Hispidol ((Z)-Hispidol)
(Synonyms: (Z)-Hispidol) 目录号 : GC31739
Hispidol ((Z)-Hispidol) ((Z)-Hispidol ((Z)-Hispidol)) 是炎症性肠病的潜在治疗剂；抑制 TNF-α；诱导单核细胞与结肠上皮细胞的粘附，IC50 为 0.50 μM.
Cas No.:5786-54-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats: To study the effect of the drugs, hispidol (10 or 30 mg/Kg/day in corn oil) is administered orally once in a day, until 5 days after TNBS administration. The doses of 10 or 30 mg/kg are selected based on previous studies. The concentration of the compound inhibiting 70% and 90% (µM) cell-to-cell adhesion is selected and regarded as the in vivo test dose (mg/kg). Sulfasalazine (300 mg/Kg/day) is administered in corn oil as a positive control. On the 6th day, the rats are sacrificed and the severity of colitis and macroscopic ulceration are evaluated by two independent investigators who are blinded to the experiments. The colon tissues (5-7 cm proximal to rectum) are cut and used to measure the amount of myeloperoxidase and for the histological examinations[1]. |
References: [1]. Kadayat TM, et al. Discovery and structure-activity relationship studies of 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives as a novel class of potential therapeutics for inflammatory bowel disease. Eur J Med Chem. 2017 Sep 8;137:575-597. | |
Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 µM.
Hispidol shows potent inhibitory effect (>70%) on the TNF-α-induced adhesion of monocytes to colon epithelial cells, which is one of the hallmark events leading to inflammatory bowel disease (IBD). Hispidol shows strong inhibitory activities against TNF-α-induced monocytic-colonic epithelial cell adhesion as well as LPS-induced TNF-α expression, is as an excellent candidate for IBD drug development. This inhibition of TNF-α expression by hispidol corresponds to the additional inhibitory activity against AP-1 transcriptional activity, which is another transcription factor required for high level TNF-α expression[1].
The oral administration of hispidol suppresses significantly and dose-dependently TNBS-induced rat colitis. Oral administration of hispidol suppresses TNBS-induced colitis in a dose-dependent manner. There is a significant recovery in body weight decrease and colon tissue edematous inflammation. A higher dose (30 mg/kg) of hispidol shows a similar recovery effect to that of 300 mg/kg sulfasalazine. In the colon tissues, TNBS induces a dramatic increase in the level of MPO, a biochemical marker of inflammation, which is suppressed significantly by hispidol in a dose-dependent manner[1].
[1]. Kadayat TM, et al. Discovery and structure-activity relationship studies of 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives as a novel class of potential therapeutics for inflammatory bowel disease. Eur J Med Chem. 2017 Sep 8;137:575-597.
| Cas No. | 5786-54-9 | SDF | |
| 别名 | (Z)-Hispidol | ||
| Canonical SMILES | O=C1C2=CC=C(O)C=C2O/C1=C\C3=CC=C(O)C=C3 | ||
| 分子式 | C15H10O4 | 分子量 | 254.24 |
| 溶解度 | DMSO : ≥ 100 mg/mL (393.33 mM) | 储存条件 | Store at -20°C |
| 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 | 3.9333 mL | 19.6665 mL | 39.3329 mL |
| 5 mM | 0.7867 mL | 3.9333 mL | 7.8666 mL |
| 10 mM | 0.3933 mL | 1.9666 mL | 3.9333 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Elucidation of Flavonoids from Carissa congesta, Polyalthia longifolia, and Benincasa hispida Plant Extracts by Hyphenated Technique of Liquid Chromatography-mass Spectroscopy
Background: Carissa congesta (CC), Polyalthia longifolia (PL), and Benincasa hispida (BH) are economically important plants. Objective: Current research encompasses identification of quercetin and rutin and their analogues by liquid chromatography-mass spectroscopy (LC-MS) from the selected plant species. Materials and methods: Fresh roots, leaves, and seeds of CC, PL, and BH plants respectively were shade-dried followed by extraction and elucidation of rutin and quercetin by LC-MS. Results: Structural elucidation of CC, PL, and BH extracts revealed the presence of flavonoids such as quercetin (m/z 301) and rutin (m/z 610) as the parent ions along with presence of close analogues such as quercetin-O-hexoside, Vicenin 2, quercetin-3-O-xyloside/arabinoside, and quercetin-3-O-glucoside were identified as fragments. Conclusions: Thus, CC, PL, and BH extracts revealed the presence of flavonoids belonging to the class of flavonols such as rutin and quercetin. Summary: Quercetin and rutin were identified from CC roots, PL leaves and BH seeds by liquid chromatography-mass spectroscopy.Quercetin was characterized at (m/z 301) and rutin (m/z 610) as the parent ion peaks.Analogues such as quercetin-O-hexoside, Vicenin 2 and quercetin-3-O-glucoside were identified as fragments.
Using claws to compare reproduction, stress and diet of female bearded and ringed seals in the Bering and Chukchi seas, Alaska, between 1953-1968 and 1998-2014
Rapid climate warming is decreasing sea ice thickness, extent and duration. Marine mammals such as bearded (Erignathus barbatus) and ringed (Pusa hispida) seals, which use sea ice for pupping, molting and resting, may be negatively affected. Claws from bearded and ringed seals store up to 14 and 12 years of sequential analyte data, respectively. These data can be used to compare reproduction, stress and diet across decades. In this study, we compare progesterone, cortisol and carbon and nitrogen stable isotopes in female bearded and ringed seals during 1953-1968 (pre-1968, a period prior to sea ice decline) to 1998-2014 (post-1998, a period during sea ice decline). When comparing these periods, bearded seals had statistically higher cortisol concentrations post-1998, and for both species δ13C was more negative post-1998, while progesterone and δ15N did not change. There was a positive relationship between progesterone and cortisol Z-scores for both species, except for ringed seals post-1998. There was a negative relationship between cortisol Z-scores and δ13C for bearded seals evident in post-1998 indicating that higher cortisol Z-scores are associated with more negative δ13C in bearded seals in recent years. This negative relationship between cortisol and δ13C in bearded seals suggests a shift to higher prey diversity, possibly due to changes in sea ice in the Pacific Arctic evident post 1998. Progesterone Z-scores corresponded to expected differences among non-pregnant, unimplanted, implanted and post-partum individuals. Using these data, pregnancy history was determined for reproductive years for each individual female sampled, which could allow for yearly pregnancy rates to be calculated given a large enough representative sample of the population. These results combine decades of observational studies with hormones and stable isotopes to infer changes in reproduction, stress and diet, as well as the connection between these life history parameters.
Importance of plant species and external silicon concentration to active silicon uptake and transport
Here, we characterized silicon (Si) uptake and xylem loading in Oryza sativa, Zea mays, Helianthus annuus and Benincase hispida in a series of hydroponic experiments. Both active and passive Si-uptake components co-exist in all the plants tested. The active component is the major mechanism responsible for Si uptake in O. sativa and Z. mays. By contrast, passive uptake prevails in H. annuus and B. hispida at a higher external Si concentration (0.85 mM), while the active component constantly exists and contributes to the total Si uptake, especially at a lower external Si concentration (0.085 mM). Short experiments showed that Si uptake was significantly suppressed in O. sativa and Z. mays by metabolic inhibitors or low temperature, regardless of external Si concentrations. By contrast, Si uptake in H. annuus and B. hispida was inhibited more significantly by metabolic inhibitors or low temperature at lower (for example, 0.085 mM) than at higher (for example, 1.70 mM) external Si concentrations. It can be concluded that both active and passive Si-uptake components co-exist in O. sativa, Z. mays, H. annuus and B. hispida, with their relative contribution being dependent much upon both plant species and external Si concentrations.
Analysis of bioactive compounds present in different crude extracts of Benincasa hispida and Cucurbita moschata seeds by gas chromatography-mass spectrometry
Plant seeds are the resources of many different bioactive components. The chemical composition of the different crude extracts from Benincasa hispida (White pumpkin) and Cucurbita moschata (Pumpkin) seeds with three different polarity-based solvents (n-hexane, n-hexane-chloroform (2:1), and methanol) was analyzed to identify the biologically active compounds. Each of the extracts was analyzed by gas chromatography-mass spectrometry. Different extracts of targeted seeds showed different biologically active compounds that have different pharmacological potentialities. 9, 12-Octadecadienoic acid (ZZ) was the most potent bioactive compound present in three different extracts of both B. hispida and C. moschata. Another bioactive compound comparatively low percentage present in both plants was n-hexadecanoic acid. Other major pharmacologically active compounds present in both plants were 9- Octadecenoic acid (Z)-, methyl ester, and 9, 12-Octadecadienoic acid methyl ester (E, E). Besides these compounds, a few more biologically active compounds were present in the two plants separately. The findings of this study support the use of these seeds in modern functional foods, nutraceuticals, and medicinal purposes, and the whole seeds would give better health benefits rather than use any extract. Although further pharmacological examinations should be carried out to conclude the medicinal application of the seeds of these two plants as well as to understand the mechanism of the potential health benefits.