Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.

Wnt^[1]

Gigantol decreases the level of phosphorylated LRP6 and cytosolic β-catenin in HEK293 cells. In breast cancer MDA-MB-231 and MDA-MB-468 cells, treatment with gigantol reduces the level of phosphorylated LRP6^[1]. Gigantol significantly inhibits the proliferation and induces apoptosis of the HepG2 cells. Gigantol at concentrations of 1, 40 and 150 µM markedly decreases the cell viability by 11.7, 30.0 and 56.4% at 24 h and 21.1, 66.8 and 85.5% at 48 h, respectively. The IC₅₀ value is 9.30 µM^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

LDD and gigantol (25–100 mg/kg, p.o.) significantly increase the hot-plate latency in comparison to vehicle-treated mice and decreased carrageenaninduced inflammation in rats^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

274.31

C₁₆H₁₈O₄

67884-30-4

Room temperature in continental US; may vary elsewhere.

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : ≥ 100 mg/mL (364.55 mM)

Ethanol : 50 mg/mL (182.28 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (9.11 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (9.11 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (9.11 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (9.11 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (9.11 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (9.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Yu S, et al. Gigantol inhibits Wnt/β-catenin signaling and exhibits anticancer activity in breast cancer cells. BMC Complement Altern Med. 2018 Feb 14;18(1):59.

  [2]. Chen H, et al. Gigantol attenuates the proliferation of human liver cancer HepG2 cells through the PI3K/Akt/NF-κB signaling pathway. Oncol Rep. 2017 Feb;37(2):865-870.

  [3]. Déciga-Campos M, et al. Antinociceptive and anti-inflammatory effects of compounds isolated from Scaphyglottis livida and Maxillaria densa. J Ethnopharmacol. 2007 Nov 1;114(2):161-8.

HepG2 cells are treated with a series of concentrations of Gigantol (1, 10, 40, 80 and 150 µM) for different time intervals (12, 24 and 48 h). The cytotoxicity is measured using MTT assays^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Rats^[3]

The anti-inflammatory activity is determined by carrageenan-induced edema test in the hind paws of rats. Sprague-Dawley rats are fasted for 15 h before the experiment with free access to water. One hundred microlitres of 1% carrageenan (10 mg/mL, Type IV, lambda) suspension is prepared 30 min before each experiment and injected into the plantar side of right hindpaw of the rats. The CH₂Cl₂-MeOH Scaphyglottis livida and Maxillaria densa extracts (150-600 mg/kg), as well as compound LDD and gigantol (25-100 mg/kg), are orally administered. The extracts, LDD and gigantol are administered 1 h before the carrageenan treatment^[3].

Mice^[3]

Mice receive an oral administration of vehicle (0.2% Tween-80) or increasing doses of Scaphyglottis livida and Maxillaria densa extracts (150–600 mg/kg) or LDD and gigantol (25-100 mg/kg) 30 min before the thermal noxious stimuli in the hot-plate test. Morphine (1.5-6 mg/kg, p.o.) is used as positive control. Mice are observed before and at 30, 60, 90 and 120 min after drugs administration^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Yu S, et al. Gigantol inhibits Wnt/β-catenin signaling and exhibits anticancer activity in breast cancer cells. BMC Complement Altern Med. 2018 Feb 14;18(1):59.

  [2]. Chen H, et al. Gigantol attenuates the proliferation of human liver cancer HepG2 cells through the PI3K/Akt/NF-κB signaling pathway. Oncol Rep. 2017 Feb;37(2):865-870.

  [3]. Déciga-Campos M, et al. Antinociceptive and anti-inflammatory effects of compounds isolated from Scaphyglottis livida and Maxillaria densa. J Ethnopharmacol. 2007 Nov 1;114(2):161-8.