ABSTRACT
Chemical investigation of the whole plant of Sauropus hirsutus Beille led to the isolation of eight quinolines and two known flavonoids. Furthermore, five quinolines were new, two were reported in plant for the first time and one was known. Cytotoxicity evaluation against cholangiocarcinoma, KKU-M156, showed that the most active compound was 4-hydroxy-6-methoxy-7,8-methylenedioxyquinaldine (IC50 20.54 ± 6.82 µM) which was a little more active than the cisplatin standard (IC50 24.39 ± 1.14 µM).
Subject(s)
Alkaloids , Antineoplastic Agents, Phytogenic , Bile Duct Neoplasms , Quinolines , Humans , Antineoplastic Agents, Phytogenic/chemistry , Alkaloids/chemistry , Bile Ducts, Intrahepatic , Cell Line, TumorABSTRACT
Ten acridones isolated from Atalantia monophylla were evaluated for effects on Alzheimer's disease pathogenesis including antioxidant effects, acetylcholinesterase (AChE) inhibition, prevention of beta-amyloid (Aß) aggregation and neuroprotection. To understand the mechanism, the type of AChE inhibition was investigated in vitro and binding interactions between acridones and AChE or Aß were explored in silico. Drug-likeness and ADMET parameters were predicted in silico using SwissADME and pKCSM programs, respectively. All acridones showed favorable drug-likeness and possessed multifunctional activities targeting AChE function, Aß aggregation and oxidation. All acridones inhibited AChE in a mixed-type manner and bound AChE at both catalytic anionic and peripheral anionic sites. In silico analysis showed that acridones interfered with Aß aggregation by interacting at the central hydrophobic core, C-terminal hydrophobic region, and the key residues 41 and 42. Citrusinine II showed potent multifunctional action with the best ADMET profile and could alleviate neuronal cell damage induced by hydrogen peroxide and Aß1-42 toxicity.
ABSTRACT
Six undescribed polyketides, 1-6, were discovered from the fruits of Knema globularia (Lam.) warb. Two known polyketides and three known lignans were also isolated. Cytotoxicities against HepG2 and KKU-M156 cells of all polyketides were evaluated. Compound 1 displayed the most cytotoxic activity against HepG2 and KKU-M156 cell lines with IC50 values of 1.57 ± 0.37 and 1.78 ± 0.14 µg mL-1, respectively. The structure of all isolates was identified using spectroscopic methods including NMR, IR, MS and ECD.
ABSTRACT
Four new benzoyltyramines, atalantums H-K (1-4) and seven known compounds were isolated from the peels of Atalantia monophylla. All compounds were tested for cytotoxicity against HeLa, HCT116 and MCF-7 cell lines, as well as normal cells (Vero cells). Compound 5 showed cytotoxicity against HeLa, HCT116 and MCF-7 cell lines with IC50 values ranging from 16-25 µg/mL but was inactive against Vero cells. Compound 6 also showed interesting results as compound 5 with IC50 values ranging from 15-18 µg/mL and an IC50 value of 80.20 µg/mL against Vero cells. This means compounds 5 and 6 can be used as lead compounds for anticancer agents.
Subject(s)
Antineoplastic Agents/isolation & purification , Rutaceae/chemistry , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Cell Line , Chlorocebus aethiops , Humans , Inhibitory Concentration 50ABSTRACT
Three new limonoids, limonophyllines A-C (1, 4 and 5), along with two known limonoids (2 and 3) and 11 acridone alkaloids (6-16) were isolated from the stems of Atalantia monophylla. All isolates were evaluated against cholangiocarcinoma, KKU-M156, and HepG2 cancer cell lines. Compounds 12, 14 and 16 displayed cytotoxicity against KKU-M156 cell line with IC50 ranging from 3.39 to 4.1 µg/mL while cytotoxicity against HepG2 cell line with IC50 ranging from 1.43 to 8.4 µg/mL. The structures of all isolated compounds were established by spectroscopic methods including 1D and 2D NMR, IR and mass spectrometry.
