New clerodane diterpenes, 12-epi-megalocarpodolide D (2) and an epimeric mixture of crotonolins A (3) and B (4), were isolated from the bark of Croton oligandrus following a bioassay-guided isolation protocol. Known compounds, megalocarpodolide D (1), 12-epi-crotocorylifuran (5), cluytyl-ferulate (6), hexacosanoyl- ferulate (7), vanillin (8), acetyl-aleuritolic acid (9) and lupeol (10), were also isolated. The structures of the isolated compounds (1–10) were elucidated by spectroscopic means. The cytotoxicity of compounds 1–10 was assessed against A549, MCF7, PC3 and PNT2 cell lines using the MTT assay. Compounds 1 and 2 showed moderate levels of activity against both A549 and MCF7 cells with 1 being the most active with IC50 values of 63.8 ± 13.8 and 136.2 ± 22.7 µM against A549 and MCF7 cells, respectively. The epimeric mixture of 3 and 4 was moderately active against A549 and PC3 cells (IC50 = 128.6 ± 31.0 and 111.2 ± 2.9 µM, respectively).

Three new alkamides, zanthoamides G-I (1-3), together with ten known compounds, araliopsine, skimmianine, N-methylplatydesminium cation, isoplatydesmine, myrtopsine, atanine, N-methylatanine, sesamin, hesperetin and hesperidin, were isolated from the fruits of Zanthoxylum zanthoxyloides. Their structures were elucidated by spectroscopic means. All isolated compounds were assessed for their cytotoxicity against A549, MCF7, PC3 and PNT2 cell lines. Among the alkamides, only zanthoamide G (1) showed low level of cytotoxicity against MCF7 cells.

Objectives The effects of a root extract of Zanthoxylum zanthoxyloides on neuroinflammation in BV-2 microglia stimulated with LPS and hemozoin were investigated. Methods ELISA, enzyme immunoassay and Griess assay were used to evaluate levels of cytokines, PGE2 and NO in culture supernatants, respectively. Microglia-mediated neurotoxicity was evaluated using a BV-2 microglia-HT-22 neuron transwell co-culture. Key findings Treatment with Z. zanthoxyloides caused reduced elevated levels of TNFα, IL-6, IL-1β, NO and PGE2, while increasing the levels of IL-10. In addition, there were reduced levels of iNOS and COX-2 proteins. This was accompanied by a prevention of microglia-mediated damage to HT-22 mouse hippocampal neurons. Z. zanthoxyloides reduced elevated levels of phospho-IκB and phospho-p65, while preventing degradation of IκB protein and DNA binding of p65. Further mechanistic studies revealed that Z. zanthoxyloides reduced the levels of pro-IL-1β and IL-1β in hemozoin-activated BV-2 microglia. This was accompanied by a reduction in caspase-1 activity and NLRP3 protein expression. Bioassay-guided fractionation resulted in the isolation of skimmianine as an anti-inflammatory compound in Z. zanthoxyloides. Conclusion This is the first report showing the inhibition of neuroinflammation in LPS- and hemozoin-activated BV-2 microglia by the root extract of Z. zanthoxyloides by targeting the activation of both NF-κB and NLRP3 inflammasome.

Guetchueng, ST, Nahar, L, Ritchie, KJ, Ismail, FMD, Dempster, NM and Sarker, SD Justicialosides A and B, two new flavone glycosides from the leaves of Ruspolia hypocrateriformis (Vahl) Milne-Redh. (Acanthaceae) http://researchonline.ljmu.ac.uk/id/eprint/10483/ Article LJMU has developed LJMU Research Online for users to access the research output of the University more effectively. ABSTRACT Two new flavone glycosides, luteolin 7-O-α-L-rhamnopyranosyl-(1→2)-β-D-xylopyranoside (1) and chrysoeriol 7-O-α-L-rhamnopyranosyl-(1→2)-β-D-xylopyranoside (2), along with five known compounds, luteolin 7-O-β-D-apiofuranosyl-(1→2)-β-D-xylopyranoside (3), grandulosides A and B (4 and 5), luteolin 7-O-[β-D-glucopyranosyl-(1→2)-α-L-rhamnosyl-(1→6)]-β-D-glucopyranoside (6) and 10H-quindoline (7) were isolated from the leaves of Ruspolia hypocrateriformis (Acanthaceae). Their structures were elucidated by spectroscopic means, including 1D and 2D NMR, HRESIMS and by comparison with published data.

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