Dryocrassin ABBA
(Synonyms: 东北贯众素) 目录号 : GN10699
Dryocrassin ABBA是一种可口服的、具有抗病毒和抗菌活性的间苯三酚衍生物。
Cas No.:12777-70-7
Sample solution is provided at 25 µL, 10mM.
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Dryocrassin ABBA is an orally active phloroglucinol derivative with antiviral and antibacterial activities[1][2]. Dryocrassin ABBA not only exhibits inhibitory activity against the neuraminidases (NAs) of the H7N9 influenza virus, with an IC50 of 3.6μM[2]; but also inhibits the SrtA enzyme of Staphylococcus aureus (S. aureus), with an IC50 of 24.17μM[3].
In vitro, pretreatment of mouse bone marrow-derived DCs (mBM-DCs) with 10 or 20μM Dryocrassin ABBA 1h before lipopolysaccharide (LPS) stimulation significantly reduced the LPS-induced emission of tumor necrosis factor-a, interleukin-6, and interleukin-12p70 without affecting cell viability[4].Treatment of HepG2 cells with 25, 50, and 75μg/mL Dryocrassin ABBA for 48h inhibited the growth of HepG2 cells in a concentration-dependent manner[5].
In vivo, oral administration of Dryocrassin ABBA with different concentration(12.5, 18, and 33mg/kg) for 7 days on SPF BALB/C female mice inoculated intra-nasally with H5N1 viruses significantly reduced mortality, prolonged survival rate, and increased body weight throughout the infection period. Moreover, 33 and 18mg/kg Dryocrassin ABBA have decreased lung index and virus loads, and significantly increased MCP-1 and IL-10 while significantly decreased IL-12, IL-6, IFN-γ and TNF-α compared to the untreated group[6]. Subcutaneous injection of Dryocrassin ABBA(100mg/kg) every 12h for 96h can attenuate injury and inflammation of mouse lung tissues caused by S. aureus and increase survival of mice[7].
References:
[1] Jin, Y. H., Jeon, S., Lee, J., Kim, S., Jang, M. S., Park, C. M., Song, J. H., Kim, H. R., & Kwon, S. (2022). Anticoronaviral Activity of the Natural Phloroglucinols, Dryocrassin ABBA and Filixic Acid ABA from the Rhizome of Dryopteris crassirhizoma by Targeting the Main Protease of SARS-CoV-2. Pharmaceutics, 14(2), 376.
[2] Hou, B., Liu, Z., Yang, X. B., Zhu, W. F., Li, J. Y., Yang, L., Reng, F. C., Lv, Y. F., Hu, J. M., Liao, G. Y., & Zhou, J. (2019). Total synthesis of dryocrassin ABBA and its analogues with potential inhibitory activity against drug-resistant neuraminidases. Bioorganic & medicinal chemistry, 27(17), 3846–3852.
[3] Zhang, B., Wang, X., Wang, L., Chen, S., Shi, D., & Wang, H. (2016). Molecular Mechanism of the Flavonoid Natural Product Dryocrassin ABBA against Staphylococcus aureus Sortase A. Molecules (Basel, Switzerland), 21(11), 1428.
[4] Fu, R. H., Wang, Y. C., Liu, S. P., Shih, T. R., Lin, H. L., Chen, Y. M., Tsai, R. T., Tsai, C. H., Shyu, W. C., & Lin, S. Z. (2014). Dryocrassin suppresses immunostimulatory function of dendritic cells and prolongs skin allograft survival. Cell transplantation, 23(4-5), 641–656.
[5] Jin, Z., Wang, W. F., Huang, J. P., Wang, H. M., Ju, H. X., & Chang, Y. (2016). Dryocrassin ABBA Induces Apoptosis in Human Hepatocellular Carcinoma HepG2 Cells Through a Caspase-Dependent Mitochondrial Pathway. Asian Pacific journal of cancer prevention : APJCP, 17(4), 1823–1828.
[6] Ou, C., Zhang, Q., Wu, G., Shi, N., & He, C. (2015). Dryocrassin ABBA, a novel active substance for use against amantadine-resistant H5N1 avian influenza virus. Frontiers in microbiology, 6, 592.
[7] Li, B., Jin, Y., Xiang, H., Mu, D., Yang, P., Li, X., Zhong, L., Cao, J., Xu, D., Gong, Q., Wang, T., Wang, L., & Wang, D. (2019). An Inhibitory Effect of Dryocrassin ABBA on Staphylococcus aureus vWbp That Protects Mice From Pneumonia. Frontiers in microbiology, 10, 7.
Dryocrassin ABBA是一种可口服的、具有抗病毒和抗菌活性的间苯三酚衍生物[1][2]。Dryocrassin ABBA不仅对H7N9流感病毒的神经氨酸酶（NAs）具有抑制作用，IC50值为3.6μM[2]；而且对金黄色葡萄球菌（S. aureus）的SrtA酶也有抑制作用，IC50为24.17μM[3]。
在体外实验中，在脂多糖（LPS）刺激前1h用10或20μM Dryocrassin ABBA预处理小鼠骨髓源性树突状细胞（mBM-DCs）可显著降低LPS诱导的肿瘤坏死因子-a、白细胞介素-6和白细胞介素-12p70的释放，且不影响细胞活力[4]。以25、50和75μg/mL Dryocrassin ABBA处理HepG2细胞 48h 后，HepG2细胞的生长以浓度依赖性的方式受到抑制[5]。
在体内，对经鼻内接种H5N1病毒的SPF级BALB/C雌性小鼠口服不同浓度（12.5、18和33mg/kg）的Dryocrassin ABBA 7天，可显著降低死亡率，延长存活率，并增加整个感染期的体重。此外，与未处理组相比，33和18mg/kg Dryocrassin ABBA处理还可显著降低肺指数和病毒载量，且显著升高MCP-1和IL-10，显著降低IL-12、IL-6、IFN-γ和TNF-α[6]。在96h内每隔12h给感染黄色葡萄球菌的小鼠皮下注射Dryocrassin ABBA (100mg/kg)，可减轻金黄色葡萄球菌对小鼠肺组织的损伤和炎症，提高小鼠的存活率[7]。
| Cell experiment [1]: | |
Cell lines | mouse bone marrow-derived DCs (mBM-DCs) |
Preparation Method | mBM-DCs were pretreated with 10 or 20μM Dryocrassin ABBA for 1h. After 1h of incubation, the cells were washed twice using PBS, followed by stimulation with 100ng/mL LPS for 20h. Media and cells were collected for subsequent evaluation of DC activation and analysis of protein expression. Three replicates were included in each experiment. |
Reaction Conditions | 10 or 20μM；1h |
Applications | Dryocrassin ABBA significantly reduced the LPS-induced emission of tumor necrosis factor-a, interleukin-6, and interleukin-12p70. The expression of LPS-induced major histocompatibility complex class II, CD40, and CD86 on DCs was also blocked by Dryocrassin ABBA. |
| Animal experiment [2]: | |
Animal models | SPF BALB/C female mice |
Preparation Method | 120 female BALB/C mice were randomly divided into six groups with 20 mice per group. The control group was administrated saline intra-nasally, while the remaining five groups were inoculated intra-nasally with 104.5 ELD50 H5N1 viruses in 100μl saline. On day 2 post inoculation mice received 0.2ml of Dryocrassin ABBA or amantadine hydrochloride by oral gavages. The dosages of the three Dryocrassin ABBA groups were 12.5, 18, and 33mg/kg body weight, and 20mg/kg body weight of amantadine hydrochloride was used as the positive drug control. Mice were given drugs for 7 days from Day 2 to Day 8. Meanwhile, the untreated and control groups received equivalent amounts of physiological saline daily. Body weight, activity, mortality rate, and survival time were monitored daily for 14 days post inoculation. |
Dosage form | 12.5, 18, and 33mg/kg/day for 7 days; p.o. |
Applications | Dryocrassin ABBA significantly reduced mortality, prolonged survival rate, and increased body weight throughout the infection period. 33 and 18mg/kg Dryocrassin ABBA have decreased lung index and virus loads, and significantly increased MCP-1 and IL-10 while significantly decreased IL-12, IL-6, IFN-γ and TNF-α compared to the untreated group. |
References: | |
| Cas No. | 12777-70-7 | SDF | |
| 别名 | 东北贯众素 | ||
| 化学名 | 2-acetyl-4-[[3-[[3-[(5-acetyl-2,6-dihydroxy-3,3-dimethyl-4-oxocyclohexa-1,5-dien-1-yl)methyl]-5-butanoyl-2,4,6-trihydroxyphenyl]methyl]-5-butanoyl-2,4,6-trihydroxyphenyl]methyl]-3,5-dihydroxy-6,6-dimethylcyclohexa-2,4-dien-1-one | ||
| Canonical SMILES | CCCC(=O)C1=C(C(=C(C(=C1O)CC2=C(C(C(=O)C(=C2O)C(=O)C)(C)C)O)O)CC3=C(C(=C(C(=C3O)C(=O)CCC)O)CC4=C(C(C(=O)C(=C4O)C(=O)C)(C)C)O)O)O | ||
| 分子式 | C43H48O16 | 分子量 | 820.29 |
| 溶解度 | 储存条件 | -20°C, protect from light | |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2191 mL | 6.0954 mL | 12.1908 mL |
| 5 mM | 0.2438 mL | 1.2191 mL | 2.4382 mL |
| 10 mM | 0.1219 mL | 0.6095 mL | 1.2191 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00%
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