Galgravin
(Synonyms: 盖尔格拉文) 目录号 : GC38610
A lignan with diverse biological activities
Cas No.:528-63-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Galgravin is a lignan that has been found in N. megapotamica and has diverse biological activities.1,2,3,4 It inhibits the binding of platelet-activating factor (PAF) to isolated rabbit platelet plasma membranes (IC50 = 4.5 ?M).1 Galgravin (3-100 ?M) inhibits osteoclast formation induced by RANKL and macrophage colony-stimulating factor (M-CSF) in mouse bone marrow-derived macrophages.2 It protects against cytotoxicity induced by human amyloid-β (25-35) (Aβ (25-35); Item No. 24155) in primary rat hippocampal neurons when used at a concentration of 10 ?M.3 Galgravin (20 mg/kg) reduces acetic acid-induced abdominal constrictions in mice and carrageenan-induced paw edema in rats.4
1.Biftu, T., Gamble, N.F., Doebber, T., et al.Conformation and activity of tetrahydrofuran lignans and analogues as specific platelet activating factor antagonistsJ. Med. Chem.29(10)1917-1921(1986) 2.Asai, M., Lee, J.-W., Itakura, Y., et al.Effects of veraguensin and galgravin on osteoclast differentiation and functionCytotechnology64(3)315-322(2012) 3.Zhai, H., Inoue, T., Moriyama, M., et al.Neuroprotective effects of 2,5-diaryl-3,4-dimethyltetrahydrofuran neolignansBiol. Pharm. Bull.28(2)289-293(2005) 4.da Silva Filho, A.A., Andrade e Silva, M.L., Carvalho, J.C.T., et al.Evaluation of analgesic and anti-inflammatory activities of Nectandra megapotamica (Lauraceae) in mice and ratsJ. Pharm. Pharmacol.56(9)1179-1184(2004)
| Cas No. | 528-63-2 | SDF | |
| 别名 | 盖尔格拉文 | ||
| Canonical SMILES | C[C@H]1[C@@H](C)[C@H](C2=CC=C(OC)C(OC)=C2)O[C@@H]1C3=CC=C(OC)C(OC)=C3 | ||
| 分子式 | C22H28O5 | 分子量 | 372.45 |
| 溶解度 | Soluble in DMSO | 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。 |
||
| 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 | 2.6849 mL | 13.4246 mL | 26.8492 mL |
| 5 mM | 0.537 mL | 2.6849 mL | 5.3698 mL |
| 10 mM | 0.2685 mL | 1.3425 mL | 2.6849 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。
Pharmacokinetic and Bioavailability Studies of Galgravin after Oral and Intravenous Administration to Rats Using HPLC-MS/MS Method
Biomed Res Int 2021 Jul 24;2021:9919789.PMID:34350295DOI:10.1155/2021/9919789.
This paper presents a new high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) method with a rapid analysis of 6 min to determine the concentration of Galgravin in rat plasma so as to study its pharmacokinetic features and bioavailability in vivo. Schisandrin was selected as the internal standard (IS). After extracting the analyte from plasma samples with ethyl acetate, methanol-H2O (0.1% formic acid) (85 : 15, v/v) was used as mobile phase to achieve chromatographic separation on a C18 reversed phase column. The MS detection was performed in positive ion mode using electrospray ionization (ESI) source. This method showed good linearity over the range of 1~500 ng/mL (R 2 > 0.999), and the lower limit of quantitation (LLOQ) was 1.0 ng/mL. The intraday precision and interday precision were both within 8.5%, whereas the accuracies were in the range of -2.6%-6.0%. The average recoveries of Galgravin in rat plasma were between 92.3% and 99.3%. Moreover, Galgravin was stable throughout storage and processing with all RSDs below 12.1%. After the successful application of this optimized method, the oral bioavailability of Galgravin was determined to be 8.5%. This study will be helpful to the future research and development of Galgravin.
Effects of veraguensin and Galgravin on osteoclast differentiation and function
Cytotechnology 2012 May;64(3):315-22.PMID:22526488DOI:10.1007/s10616-011-9416-z.
The dried flower buds of Magnolia sp. are widely used as herbal medicines because of their anti-inflammatory, anti-malarial and anti-platelet activities. Here, we found that veraguensin and Galgravin, lignan compounds derived from Magnolia sp., dose-dependently inhibited osteoclast formation in co-cultures of bone marrow cells and osteoblastic cells. These compounds also inhibited receptor activator of nuclear factor κB ligand (RANKL)-induced osteoclast differentiation in RAW264.7 cells and bone marrow macrophages. In the RANKL-induced signaling pathway, veraguensin and Galgravin reduced p38 phosphorylation and suppressed the expression of c-Fos, a key transcription factor for osteoclastogenesis. Veraguensin and Galgravin also inhibited osteoclastic pit formation, which was accompanied by decreased mature osteoclast viability. In conclusion, these results indicate that veraguensin and Galgravin can inhibit bone resorption and may offer novel compounds for the development of drugs to treat bone-destructive diseases such as osteoporosis.
O-demethylation of 7,7'-epoxylignans by Aspergillus niger
Phytochemistry 1996 Sep;43(1):111-3.PMID:8987506DOI:10.1016/0031-9422(96)00222-1.
Biotransformation of the 7,7'-epoxylignans, (+)-veraguensin, (+)-galbelgin and Galgravin by Aspergillus niger has been investigated. These lignans were converted to their corresponding 4,4'-O-demethyl derivatives, (+)-verrucosin, (+)-fragransin A2 and nectandrin B.
Neuroprotective effects of 2,5-diaryl-3,4-dimethyltetrahydrofuran neolignans
Biol Pharm Bull 2005 Feb;28(2):289-93.PMID:15684486DOI:10.1248/bpb.28.289.
We previously reported the neurotrophic effects of talaumidin (1) from Aristolochia arcuata MASTERS. In the present study, we compared the neurotrophic and neuroprotective effects of six other 2,5-diaryl-3,4-dimethyltetrahydrofuran neolignans isolated from the same plant, veraguensin (2), Galgravin (3), aristolignin (4), nectandrin A (5), isonectandrin B (6), and nectandrin B (7), with compound 1 in primary cultured rat neurons. Compounds 3-7 promoted neuronal survival and neurite outgrowth, among which compounds 6 and 7 showed neurotrophic activity comparable with that of 1. Furthermore, compounds 1-7 protected hippocampal neurons against amyloid beta peptide (Abeta25-35)-induced cytotoxicity, while compounds 1 and 4-7 protected against neuronal death from 1-methyl-4-phenylpyridinium ion (MPP+)-induced toxicity in cultured rat hippocampal neurons.
Antitumor plants. X. Constituents of Nectandra rigida
J Nat Prod 1980 May-Jun;43(3):353-9.PMID:7400821DOI:10.1021/np50009a006.
The major cytotoxic activity of crude extracts of Nectandra rigida Nees is due to dehydrodiisoeugenol,the sample isolated being slightly enriched in the dextrorotatory enantiomer. Galgravin and two new tetrahydrofuranoid lignans, nectandrin A and nectandrin B, were also isolated and characterized along with small quantities of vanillin, 2,6-dimethoxybenzoquinone, and the known lauraceous alkaloid laurelliptine. The neolignans are of potential chemotaxonomic significance in the study of the Lauraceae.