Corytuberine
(Synonyms: 紫堇块茎碱) 目录号 : GC35733
Corytuberine 是来自 Dicranostigma leptopodum 的阿朴吗啡生物碱分离物。Corytuberine 对 SMMC-7721 肿瘤细胞显示毒性。
Cas No.:517-56-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Corytuberine is an aporphine alkaloid isolated from Dicranostigma leptopodum. Corytuberine displays cytotoxicity against SMMC-7721 tumor cells[1].
[1]. Sun R, et al. Cytotoxicity of Aporphine, Protoberberine, and Protopine Alkaloids from Dicranostigma leptopodum (Maxim.) Fedde. Evid Based Complement Alternat Med. 2014;2014:580483.
| Cas No. | 517-56-6 | SDF | |
| 别名 | 紫堇块茎碱 | ||
| Canonical SMILES | OC1=C2C3=C(C=C1OC)CCN(C)[C@@]3([H])CC4=CC=C(OC)C(O)=C24 | ||
| 分子式 | C19H21NO4 | 分子量 | 327.37 |
| 溶解度 | Soluble in DMSO | 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。 |
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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 | 3.0546 mL | 15.2732 mL | 30.5465 mL |
| 5 mM | 0.6109 mL | 3.0546 mL | 6.1093 mL |
| 10 mM | 0.3055 mL | 1.5273 mL | 3.0546 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。
Neuroleptic-like, anticonvulsant and antinociceptive effects of aporphine alkaloids: bulbocapnine, Corytuberine, boldine and glaucine
Arch Int Pharmacodyn Ther 1988 Nov-Dec;296:255-81.PMID:2907279doi
The aporphine alkaloids bulbocapnine, Corytuberine, boldine and glaucine were studied in mice and compared with haloperidol, phenobarbital and morphine. All aporphines inhibited the exploratory rearing activity and elicited palpebral ptosis, catalepsy, hypothermia, and prolonged anesthesia by thiopental. They also reduced nociception (hot plate; phenylquinone-induced writhing) and (except for Corytuberine) were anticonvulsant against harman and picrotoxin, but not against bicuculline and pentetrazol; Corytuberine was proconvulsant. The aporphines (except for Corytuberine) antagonized the apomorphine- and methylphenidate-induced stereotyped gnawing and also the apomorphine-induced climbing activity; Corytuberine was prostereotypic. The antignawing effects (including those of haloperidol) were stronger when the antagonists were administered after the agonists (gnawing full-fletched) rather than before them: this led to the speculation of a metaphilic interaction at central site(s). Clonazepam inhibited the antistereotypic effect (vs apomorphine) more potently with the aporphines than with haloperidol. The antinociceptive effect (writhing) of the aporphines was, in contrast to that of morphine, resistant to both naloxone and yohimbine. The latter applied also to the antilicking action in the hot plate test; the antijumping effect of boldine was (like that of morphine) antagonized by both yohimbine and naloxone, whereas that of Corytuberine was inhibited only by naloxone and that of bulbocapnine preferentially by yohimbine. Hence, opioid and adrenergic mechanisms are unequally involved in the antinociceptive effects of the aporphines. The present results also showed that licking and jumping (in the hot plate test) are pharmacologically different phenomena. In low doses, the aporphines and haloperidol antagonized the antinociceptive effect of morphine (hot plate); hence, these drugs may be considered partial agonists or partial antagonists, respectively.
A multi-omics strategy resolves the elusive nature of alkaloids in Podophyllum species
Mol Biosyst 2014 Nov;10(11):2838-49.PMID:25166004DOI:10.1039/c4mb00403e.
Podophyllum hexandrum and, to a much lesser extent P. peltatum, are sources of podophyllotoxin, extensively used as a chemical scaffold for various anti-cancer drugs. In this study, integrated omics technologies (including advanced mass spectrometry/metabolomics, transcriptome sequencing/gene assemblies, and bioinformatics) gave unequivocal evidence that both plant species possess a hitherto unknown aporphine alkaloid metabolic pathway. Specifically, RNA-seq transcriptome sequencing and bioinformatics guided gene assemblies/analyses in silico suggested presence of transcripts homologous to genes encoding all known steps in aporphine alkaloid biosynthesis. A comprehensive metabolomics analysis, including UPLC-TOF-MS and MALDI-MS imaging in situ, then enabled detection, identification, localization and quantification of the aporphine alkaloids, magnoflorine, Corytuberine and muricinine, in the underground and aerial tissues. Interestingly, the purported presence of alkaloids in Podophyllum species has been enigmatic since the 19th century, remaining unresolved until now. The evolutionary and phylogenetic ramifications of this discovery are discussed.
Functional characterizations of malonyl-CoA:acyl carrier protein transacylase (MCAT) in Eimeria tenella
Mol Biochem Parasitol 2012 Jul;184(1):20-8.PMID:22525053DOI:10.1016/j.molbiopara.2012.04.002.
Eimeria tenella, an apicomplexan parasite in chickens, possesses an apicoplast and its associated metabolic pathways including the Type II fatty acid synthesis (FAS II). Malonyl-CoA:acyl-carry protein transacylase (MCAT) encoded by the fabD gene is one of the essential enzymes in the FAS II system. In the present study, the entire E. tenella MCAT gene (EtfabD) was cloned and sequenced. Immunolabeling located this protein in the apicoplast organelle in coccidial sporozoites. Functional replacement of the fabD gene with amber mutation of E. coli temperature-sensitive LA2-89 strain by E. tenella EtMCAT demonstrated that EcFabD and EtMCAT perform the same biochemical function. The recombinant EtMCAT protein was expressed and its general biochemical features were also determined. An alkaloid natural product Corytuberine (CAS: 517-56-6) could specifically inhibit the EtMCAT activity (IC(50)=16.47μM), but the inhibition of parasite growth in vitro by Corytuberine was very weak (the predicted MIC(50)=0.65mM).
Rat CYP2D2, not 2D1, is functionally conserved with human CYP2D6 in endogenous morphine formation
FEBS Lett 2012 Jun 21;586(13):1749-53.PMID:22641033DOI:10.1016/j.febslet.2012.05.021.
The assumption that CYP2D1 is the corresponding rat cytochrome to human CYP2D6 has been revisited using recombinant proteins in direct enzyme assays. CYP2D1 and 2D2 were incubated with known CYP2D6 substrates, the three morphine precursors thebaine, codeine and (R)-reticuline. Mass spectrometric analysis showed that rat CYP2D2, not 2D1, catalyzed the 3-O-demethylation reaction of thebaine and codeine. In addition, CYP2D2 incubated with (R)-reticuline generated four products Corytuberine, pallidine, salutaridine and isoboldine while rat CYP2D1 was completely inactive. This intramolecular phenol-coupling reaction follows the same mechanism as observed for CYP2D6. Michaelis-Menten kinetic parameters revealed high catalytic efficiencies for rat CYP2D2. These findings suggest a critical evaluation of other commonly accepted, however untested, CYP2D1 substrates.
Lipoxygenase inhibition and antioxidant properties of protoberberine and aporphine alkaloids isolated from Mahonia aquifolium
Planta Med 1995 Aug;61(4):372-3.PMID:7480190DOI:10.1055/s-2006-958107.
Products of lipoxygenase metabolism play a role in the pathogenesis of psoriasis. Four protoberberine alkaloids, berberine, oxyberberine, jatrorrhizine, columbamine, and two aporphine alkaloids, magnoflorine, and Corytuberine, isolated from Mahonia aquifolium, were tested for lipoxygenase inhibition. Oxyberberine, Corytuberine, and columbamine were the most potent lipoxygenase inhibitors tested, whereas berberine and magnoflorine exhibited only low potencies. A strong linear correlation (r = 0.866) between lipoxygenase inhibition and lipid antioxidant properties of these compounds was found. These data suggest that the mechanism of lipoxygenase inhibition by these alkaloids may be linked to the inhibition of lipid hydroperoxide substrate accumulation. Inhibition of lipoxygenase by these compounds may contribute to the therapeutic effect of M. aquifolium extracts in the treatment of psoriasis.