Three compounds with diuretic potential were identified from the 95% ethanol extract of Pyrrosia petiolosa (Christ) Ching. Among them, one was a new benzanilide named petiolide A (1), and the other two were phenolic derivatives barbatic acid (2) and kaempferol (3). Their structures were elucidated based on extensive spectral analyses and comparison with the literature data. The docking experiments of all compounds into the active site of the With-No-Lysine kinase 1 (WNK1) domain demonstrated that kaempferol (3) was the most effective component with diuretic potential for its comparative diuretic effect to that of an orally bioavailable WNK inhibitor WNK463 (docking score −10.99 vs −11.09).
Five 3-formyl-2-arylbenzofuran derivatives, including three new compounds (1-3) and two known analogues (4-5), were identified from the 95% EtOH extract of Itea yunnanensis. Extensive spectroscopic analyses were performed for the structure elucidation of all new benzofurans, and single-crystal X-ray diffraction analyses were further employed for the structure verification of iteafuranals C (1) and D (2). In MTT assay, iteafuranal E (3) and iteafuranal A (4) displayed significant growth inhibition effect on SK-Hep-1 cells with IC50 values of 5.365 μM and 6.013 μM, respectively. The colony formation assay of 3 and 4 further confirmed their remarkable inhibitory effect on cell growth. Preliminary mechanism study demonstrated that 3 remarkably down-regulated the phosphorylation level of ERK, which suggested 3 could inhibit cell growth and induce apoptosis of SK-Hep-1 cells by blocking RAS/RAF/MEK/ERK signaling pathway. This study highlighted the potential of 3-fomyl-2-benzofuran derivatives as novel lead compounds to treat Hepatocellular carcinoma. Graphical Abstract
A new sesquiterpene, 1-carbonyl-2,8-dihydroxy-11-oxabicyclo [4,4,1] germacra- 2(3),4(5),6(7),8(9)-tetraene (1) and four known compounds (3E, 23E)-3-caffeoyl-23-coumaroylhederagenin (2), (3E, 23E)-dicoumaroylhederagenin (3), morettinone (4), 24-ehylcholesta-3,6-dione (5) were isolated from the ethyl acetate layer of the fibrous root of Alangium chinense (Lour.) Harms. The structure of compound 1 was characterized by its 1H-NMR, 13C-NMR, DEPT, HMBC, HSQC spectrums, and the structures of the known compounds were determined by comparison of their spectroscopic data with those reported by the literatures. The obtained compounds were evaluated for their anti-inflammatory against cyclooxygenase (COX-2). Compound 1 has a good inhibitory effect against COX-2 with IC50 20.43 ± 4.72 μM. The compounds 2–5 have inhibitory effect against COX-2 with IC50 49.19 ± 0.76, 23.29 ± 0.99, 47.78 ± 1.33, and 44.44 ± 0.12 μM, respectively. Graphical Abstract
21 January 2020 in Zeitschrift für Kristallographie - New Crystal Structures