Robustine
(Synonyms: 大叶桉亭) 目录号 : GC60329Robustine,是一种来自 Dictamnus albus 的呋喃喹啉生物碱,在体外对人磷酸二酯酶 5 (hPDE5A) 具有抑制作用。
Cas No.:2255-50-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Robustine, a furoquinoline alkaloid, from Dictamnus albus, exhibits inhibitory potency against human phosphodiesterase 5 (hPDE5A) in vitro[1].
[1]. Nam KW, et al. Inhibitory effects of furoquinoline alkaloids from Melicope confusa and Dictamnus albus against human phosphodiesterase 5 (hPDE5A) in vitro. Arch Pharm Res. 2005 Jun;28(6):675-9.
Cas No. | 2255-50-7 | SDF | |
别名 | 大叶桉亭 | ||
Canonical SMILES | OC1=C2N=C(OC=C3)C3=C(OC)C2=CC=C1 | ||
分子式 | C12H9NO3 | 分子量 | 215.2 |
溶解度 | 储存条件 | 4°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。 |
||
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.6468 mL | 23.2342 mL | 46.4684 mL |
5 mM | 0.9294 mL | 4.6468 mL | 9.2937 mL |
10 mM | 0.4647 mL | 2.3234 mL | 4.6468 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。
Active constituents of Zanthoxylum nitidium from Yunnan Province against leukaemia cells in vitro
BMC Chem 2021 Jul 23;15(1):44.PMID:34301301DOI:10.1186/s13065-021-00771-0.
Zanthoxylum nitidium (Roxb.) DC (Rutaceae) is well known for inhibiting the proliferation of human gastric, liver, kidney and lung cancer cells, though research on its potential use in treating leukaemia is relatively rare. Twenty-six compounds were isolated from the chloroform and petroleum ether extracts of the roots and leaves of Z. nitidium (Zanthoxylum nitidium). They were ( +)-9'-O-transferuloyl-5, 5'-dimethoxylaricriresinol (1), 8-(3'-oxobut-1'-en-1'-yl)-5, 7-dimethoxy-coumarin (2), 5, 7, 8-trimethoxy-coumarin (3), 5-(3', 3'-dimethyl-2'-butenyloxy)-7, 8-dimethoxy-coumarin (4), 2-(5-methoxy-2-methyl-1H-indol-3-yl) methyl acetate (5), 2'-(5, 6-dihydrochleletrythrine-6-yl) ethyl acetate (6), 6-acetonyldi-hydrochelerythrine (7), 6β-hydroxymethyldihydronitidine (8), bocconoline (9), zanthoxyline (10), O-methylzanthoxyline (11), rhoifoline B (12), N-nornitidine (13), nitidine (14), chelerythrine (15), 4-hydroxyl-7,8-dimethoxy-furoquinoline (16), dictamnine (17), γ-fagarine (18), skimmianine (19), Robustine (20), R-( +)-platydesmine (21), 4-methoxyl-1-methyl-2-quinoline (22), 4-methoxy-2-quinolone (23), liriodenine (24), aurantiamide acetate (25), 10-O-demethyl-12-O-methylarnottianamide (26). Four among them, compounds 4 - 6 and 16, were first confirmed in this study by UV, IR, 1D, 2D NMR and HR-ESI-MS spectra. Compounds 1 - 2 and 11 were isolated from Z. nitidium for the first time. Of the assayed compounds, 1, 2, 9, 10, 14, 15 and 24, exhibited good inhibitory activities in the leukaemia cell line HEL, whereas compound 14 (IC50: 3.59 µM) and compound 24 (IC50: 15.95 µM) exhibited potent inhibitory activities. So, to further investigate the possible mechanisms, cell cycle and apoptosis assays were performed, which indicated that compound 14 causes obvious S-phase arrest in HEL cells and induced apoptosis, whereas compound 24 only induced apoptosis. The present results suggested both compounds 14 and 24 are promising potential anti-leukaemia drug candidates.
A new quinoline alkaloid from the roots of Dictamnus angustifolius
Chin J Nat Med 2014 Mar;12(3):222-4.PMID:24702810DOI:10.1016/S1875-5364(14)60037-6.
Aim: To investigate the quinoline alkaloids from the roots of Dictamnus angustifolius G.Don ex Sweet (Rutaceae). Method: The quinoline alkaloids were isolated by various column chromatographic methods and their structures were elucidated on the basis of spectral analysis. Results: A new quinoline alkaloid, 5-methoxylrobustine (1), along with five known quinoline alkaloids were obtained, and their structures were identified as dictamnine (2), Robustine (3), isopteleine (4), γ-fagarine (5), and skimmianine (6). Cytotoxicity testing of these alkaloids showed that all of them had weak cytotoxic activities against human breast cancer cells (MCF7). Conclusion: Compound 1 is a new quinoline alkaloid. Alkaloid 3 showed stronger anti-proliferation effect than the other alkaloids.
Neolignans, a coumarinolignan, lignan derivatives, and a chromene: anti-inflammatory constituents from Zanthoxylum avicennae
J Nat Prod 2008 Feb;71(2):212-7.PMID:18211005DOI:10.1021/np070594k.
Eight new compounds, including four new neolignans, (7' S,8' S)-bilagrewin ( 1), (7' S,8' S)-5-demethoxybilagrewin ( 2), (7' S,8' S)-5- O-demethyl-4'- O-methylbilagrewin ( 3), and (7' S,8' S)-nocomtal ( 4), a new coumarinolignan, (7' S,8' S)-4'- O-methylcleomiscosin D ( 5), two new lignan derivatives, (+)-9'- O-( Z)-feruloyl-5,5'-dimethoxylariciresinol ( 6) and (+)-9'- O-( E)-feruloyl-5,5'-dimethoxylariciresinol ( 7), and a new chromene, ( E)-3-(2,2-dimethyl-2 H-chromen-6-yl)prop-2-enal ( 8), have been isolated from the stem wood of Zanthoxylum avicennae, together with 18 known compounds ( 9- 26). The structures of these new compounds were determined through spectroscopic and MS analyses. (7' S,8' S)-4'- O-Methylcleomiscosin D ( 5), cleomiscosin D ( 9), skimmianine ( 18), Robustine ( 19), and integrifoliolin ( 23) exhibited inhibition (IC 50 < or = 18.19 microM) of superoxide anion generation by human neutrophils in response to formyl- l-methionyl- l-leucyl- l-phenylalanine/cytochalasin B (FMLP/CB). In addition, skimmianine ( 18) inhibited FMLP/CB-induced elastase release with an IC 50 value of 19.15 +/- 0.66 microM.
A new prenylated arylnaphthalene lignan from Haplophyllum myrtifolium
Fitoterapia 2003 Sep;74(6):564-9.PMID:12946719DOI:10.1016/s0367-326x(03)00147-3.
A novel prenylated arylnaphthalene lignan, 7-O-(3-methyl-2-butenyl)isodaurinol, was isolated from Haplophyllum myrtifolium and identified on the basis of detailed spectral analyses, including 2D-NMR spectrometry. The known furoquinoline alkaloids, dictamnine, Robustine, gamma-fagarine and skimmianine, the aryltetralin lignan (-)-1beta-polygamain and the flavone chrysosplenetin were isolated from the same source.
Alkaloids and coumarins of Thamnosma montana
Lloydia 1976 Mar-Jun;39(2-3):134-40.PMID:948238doi
From the turpentine broom, Thamnosma montana, four alkaloids and three coumarins were isolated and characterized. Skimmianine (5), N-methyl-acridone (4) and 5-(3'-methyl-2',3'-dihydroxybutanyl)-8-methoxypsoralen (1) were obtained previously from T. montana. Robustine (2) is reported from a Thamnosma species for the first time and acridone (6), thamnosmonin (9), and thamontanin (14) are reported from a natural source for the first time. Evidence for the structures of the new isolates is presented.