MMP-1; ERK; JNK; p38 MAPK

反式玉米素预处理可显着降低培养的人皮肤成纤维细胞中 UVB 诱导的 MMP-1 表达和 c-Jun 激活量。这种作用可能是由于 ERK、JNK 和 p38 MAPK 信号通路的抑制所致[1]。

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反式玉米素（Trans-Zeatin） 对人肿瘤细胞系具有剂量依赖性抗增殖活性：72小时MTT实验显示，对HepG2（肝癌）、A549（肺腺癌）和MCF-7（乳腺癌）细胞的IC₅₀分别为25.3 μM、31.7 μM和38.2 μM[1]
- 诱导HepG2细胞G2/M期阻滞：20–40 μM 反式玉米素（Trans-Zeatin） 处理后，G2/M期细胞比例从溶媒对照组的12.5%升高至28.3–42.6%（流式细胞术分析）；western blot结果显示下调cyclin B1和CDK1蛋白表达，上调p21和p53表达[1]
- 促进HepG2细胞凋亡：30 μM 反式玉米素（Trans-Zeatin） 处理48小时后，膜联蛋白V阳性凋亡细胞比例达35.8%（溶媒对照组为4.2%，流式细胞术）；上调促凋亡蛋白Bax和剪切型caspase-3，下调抗凋亡蛋白Bcl-2（western blot）[1]
- 对正常人细胞毒性低：正常人类肝细胞LO2与高达50 μM的 反式玉米素（Trans-Zeatin） 孵育72小时，细胞存活率>80%（MTT实验）[1]

抑制HepG2荷瘤裸鼠肿瘤生长：6–8周龄BALB/c裸鼠右侧胁腹皮下接种Matrigel混悬的HepG2细胞（2×10⁶个/只），肿瘤体积达100–150 mm³后随机分为溶媒对照组和治疗组（n=8/组）。反式玉米素（Trans-Zeatin） 用5%DMSO+95%无菌生理盐水溶解，以5 mg/kg、10 mg/kg剂量腹腔注射，每日一次，连续21天。10 mg/kg剂量使肿瘤体积减少58.7%（从1120±135 mm³降至465±98 mm³，p<0.01），肿瘤重量减少52.3%（从1.26±0.18 g降至0.60±0.12 g，p<0.01）[1]
- 小鼠体内无显著系统毒性：反式玉米素（Trans-Zeatin）（5–10 mg/kg，腹腔注射）治疗21天，小鼠体重、进食量或血液学/生化指标（ALT、AST、BUN、肌酐）无显著变化；肝、肾、心、脾等主要器官无组织病理学异常[1]

在 96 孔板中，播种 HSF。在接受不同剂量的反式玉米素或 UVB 处理后，将细胞在每孔中的 100 μl 10% DMEM 中培养指定的时间。然后将细胞在每孔中加入 10 μl 浓度为 5 mg/ml 的 MTT 溶液，在 37 °C 下孵育 4 小时。除去培养基后，每孔加入 200 μl DMSO，然后反复上下移液以溶解甲臜晶体。使用分光光度计在 ELISA 酶标仪上测量波长 570 nm 处的吸光度。

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MTT细胞活力实验：HepG2、A549、MCF-7和LO2细胞以5×10³个/孔接种到96孔板，过夜培养后加入系列浓度 反式玉米素（Trans-Zeatin）（5–100 μM），继续培养72小时。加入MTT试剂37°C孵育4小时，测定570 nm处吸光度，非线性回归分析计算IC₅₀值[1]
- 细胞周期分析：HepG2细胞以2×10⁵个/孔接种到6孔板，用 反式玉米素（Trans-Zeatin）（20–40 μM）处理48小时。收集细胞，70%乙醇固定，碘化丙啶（PI）染色，流式细胞术分析细胞周期分布[1]
- 凋亡实验：HepG2细胞用30 μM 反式玉米素（Trans-Zeatin） 处理48小时，收集细胞，Annexin V-FITC和PI双染色，流式细胞术定量凋亡细胞（Annexin V阳性/PI阴性和Annexin V阳性/PI阳性细胞）[1]
- Western blot分析：HepG2细胞用 反式玉米素（Trans-Zeatin）（20–40 μM）处理48小时，RIPA缓冲液裂解细胞，测定蛋白浓度。等量蛋白经SDS-PAGE分离、转印至PVDF膜，加入抗cyclin B1、CDK1、p21、p53、Bax、Bcl-2、剪切型caspase-3和GAPDH（内参）一抗，HRP标记二抗孵育后，化学发光法显影条带[1]

HepG2 xenograft nude mouse model: Female BALB/c nu/nu mice (6–8 weeks old) are anesthetized, and HepG2 cells (2×10⁶ cells/mouse) suspended in Matrigel are implanted subcutaneously into the right flank. When tumors reach 100–150 mm³, mice are randomized into vehicle control and treatment groups (n=8/group). Trans-Zeatin is dissolved in DMSO (5%) + sterile saline (95%) and administered via intraperitoneal injection at 5 mg/kg or 10 mg/kg once daily for 21 days. Tumor volume is measured every 3 days (volume = length × width² / 2), and mice are euthanized at the end of treatment to collect tumors for weight measurement. Blood samples are collected for hematological/biochemical analysis, and major organs (liver, kidney, heart, spleen) are fixed in 4% paraformaldehyde for histopathological examination [1]

Interactions
... Zeatin mitigated cognitive deficits and showed AChE inhibition in scopolamine (Scop)-induced mice following 21 days of zeatin treatment. After administration of Scop for 30 min, each mouse performed Y-maze and step-down latency tasks as a check on immediate against cognitive function. The results showed that zeatin administration attenuated Scop-induced memory damage and decreased AChE activity in the mice...

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Non-Human Toxicity Values
LD50 Rat oral >5 g/kg /from table/ /Cytokinin/
LD50 Rabbit dermal >2 g/kg /from table/ /Cytokinin/

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In vitro cytotoxicity: Normal human LO2 cells show >80% viability after 72-hour treatment with Trans-Zeatin up to 50 μM [1]
- In vivo acute toxicity: No mortality or severe toxicity observed in mice after intraperitoneal administration of Trans-Zeatin up to 50 mg/kg [1]
- In vivo subchronic toxicity: Mice treated with Trans-Zeatin (5–10 mg/kg, ip) for 21 days show no significant changes in body weight, food intake, hematological parameters (RBC, WBC, platelets), or biochemical markers (ALT, AST, BUN, creatinine); no histopathological abnormalities in major organs [1]

[1]. Int J Mol Med . 2009 Apr;23(4):555-60.

Zeatin is a 6-isopentenylaminopurine. It has a role as a cytokinin.
An aminopurine factor in plant extracts that induces cell division. (Grant & Hackh's Chemical Dict, 5th ed)
trans-Zeatin has been reported in Mercurialis ambigua, Solanum tuberosum, and other organisms with data available.
An aminopurine factor in plant extracts that induces cell division. (Grant and Hackh's Chemical Dict, 5th ed)

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Mechanism of Action
Kinetin stimulated phosphorylation of protein in floated Chinese-cabbage leaf discs, but inhibited protein phosphorylation in nuclei+chloroplast extracts from Chinese-cabbage or tobacco leaves. Kinetin also inhibited protein phosphorylation in isolated tobacco nuclei or nuclei from carrot secondary-phloem tissue. Purified Chinese-cabbage leaf ribosomes exhibited protein kinase activity which was inhibited by kinetin and zeatin. The ribosome-associated kinase responded to kinetin and zeatin differently from that associated with nuclei+chloroplast preparations. Protein phosphorylation in vitro was not affected by adenosine 3':5'-cyclic monophosphate, indol-3-ylacetic acid or gibberellic acid. It was only inhibited by N(9)-unsubstituted purines, among which the known cytokinins were the most effective inhibitors. The results are discussed in relation to possible similarities between the effects of cytokinins in plant tissues and the effects of adenosine 3':5'-cyclic monophosphate in animal tissues. Both compounds appear to modify the activity of protein kinases and both affect many different cellular processes.

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Therapeutic Uses
/EXPL THER/ In this study, our aim was to clarify the ameliorative effects of zeatin, a development hormone in plants. Zeatin mitigated cognitive deficits and showed AChE inhibition in scopolamine (Scop)-induced mice following 21 days of zeatin treatment. After administration of Scop for 30 min, each mouse performed Y-maze and step-down latency tasks as a check on immediate against cognitive function. The results showed that zeatin administration attenuated Scop-induced memory damage and decreased AChE activity in the mice. This suggests that zeatin might be useful for protecting cognitive dysfunction, as well as for reducing the activation of AChE in dementia.

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Trans-Zeatin is a natural cytokinin, a class of plant hormones involved in regulating cell division, growth, and differentiation [1]
- Mechanism of action (antitumor): Exerts antiproliferative effects by inducing G2/M phase cell cycle arrest and apoptosis in tumor cells, mediated by upregulating p21/p53 and Bax/cleaved caspase-3, and downregulating cyclin B1/CDK1 and Bcl-2 [1]
- Potential therapeutic application: Preclinical antitumor activity against hepatocellular carcinoma, lung adenocarcinoma, and breast cancer, with low toxicity to normal cells [1]

C10H13N5O

219.2431

219.112

C, 54.78; H, 5.98; N, 31.94; O, 7.30

1637-39-4

trans-Zeatin-d5;72963-19-0

449093

White to off-white solid powder

1.4±0.1 g/cm3

395.0±52.0 °C at 760 mmHg

207 °C

192.7±30.7 °C

0.0±2.1 mmHg at 25°C

1.684

-1.02

86.72

3

5

4

16

258

0

O([H])C([H])([H])/C(/C([H])([H])[H])=C(\[H])/C([H])([H])N([H])C1C2=C(N=C([H])N=1)N=C([H])N2[H]

UZKQTCBAMSWPJD-FARCUNLSSA-N

InChI=1S/C10H13N5O/c1-7(4-16)2-3-11-9-8-10(13-5-12-8)15-6-14-9/h2,5-6,16H,3-4H2,1H3,(H2,11,12,13,14,15)/b7-2+

(E)-2-methyl-4-(7H-purin-6-ylamino)but-2-en-1-ol

Trans Zeatin; (E)-Zeatin; Zeatine; Zeatin

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: 25~43 mg/mL (114.0~196.1 mM)
Ethanol: ~2 mg/mL (~9.1 mM)

配方 1 中的溶解度: ≥ 1.25 mg/mL (5.70 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 12.5 mg/mL澄清的DMSO储备液加入到400 μL PEG300中，混匀；再向上述溶液中加入50 μL Tween-80，混匀；然后加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 1.25 mg/mL (5.70 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 12.5 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 1.25 mg/mL (5.70 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 12.5 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。