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Gamma-Mangostin

Catalog No.GC38227 Copy One-Click Copy Product Info

Gamma-Mangostin is a competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent cyclooxygenase-2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor.

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Gamma-Mangostin Chemical Structure

Cas No.: 31271-07-5

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10mM (in 1mL DMSO)
$77.00
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1mg
$32.00
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5mg
$70.00
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10mg
$112.00
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20mg
$182.00
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Sample solution is provided at 25 µL, 10mM.



Description of Gamma-Mangostin

Gamma-Mangostin is a competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent cyclooxygenase-2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilizes the TTR tetramer[1]. Gamma-Mangostin has antibacterial, anticancer, antioxidant properties[2].

In vitro, Gamma-Mangostin inhibited cell proliferation and colony formation in six different colon cancer cell lines, HCT116, SW480, LS174T, RKO, HT29 and DLD1, the 48h IC50 values ranged from 10-15µM for colon cancer cell lines[2]. Gamma-Mangostin inhibited cell proliferation on U87 MG (astrocytoma glioblastoma, grade III) and GBM 8401 (glioblastoma multiforme, grade IV),the IC50 values of Gamma-Mangostin at 24 hours were 74.14±2.93 and 64.67±2.42μM[3]. Gamma-Mangostin treatment (80μM; 1h) increased intracellular peroxide levels in U87 MG and GBM 8401 cells[3]. Gamma-Mangostin treatment inhibited LPS-induced NO release with IC50 about 6.0µM in RAW264.7 cells[4].

In vivo, treatment of Gamma-Mangostin (5mg/kg; i.p.; 21 days) inhibited tumor xenograft growth in nude mice harboring HCT116 tumor xenografts[2]. Treatment of Gamma-Mangostin (10, and 30mg/kg; single oral dose) markedly improved scopolamine-induced memory impairment in mice[5].

References:
[1]. Chairungsrilerd, Nattaya, et al. "γ-Mangostin, a novel type of 5-hydroxytryptamine 2A receptor antagonist." Naunyn-Schmiedeberg's archives of pharmacology 357.1 (1997): 25-31.
[2]. Krishnamachary, Balaji, et al. "Targeting transcription factor TCF4 by γ-Mangostin, a natural xanthone." Oncotarget 10.54 (2019): 5576.
[3]. Chang, Hui-Fang, et al. "Apoptotic effects of γ-mangostin from the fruit hull of Garcinia mangostana on human malignant glioma cells." Molecules 15.12 (2010): 8953-8966.
[4]. Tewtrakul, Supinya, Chatchai Wattanapiromsakul, and Wilawan Mahabusarakam. "Effects of compounds from Garcinia mangostana on inflammatory mediators in RAW264. 7 macrophage cells." Journal of Ethnopharmacology 121.3 (2009): 379-382.
[5]. Lee, Youngmun, et al. "Inhibition of oxidative neurotoxicity and scopolamine‐induced memory impairment by γ‐Mangostin: in vitro and in vivo evidence." Oxidative medicine and cellular longevity 2019.1 (2019): 3640753.

Protocol of Gamma-Mangostin

Cell experiment [1]:

Cell lines

HCT116, SW480, RKO, DLD1, HT29 and LS174T cell lines

Preparation Method

Cells were grown in 96 well plates and treated with different concentration of Gamma-Mangostin. Proliferation was analyzed by a hexoseaminidase assay. For clonogenicity assay, six-well plates were seeded with 500 viable cells per well and allowed to grow for 24h. The cells were then incubated in the presence of varying concentrations of Gamma-Mangostin for 48h. Gamma-Mangostin containing medium was then removed, and the cells were rinsed in phosphate buffered saline (PBS) and incubated for an additional 10 days in complete medium. The colonies obtained were washed with PBS and fixed in 10% formalin for 10 minutes at room temperature, followed by washing with PBS and staining with Crystal violet.

Reaction Conditions

0-40µM; 48h

Applications

The 50% inhibitory concentration values of Gamma-Mangostin at 48 hours were ranging from 10-15µM for colon cancer cell lines.
Animal experiment [2]:

Animal models

Six-week-old ICR mice

Preparation Method

The animals were orally administered with Gamma-Mangostin (5, 10, and 30mg/kg in 40%v/v PEG in water), donepezil (10mg/kg), or vehicle (for control and scopolamine groups). After 30min of administration, memory impairment was induced by intraperitoneal administration of scopolamine (3mg/kg, prepared in normal saline); the control group received normal saline only. Following 30min of scopolamine injection, the acquisition trial was initiated.

Dosage form

5, 10, and 30mg/kg; oral; once

Applications

The groups administered with Gamma-Mangostin at the dosages of 10 and 30mg/kg significantly restored the scopolamine-induced decrease in time latency.

References:
[1]. Krishnamachary, Balaji, et al. "Targeting transcription factor TCF4 by γ-Mangostin, a natural xanthone." Oncotarget 10.54 (2019): 5576.
[2]. Lee, Youngmun, et al. "Inhibition of oxidative neurotoxicity and scopolamine‐induced memory impairment by γ‐Mangostin: in vitro and in vivo evidence." Oxidative medicine and cellular longevity 2019.1 (2019): 3640753.

Chemical Properties of Gamma-Mangostin

Cas No. 31271-07-5 SDF
Canonical SMILES O=C1C2=C(OC3=C1C(C/C=C(C)\C)=C(O)C(O)=C3)C=C(O)C(C/C=C(C)\C)=C2O
Formula C23H24O6 M.Wt 396.43
Solubility DMSO: 250 mg/mL (630.63 mM) Storage Store at 2-8°C
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Gamma-Mangostin

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1 mg 5 mg 10 mg
1 mM 2.5225 mL 12.6126 mL 25.2251 mL
5 mM 504.5 μL 2.5225 mL 5.045 mL
10 mM 252.3 μL 1.2613 mL 2.5225 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 28 reference(s) in Google Scholar.)

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