GKK1032B
目录号 : GC45811
A fungal metabolite
Cas No.:358375-11-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >70.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GKK1032B is a fungal metabolite originally isolated from Penicillium sp. GKK1032 that has antiproliferative and antibacterial activities.1,2 GKK1032B inhibits the growth of HeLa S3 cervical and MCF-7 breast cancer cells (IC50s = 17.7 and 14.71 μM, respectively) and Vero cells (IC50 = 29.55 μM). It also inhibits the growth of B. subtilis (MIC = 20.8 μg/ml) and M. tuberculosis (MIC = 48.35 μM).
|1. Li, X.-W., Ear, A., and Nay, B. Hirsutellones and beyond: Figuring out the biological and synthetic logics toward chemical complexity in fungal PKS-NRPS compounds. Nat. Prod. Rep. 30(6), 765-782 (2013).|2. Rukachaisirikul, V., Satpradit, S., Klaiklay, S., et al. Polyketide anthraquinone, diphenyl ether, and xanthone derivatives from the soil fungus Penicillium sp. PSU-RSPG99. Tetrahedron 70(34), 5148-5152 (2014).
| Cas No. | 358375-11-8 | SDF | |
| Canonical SMILES | C[C@@H]1C[C@H](C)[C@]2([H])[C@@]([C@@](C(C)=C[C@@](C=C)(C)[C@]3([H])C4=O)([H])[C@]3([H])[C@]2([H])OC5=CC=C(C[C@@]6([H])[C@@]4([H])C(NC6=O)=O)C=C5)(C)C1 | ||
| 分子式 | C32H39NO4 | 分子量 | 501.7 |
| 溶解度 | Dichloromethane: soluble,DMSO: soluble,Ethanol: soluble | 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 | 1.9932 mL | 9.9661 mL | 19.9322 mL |
| 5 mM | 0.3986 mL | 1.9932 mL | 3.9864 mL |
| 10 mM | 0.1993 mL | 0.9966 mL | 1.9932 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。
GKK1032B from endophytic Penicillium citrinum induces the apoptosis of human osteosarcoma MG63 cells through caspase pathway activation
Chin J Nat Med 2022 Jan;20(1):67-73.PMID:35101251DOI:10.1016/S1875-5364(21)60108-5.
Chemical investigation of the culture extract of an endophytic Penicillium citrinum from Dendrobium officinale, afforded nine citrinin derivatives (1-9) and one peptide-polyketide hybrid GKK1032B (10). The structures of these compounds were determined by spectroscopic methods. The absolute configurations of 1 and 2 were determined for the first time by calculation of electronic circular dichroism (ECD) data. Among them, GKK1032B (10) showed significant cytotoxicity against human osteosarcoma cell line MG63 with an IC50 value of 3.49 μmol·L-1, and a primary mechanistic study revealed that it induced the apoptosis of MG63 cellsvia caspase pathway activation.
GKK1032C, a new alkaloid compound from the endophytic fungus Penicillium sp. CPCC 400817 with activity against methicillin-resistant S. aureus
J Antibiot (Tokyo) 2019 Apr;72(4):237-240.PMID:30737454DOI:10.1038/s41429-019-0144-5.
Five alkaloid compounds (1-5), including one new compound, GKK1032C (1), and four known compounds, pyrrospirones E (2) and F (3), and GKK1032B (4) and A2 (5) were isolated from the culture of endophytic fungus Penicillium sp. CPCC 400817. The planar structures of all compounds were elucidated by NMR and MS spectra. The relative configuration of new compound GKK1032C (1) was deduced from the vicinal J-values and ROESY spectral data. Compound 1 exhibited potent antibacterial activity against methicillin-resistant Staphylococcus aureus with an MIC value of 1.6 μg ml-1.
Chromone Derivatives and Other Constituents from Cultures of the Marine Sponge-Associated Fungus Penicillium erubescens KUFA0220 and Their Antibacterial Activity
Mar Drugs 2018 Aug 20;16(8):289.PMID:30127313DOI:10.3390/md16080289.
A previously unreported chromene derivative, 1-hydroxy-12-methoxycitromycin (1c), and four previously undescribed chromone derivatives, including pyanochromone (3b), spirofuranochromone (4), 7-hydroxy-6-methoxy-4-oxo-3-[(1E)-3-oxobut-1-en-1-yl]-4H-chromene-5-carboxylic acid (5), a pyranochromone dimer (6) were isolated, together with thirteen known compounds: β-sitostenone, ergosterol 5,8-endoperoxide, citromycin (1a), 12-methoxycitromycin (1b), myxotrichin D (1d), 12-methoxycitromycetin (1e), anhydrofulvic acid (2a), myxotrichin C (2b), penialidin D (2c), penialidin F (3a), SPF-3059-30 (7), GKK1032B (8) and secalonic acid A (9), from cultures of the marine sponge- associated fungus Penicillium erubescens KUFA0220. Compounds 1a⁻e, 2a, 3a, 4, 7⁻9, were tested for their antibacterial activity against Gram-positive and Gram-negative reference and multidrug-resistant strains isolated from the environment. Only 8 exhibited an in vitro growth inhibition of all Gram-positive bacteria whereas 9 showed growth inhibition of methicillin-resistant Staphyllococus aureus (MRSA). None of the compounds were active against Gram-negative bacteria tested.