6.9862 mL 17.4654 mL
10 mM 0.3493 mL 1.7465 mL 3.4931 mL 8.7327 mL
15 mM 0.2329 mL 1.1644 mL 2.3287 mL 5.8218 mL
20 mM 0.1747 mL 0.8733 mL 1.7465 mL 4.3664 mL
25 mM 0.1397 mL 0.6986 mL 1.3972 mL 3.4931 mL
30 mM 0.1164 mL 0.5822 mL 1.1644 mL 2.9109 mL
40 mM 0.0873 mL 0.4366 mL 0.8733 mL 2.1832 mL
50 mM 0.0699 mL 0.3493 mL 0.6986 mL 1.7465 mL
60 mM 0.0582 mL 0.2911 mL 0.5822 mL 1.4555 mL
80 mM 0.0437 mL 0.2183 mL 0.4366 mL 1.0916 mL
100 mM 0.0349 mL 0.1747 mL 0.3493 mL 0.8733 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Helichrysetin
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