2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. ATM/ATR Checkpoint Kinase (Chk) MDM-2/p53 E1/E2/E3 Enzyme CDK Reactive Oxygen Species (ROS) Apoptosis
  4. Americanin A

Americanin A，一种 neolignan，可从 Phytolacca americana 的种子中分离得到。Americanin A 可激活 ATM 和 ATR，从而启动后续的信号转导级联反应，包括 Chk1、Chk2 以及肿瘤抑制蛋白 p53。Americanin A 选择性地靶向 Skp2 进行降解，从而稳定 p27。Americanin A 抑制 Cyclin B1 及其结合伙伴 cdc2 的活性，以阻止进入有丝分裂 (Mitosis)。Americanin A 通过产生过量的 ROS 诱导细胞凋亡 (Apoptosis)。Americanin A 对结直肠癌具有抗肿瘤活性。

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Americanin A

Americanin A Chemical Structure

CAS No. : 69506-79-2

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Americanin A 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Americanin A is a neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer[1].

IC50 & Target[1]

Chk1

 

Chk2

 

ATM

 

ATR

 

体外研究
(In Vitro)

Americanin A (24-72 h) 可选择性抑制人类癌细胞的增殖 (IC₅₀ 9.0-66.4 μM)，对 MRC-5 正常细胞无显著作用，并以浓度和时间依赖的方式抑制 HCT116 细胞[1]。
Americanin A (7.5-30 μM；24 h) 可诱导 HCT116 细胞发生 G2/M 期细胞周期阻滞，其中 30 μM 浓度可使 G2/M 期细胞占比提升至 38.9%[1]。
Americanin A (7.5-30 μM；24 h) 可诱导 HCT116 细胞发生 DNA 损伤，表现为磷酸化 H2A.X 水平升高和乙酰化 H3 水平降低 [1]。
Americanin A (7.5-30 μM；48 h) 可诱导 HCT116 细胞发生细胞凋亡，其中 30 μM 浓度处理可使亚 G1 期细胞占比升高至 52.0%[1]。

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

Americanin A 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A549, Caki-1, K562, HCT116, SW480, HCT-15, RKO, MRC-5
Concentration: IC₅₀ values (9.0–66.4 μM for cancer cells; >100 μM for MRC-5)
Incubation Time: 24 h, 48 h, 72 h
Result: Inhibited proliferation of A549 (IC₅₀ 39.1 μM), Caki-1 (IC₅₀ 66.4 μM), K562 (IC₅₀ 12.9 μM), HCT116 (IC₅₀ 9.0 μM), SW480 (IC₅₀ 27.4 μM), HCT-15 (IC₅₀ 12.5 μM), RKO (IC₅₀ 24.4 μM) cells; measured HCT116 IC₅₀ values of 24.1 μM (24 h), 9.6 μM (48 h), 8.7 μM (72 h); showed no significant inhibition of MRC-5 cells (IC₅₀ > 100 μM).

Cell Cycle Analysis[1]

Cell Line: HCT116
Concentration: 7.5, 15, 30 μM
Incubation Time: 24 h
Result: Increased the proportion of G₂/M phase cells from 20.6% (untreated) to 38.9% at 30 μM; increased sub-G₁ cell proportion (apoptosis indicator) concentration-dependently, but the increase was not significant at 24 h.

Western Blot Analysis[1]

Cell Line: HCT116
Concentration: 7.5, 15, 30 μM
Incubation Time: 24 h
Result: Suppressed expression of cyclin A, cyclin B1, phosphorylated cyclin B1 (Ser147), CDK2, and cdc2 in a concentration-dependent manner.\nIncreased phosphorylation of histone H2A.X (Ser139) and decreased acetylation of histone H3 (Lys9) concentration-dependently.

Apoptosis Analysis[1]

Cell Line: HCT116
Concentration: 7.5, 15, 30 μM
Incubation Time: 48 h
Result: Increased sub-G₁ cell proportion from 6.5% (untreated) to 52.0% at 30 μM; showed increased early and late apoptotic cells concentration-dependently via annexin V/FITC staining.
体内研究
(In Vivo)

Americanin A (5-10 mg/kg；腹腔注射；每周 3 次) 可通过 Skp2 依赖的 p27 稳定作用抑制裸鼠体内 HCT116 肿瘤异种移植物的生长，在 5 mg/kg 和 10 mg/kg 剂量下的肿瘤体积抑制率分别为 45.0%和 55.7%[1]。

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

Animal Model: BALB/c-nu (female, 4-6 weeks old, HCT116 tumor xenograft)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: i.p.; three times a week
Result: Reduced tumor volumes by 45.0% (5 mg/kg) and 55.7% (10 mg/kg) compared to vehicle; Increased expressions of p21 and p27, and decreased Skp2 expression in excised tumors; Showed pronounced p27 staining and diminished Skp2 and Ki-67 staining via immunohistochemistry; Observed no overt toxicity or body weight changes.
分子量

328.32

Formula

C18H16O6
CAS 号
结构分类
初始来源
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.
纯度 & 产品资料
参考文献

Americanin A 相关分类

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Keywords:

Americanin A69506-79-2ATM/ATRCheckpoint Kinase (Chk)MDM-2/p53E1/E2/E3 EnzymeCDKReactive Oxygen Species (ROS)ApoptosisAtaxia telangiectasia mutatedATM and RAD3 relatedE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseCyclin dependent kinasecyclin B1ATRHCT116 cellscdc2p53Chk2Chk1colon cancerATMSkp2Inhibitorinhibitorinhibit

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