Aglafoline (Aglafolin)
(Synonyms: Aglafolin; Rocaglamide U; (-)-Methyl rocaglate) 目录号 : GC32462Aglafoline (Aglafolin) 以选择性和浓度依赖性方式抑制 PAF(血小板激活因子)在洗涤过的兔血小板中诱导的聚集和 ATP 释放反应。
Cas No.:143901-35-3
Sample solution is provided at 25 µL, 10mM.
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- Purity: >98.50%
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Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor). The IC50 values of Aglafoline on PAF (3.6 nM)-induced platelet aggregation were about 50 μM.ic50 value: 50 μMTarget: PAFin vitro: Aglafoline also inhibits [3H]PAF (3.6 nM) binding to washed rabbit platelets with an IC50 value of 17.8 ± 2.6 μM. The concentration-response curve of PAF-induced platelet aggregation was shifted to the right by Aglafoline with pA2 and pA10 values of 5.97 and 5.04, respectively. Although thromboxane B2 formation caused by collagen and thrombin was partially suppressed by Aglafoline, thromboxane B2 formation caused by ionophore A23187 and arachidonic acid was not affected. Aglafoline inhibited the [3H]inositol monophosphate formation caused by PAF but not that caused by collagen or thrombin in the presence of indomethacin (20 μM). [1]in vivo: The cAMP content of washed rabbit platelets was not affected by Aglafoline. Rat femoral intravenous administration of Aglafoline (10 mg/kg) did not affect blood pressure. However, Aglafoline (10 mg/kg) both prophylactically and therapeutically antagonized PAF (2.5 μg/kg)-induced hypotensive shock in rats. Intravenous PAF (30 ng/kg) caused severe bronchoconstriction in guinea pigs. This effect was completely blocked by Aglafoline. This implies Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo.[1]
[1]. Ko FN, et al. PAF antagonism in vitro and in vivo by aglafoline from Aglaia elliptifolia Merr. Eur J Pharmacol. 1992 Jul 21;218(1):129-35.
Cas No. | 143901-35-3 | SDF | |
别名 | Aglafolin; Rocaglamide U; (-)-Methyl rocaglate | ||
Canonical SMILES | O=C([C@H]([C@H]1C2=CC=CC=C2)[C@@H](O)[C@]3(O)[C@@]1(C4=CC=C(OC)C=C4)OC5=CC(OC)=CC(OC)=C35)OC | ||
分子式 | C28H28O8 | 分子量 | 492.52 |
溶解度 | Ethanol : 100 mg/mL (203.04 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.0304 mL | 10.1519 mL | 20.3037 mL |
5 mM | 0.4061 mL | 2.0304 mL | 4.0607 mL |
10 mM | 0.203 mL | 1.0152 mL | 2.0304 mL |
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Activity of selected phytochemicals against Plasmodium falciparum
Acta Trop 2012 Aug;123(2):96-100.PMID:22537982DOI:10.1016/j.actatropica.2012.04.002.
According to the WHO, in 2008, there were 247 million reported cases of malaria and nearly one million deaths from the disease. Parasite resistance against first-line drugs, including artemisinin and mefloquine, is increasing. In this study the plant-derived compounds Aglafolin, rocaglamid, kokusaginine, arborine, arborinine and tuberostemonine were investigated for their anti-plasmodial activity in vitro. Fresh Plasmodium falciparum isolates were taken from patients in the area of Mae Sot, north-western Thailand in 2008 and the inhibition of schizont maturation was determined for the respective compounds. With inhibitory concentrations effecting 50%, 90% and 99% inhibition (IC(50), IC(90) and IC(99)) of 60.95 nM, 854.41 nM and 7351.49 nM, respectively, rocaglamid was the most active of the substances, closely followed by Aglafoline with 53.49 nM, 864.55 nM and 8354.20 nM. The activity was significantly below that of artemisinin, but moderately higher than that of quinine. Arborine, arborinine, tuberostemonine and kokusaginine showed only marginal activity against P. falciparum characterized by IC(50) and IC(99) values higher than 350 nM and 180 μM, respectively, and regressions with relatively shallow slopes S>14.38. Analogues of rocaglamid and Aglafoline merit further exploration of their anti-plasmodial activity.
Cytotoxic and antiplatelet aggregation principles from Aglaia elliptifolia
J Nat Prod 1997 Jun;60(6):606-8.PMID:9214732DOI:10.1021/np970163+.
Two related 1H-2,3,3a,8b-tetrahydrocyclopenta[b]benzofurans, Aglafolin (1a) and rocaglamide (2), isolated from the stems of Aglaia elliptifolia, showed significant cytotoxicity in six cancer cell lines. Aglafolin (1a) was also found to completely block platelet aggregation caused by arachidonic acid and platelet-activating factor at 100 microM and 2 ng/mL, respectively.