1. Apoptosis
  2. Apoptosis MDM-2/p53
  3. Gallium maltolate

Gallium maltolate (GAM) 是一种口服有效的,由镓 (Gallium) 和麦芽酚酸 (Maltolate) 结合而成的化合物。Gallium maltolate 可激活 Hut78 细胞的氧化应激和 p53 通路。Gallium 通过干扰金属蛋白酶 (如铁代谢) 的核心机制,既能抑制细菌生长,促进伤口愈合 (如马增生性肠病、马慢性伤口感染),又能抑制肿瘤细胞增殖、诱导其凋亡 (apotosis) (如皮肤T细胞淋巴瘤、胶质细胞瘤),同时调节免疫微环境。Maltolate 是一种有机配体,能够增强 Gallium 的稳定性和生物利用度。Gallium maltolate 可用于抗炎、抗菌、抗癌研究。

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Gallium maltolate

Gallium maltolate Chemical Structure

CAS No. : 108560-70-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gallium maltolate (GAM) is an orally effective compound formed by the combination of Gallium and Maltolate. Gallium maltolate can activate the oxidative stress and p53 pathways in Hut78 cells. Gallium, through its core mechanism of interfering with metalloproteinases (such as iron metabolism), not only inhibits bacterial growth and promotes wound healing (e.g., equine proliferative enteropathy and equine chronic wound infections) but also inhibits tumor cell proliferation, induces apotosis (e.g., cutaneous T-cell lymphoma and glioma), while regulating the immune microenvironment. Maltolate is an organic ligand that can enhance the stability and bioavailability of gallium. Gallium maltolate can be used in anti-inflammatory, antibacterial, and anticancer research[1][2][3][4][5].

体外研究
(In Vitro)

Gallium maltolate (0-500 μM, 0-4 d) 对 HuT78 和 HH 细胞表现出剂量和时间相关的细胞毒性作用[1]
Gallium maltolate (0-150 μM, 8-24 h) 可诱导 Hut78 细胞凋亡,并导致细胞内氧气消耗率呈剂量依赖性降低[1]
Gallium maltolate (0-1 d) 会激活 Hut78 细胞的氧化应激和 p53 通路[1]
Gallium maltolate 对耐甲氧西林金黄色葡萄球菌 (MRSA) 菌株和非耐药金黄色葡萄球菌 (MSSA) 菌株均显示出 750 μM 的最小抑菌浓度[3]
Gallium maltolate (25-15000 μM) 在抗菌浓度下对皮肤细胞 (hDF) 的影响相对较小,其 IC50 值为 2220 μM[3]

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

Cell Cytotoxicity Assay[1]

Cell Line: HuT78 and HH cells
Concentration: 100, 200, 300, 400 and 500 μM
Incubation Time: 0, 1, 2, 3 and 4 d
Result: More sensitive in HuT78 cells (complete death occurred after 3 days of treatment at 100 μM).
Observed mitochondrial function inhibition at an early stage (8 hours).
Had a relatively low toxicity to normal keratinocytes (HaCaT) and shows selective toxicity.

Apoptosis Analysis[1]

Cell Line: HuT78 cells
Concentration: 100 μM
Incubation Time: 24 h
Result: Showed marked increases of annexin V or 7-AAD positivity.
体内研究
(In Vivo)

Gallium maltolate (400 μg/per mouse, 瘤周注射给药, 每日一次, 持续 5 天) 能有效抑制小鼠皮肤 T 细胞淋巴瘤 (CTCL) 肿瘤的生长,并创造不利于肿瘤生长的微环境[1]
Gallium maltolate (50 mg/kg, 经鼻胃管给药, 每两天一次, 持续 15 周) 在感染家兔中对马增生性肠炎(PEP) 的疗效似乎与 Doxycycline (HY-N0565) 相当[2]
Gallium maltolate (50 mg/kg, p.o., 每日一次, 用药两周,停药一周一个治疗周期) 在大鼠难治性胶质母细胞瘤 (trGBM) 异种移植模型中表现出强效的抗肿瘤作用[4]
Gallium maltolate (1.25 mL/wound, 0.5% 溶于石油基底, 局部给药, 一周两次共 21 天) 对马的非感染性和感染性伤口愈合具有有益作用[5]

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

Animal Model: Hut78 or HH cells induced xenograft CTCL mouse model established in C57BL/6 mice[1]
Dosage: 400 μg/per mouse
Administration: Administered by peritumoral injection, once daily, for 5 consecutive days starting on 1st wk, 2nd wk, or 3rd wk
Result: Preventive treatment (started from the first week) was the most effective, with 60% of the mice showing no tumor formation.
Had a significant inhibitory effect on tumors that had already formed (still effective from the second and third weeks of treatment).
Significantly reduced the vascularization of tumors (CD31+ area).
Increased the chemotactic factors (CXCL10/11) induced by IFN-γ, and decreased the immunosuppressive cytokine IL-10.
Animal Model: Lawsonia intracellularis infection model established in in juvenile female rabbits (5-6 weeks)[2]
Dosage: 50 mg/kg
Administration: By nasogastric tube, every second day for 15 weeks
Result: Was a significant inhibition of weight loss during the treatment period (8-14 days).
No significant reduction in the amount of bacterial DNA.
Did not interfere with the host's generation of protective immune response.
Alleviated the intestinal lesions, but not as effectively as with doxycycline.
Animal Model: Xenograft model of trGBM established in male and female athymic rats (180-250g)[4]
Dosage: 50 mg/kg
Administration: Oral administration (p.o.), once daily on a two-week on, one-week off treatment cycle
Result: Significantly reduced the growth rate and delayed the progression time of the tumor.
The risk of death has decreased by 79%.
Neurological symptoms appeared later, weight remained stable and no treatment-related toxicity.
Characterized by an absence of an invasive edge and a significant reduction in both, MIB-1% and mitotic index.
Decreased the expression of pro-angiogenic markers (von Willebrand Factor and VEGF) and increased the expression of anti-angiogenic markers, such as Angiopoietin-2.
Animal Model: Equine wound with non-infected and infected healing model established in horses (mean age was 7 years and mean weight was 446 kg)[5]
Dosage: 1.25 mL/wound, 0.5% in a petroleum base
Administration: Topical administration, twice a week for 21 days
Result: The non-infected wound area has shrunk and the granulation tissue remains flat with TGF-β increasement and MMP decreasement.
The bacterial load in the infected wound decreased, and the wound area shrank by 69% in the fourth week, with inflammation also reduced.
分子量

445.03

Formula

C18H15GaO9

CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
细胞实验: 

H2O 中的溶解度 : 2 mg/mL (4.49 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2470 mL 11.2352 mL 22.4704 mL
5 mM --- --- ---
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* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 2 mg/mL (4.49 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器
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纯度 & 产品资料
参考文献

完整储备液配制表

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.2470 mL 11.2352 mL 22.4704 mL 56.1760 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • 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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Gallium maltolate
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HY-106426
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