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  3. Bartogenic acid

Bartogenic acid 是一种 NF-κB 抑制剂,可于玉蕊 (Barringtonia racemosa) 果实中发现。Bartogenic acid 可提高过氧化氢酶、超氧化物歧化酶及谷胱甘肽水平。Bartogenic acid 抑制脂质过氧化并下调炎症标志物表达。Bartogenic acid 可用于卵巢癌、皮肤癌及炎症性疾病的相关研究。

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Bartogenic acid

Bartogenic acid Chemical Structure

CAS No. : 79355-89-8

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  • 生物活性

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生物活性

Bartogenic acid is an orally active NF-κB inhibitor, found in Barringtonia racemosa fruits. Bartogenic acid increases catalase, superoxide dismutase, and glutathione levels. Bartogenic acid inhibits lipid peroxidation and suppresses inflammation markers. Bartogenic acid can be used for the research of ovarian cancer, skin cancer, and inflammatory conditions[1][2][3][4].

IC50 & Target[1]

NF-κB

 

体外研究
(In Vitro)

Bartogenic acid (0.1-100 μM;48 小时) 可在体外抑制人卵巢癌 SKOV-3 细胞的生长,其 IC50 为 15.72 μM[1]
Bartogenic acid (48 h) 可强效且选择性地对人皮肤癌细胞 SCC-13 产生细胞毒性 (IC50=7.5 µM),其选择性指数为 4.05[2]

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

Cell Viability Assay[1]

Cell Line: human ovarian cancer SKOV-3 cells
Concentration: 0.1 μM; 1 μM; 10 μM; 50 μM; 100 μM
Incubation Time: 48 h
Result: Dose-dependently reduced the viability of SKOV-3 cells, with an IC50 value of 15.72 μM after 48 h of treatment.
Decreased as the concentration of bartogenic acid increased.
体内研究
(In Vivo)

Bartogenic acid (3 mg/kg;静脉注射;每日一次;共 21 天) 可使 SCID 小鼠体内 SKOV-3 卵巢肿瘤的生长抑制 41.47%[1]
Bartogenic acid (1-4 mg/kg;口服/局部给药;每日;13.5 周) 对 DMBA (HY-W011845)/巴豆油诱导的 Swiss albino 小鼠皮肤癌具有剂量依赖性化学预防作用,其中 4 mg/kg 口服剂量组的肿瘤发生率最低 (36.1%),且抗氧化标志物水平和皮肤结构接近正常[2]
Bartogenic acid (2-10 mg/kg;口服;每日一次,共 21 天) 可保护大鼠免受 CFA (HY-153808) 诱导的原发性和继发性关节炎损伤、体重变化和血液学紊乱[4]

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

Animal Model: SCID (female, 5 weeks old, subcutaneous inoculation of SKOV-3 cells to establish a xenograft model)[1]
Dosage: 3 mg/kg
Administration: i.v.; daily; 21 days
Result: Achieved 41.47% tumor growth inhibition (p < 0.001) compared to vehicle controls, with mean tumor volume of 364.70 mm3 on day 21.
Showed no significant reduction in NF-κB H score, viable tumor cell score, fibrosis score, TGF-β1 levels, or MMP9 levels, but significantly increased necrosis score (p < 0.05).
Animal Model: Swiss albino (6-8 weeks old, 23-25 gm, DMBA/Croton oil-induced two-stage skin carcinogenesis)[2]
Dosage: 1 mg/kg; 2 mg/kg; 4 mg/kg
Administration: p.o.; daily; 13.5 weeks; topical; daily; 13.5 weeks
Result: Reduced tumor incidence to 89.3%, with an average of 9.72 tumors per tumor-bearing mouse, mean tumor volume of 124.8 mm3, and mean tumor weight of 1.01 gm at 1 mg/kg oral dose.
Partially restored glutathione (GSH) content and activities of catalase, superoxide dismutase (SOD), and glutathione peroxidase (GSHPx), with mild histopathological improvement at 1 mg/kg oral dose.
Reduced tumor incidence to 52.4%, with an average of 6.34 tumors per tumor-bearing mouse, mean tumor volume of 89.7 mm3, and mean tumor weight of 0.61 gm at 2 mg/kg oral dose.
Significantly reduced skin malondialdehyde (MDA) levels to 125.7 μg/mg protein, restored GSH content to near-normal levels, significantly increased catalase, SOD, and GSHPx activities, and preserved normal skin architecture with only mild epidermal cell invasion at 2 mg/kg oral dose.
Reduced tumor incidence to 36.1%, with an average of 4.19 tumors per tumor-bearing mouse, mean tumor volume of 45.6 mm3, and mean tumor weight of 0.11 gm at 4 mg/kg oral dose.
Significantly reduced skin MDA levels to 104.5 μg/mg protein, restored GSH content and catalase, SOD, and GSHPx activities to near-normal levels, and preserved fully normal skin architecture with no epidermal thickening or cell invasion at 4 mg/kg oral dose.
Reduced tumor incidence to 48.2%, with an average of 8.21 tumors per tumor-bearing mouse, mean tumor volume of 63.5 mm3, and mean tumor weight of 0.51 gm at 4 mg/kg topical dose.
Reduced skin MDA levels to 141.6 μg/mg protein, restored GSH content and catalase, SOD, and GSHPx activities to near-normal levels, and showed mild to moderate histopathological improvement at 4 mg/kg topical dose.
Animal Model: Wistar rats (either sex, 100-150 g, Complete Freund’s Adjuvant-induced arthritis)[3]
Dosage: 2 mg/kg; 5 mg/kg; 10 mg/kg
Administration: p.o.; daily; 21 days
Result: Reduced primary arthritic lesions to 113% rise in injected paw volume and secondary lesions to 15% rise in non-injected paw volume at 2 mg/kg, 109% rise and 12% rise at 5 mg/kg, and 91% rise and 11% rise at 10 mg/kg (all P < .01).
Resulted in 37 g body weight gain at 2 mg/kg, 36 g gain at 5 mg/kg, and 39 g gain at 10 mg/kg (all P < .01).
Reduced thymus weight to 0.12 g and spleen weight to 0.96 g at 2 mg/kg, 0.12 g and 0.84 g at 5 mg/kg, and 0.085 g and 0.74 g at 10 mg/kg (all thymus weights and 5 mg/kg, 10 mg/kg spleen weights P < .05 or P < .01).
Reduced WBC count to 7.5 ×103/mm3, ESR to 12 mm/h, CRP to 4.4 mg/dL, and RF to 37 IU/mL at 2 mg/kg; increased RBC count to 9 ×106/mm3, reduced WBC count to 7.2 ×103/mm3, increased Hb to 15 mg%, reduced CRP to 2.2 mg/dL, and RF to 33 IU/mL at 5 mg/kg; increased RBC count to 9.8 ×106/mm3, reduced WBC count to 5.6 ×103/mm3, reduced ESR to 11 mm/h, increased Hb to 16 mg%, reduced CRP to 1.4 mg/dL, and RF to 23 IU/mL at 10 mg/kg (all significant vs control, P < .01).
Reduced arthritis score to median 6 (4, 8), flexion pain test score to median 1.5 (1, 2), mobility score to median 1.5 (1, 2), and improved stance score to median 3 (2, 3) at 10 mg/kg (P < .05 or P < .01); 2 mg/kg and 5 mg/kg showed non-significant pain score improvements.
Protected against soft tissue swelling, periarticular bone resorption, bone erosion, and joint space narrowing in the adjuvant-injected paw at 10 mg/kg.
分子量

518.68

Formula

C30H46O7

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
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    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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Bartogenic acid
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HY-N19717
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