3804-70-4Relevant articles and documents
Angelmarin, a novel anti-cancer agent able to eliminate the tolerance of cancer cells to nutrient starvation
Awale, Suresh,Nakashima, Eduardo M.N.,Kalauni, Surya K.,Tezuka, Yasuhiro,Kurashima, Yukiko,Lu, Jie,Esumi, Hiroyasu,Kadota, Shigetoshi
, p. 581 - 583 (2006)
The CH2Cl2-soluble extract of Angelica pubescens was found to kill PANC-1 cancer cells preferentially under nutrition starvation at a concentration of 50 μg/ml, with virtually no cytotoxicity under nutrient-rich conditions. Further bioassay-guided fractionation and isolation led to the isolation of a novel compound named angelmarin as the primary compound responsible for the preferential cytotoxicity; the compound exhibited 100% preferential cytotoxicity against PANC-1 cells at a concentration of 0.01 μg/ml.
Design, synthesis and biological evaluation of novel osthole-based derivatives as potential neuroprotective agents
Zhang, Li,Wu, Yuhang,Yang, Guixiang,Gan, Haixian,Sang, Dayong,Zhou, Jiye,Su, Lin,Wang, Rui,Ma, Lei
, (2020/11/03)
A total of 26 compounds based on osthole skeleton were designed, synthesized. Their cytoprotective abilities of antioxidation, anti-inflammation and Aβ42(Amyloid β-protein 42)-induced neurotoxicity were evaluated by MTT assays. Mechanism of the action of selected compounds were investigated by molecular docking. AlogP, logS and blood–brain barrier (BBB) permeability of all these compounds were simulated by admetSAR. Most of the compounds showed better antioxidative and anti-inflammatory activities compared with osthole, especially OST7 and OST17. The compound OST7 showed relative high activity in neuroprotection against H2O2 (45.7 ± 5.5%), oxygen glucose deprivation (64.6 ± 4.8%) and Aβ42 (61.4 ± 5.2%) at a low concentration of 10 μM. EC50 of selected compounds were measured in both H2O2 and OGD induced cytotoxicity models. Moreover, NO inhibiting ability of OST17(50.4 ± 7.1%) already surpassed the positive drug indomethacin. The structure activity relationship study indicated that introduction of piperazine group, tetrahydropyrrole group and aromatic amine group might be beneficial for enhancement of osthole neuroprotective properties. Molecular docking explained that the reason OST7 exhibited relatively stronger neuroprotection against Aβ because of the greater area of interactions between molecule and target protein. OST7 and OST17 both provided novel methods to investigate osthole as anti-AD drugs.
Accessing columbianetin-containing natural products via a domino on-water, in-water process
Beare, Kaitlin D.,McErlean, Christopher S.P.
supporting information, p. 1056 - 1058 (2013/04/10)
A domino on-water, in-water process has been developed for the rapid and efficient synthesis of (±)-columbianetin. This highlights the operational simplicity of on-water chemistry. The domino process forms the key step in the synthesis of the columbianetin-containing natural products (±)- columbianetin acetate, (±)-zosimin, (±)-libanorin and (±)-angelmarin.
Protecting group free syntheses of (±)-columbianetin and (±)-angelmarin
Harris, Eric B.J.,Banwell, Martin G.,Willis, Anthony C.
, p. 6887 - 6889 (2012/02/05)
A five-step and protecting group free synthesis of (±)-columbianetin from cyclohexane-1,3-dione is reported. The former compound was converted into its p-hydroxycinnamate derivative, (±)-angelmarin, using Coster's esterification procedure. Efforts to modi
