Prospects of targeting JAK/STAT signal transduction pathways for vasculitis.

Vasculitis is the inflammation of blood vessels caused by autoimmunity and/or autoinflammation, and its etiology and pathogenesis remain largely unknown. The Janus kinase (JAK) and Signal transduction Transcription Activator (STAT) signal transduction pathways are a group of molecules involved in the major pathways by which many cytokines exert and integrate their functions, and their dysregulation has been implicated in the pathogenesis of a variety of autoimmune diseases. However, current data supporting the role of the JAK/STAT pathway in the development of vasculitis is limited. In terms of treatment, glucocorticoids and immunosuppressants have been the standard therapy. However, because of the huge burden of treatment side effects, people have long waited for new treatment options. JAK inhibitors reduce the production of multiple cytokines and inhibit inflammation by targeting the JAK/STAT pathway, and have the advantage of rapidly acting in oral formulations, reducing glucocorticoid dependence and associated adverse events, especially in refractory cases. Therefore, JAK inhibitors are expected to be a promising drug for the treatment of vasculitis.

Triterpenoid prosapogenols and prosapogenins from the husks of Xanthoceras sorbifolia.

Two new prosapogenins, 16-O-acetyl-21-O-(4-angeloyl)-alpha-l-rhamnopyranosyl barringtogenol C (1), 28-O-beta-d-glucopyranosyl 16-deoxybarringtogenol C (2), were isolated from the acid hydrolyzate of the crude saponin obtained from the husks of Xanthoceras sorbifolia Bunge, along with six known triterpenoids. These structures were established on the basis of chemical and detailed spectral evidences. Compounds 1 and 2 showed cytotoxic activity against human cell lines (A375-S2, HeLa).

Two new triterpenoids from the carpophore of Xanthoceras sorbifolia Bunge.

Two new triterpenoids were isolated from the dried carpophore of Xanthoceras sorbifolia Bunge (Sapindaceae). By means of spectroscopic data (1D and 2D NMR, ESI-MS) and chemical evidence, their structures were established as 16-O-acetyl-21-O-(3',4'-di-O-angeloyl)-beta-D-fucopyranosyl theasapogenol B (1) and 3beta,23-dihyroxy-lup-20(29)en-28-oic acid -23-caffeate (2).

Thiophenes from Echinops latifolius.

Six thiophenes were isolated and purified from ethanol extract of the roots of Echinops latifolius Tausch. Their structures were identified on the basis of spectral data. Among them, 5-(3-hydroxmethyl-3-isovaleroyloxyprop-1-ynyl)-2,2'-bithiophene (6) is a new compound, and 5-(3-hydroxy-4-isovaleroyloxybut-1-ynyl)-2,2'-bithiophene (5) was isolated from this plant for the first time.

A new sesquiterpene ester inhibiting no production from the fruits of Celastrus orbiculatus.

A new beta-dihydroagarofuran sesquiterpene ester, 1beta,2beta,6alpha, 13-tetraacetoxy-9alpha-cinnamoyloxy-beta-dihydroagarofuran (1), and the known compound 1beta,6alpha,13-triacetoxy-9alpha-benzoyloxy-beta-dihydroagarofuran (2), have been isolated from the fruits of Celastrus orbiculatus Thunb. Their structures have been elucidated on the basis of spectroscopic methods. Compound 1 shows moderate activity of inhibiting LPS-induced nitric oxide production in murine macrophage RAW264.7 cells, with an IC50 of 55.4 microM.

A new perylenequinone from the fruit bodies of Bulgaria inquinans.

A new perylenequinone, 4,9-dihydroxy-1,2,11,12-tetrahydroperylene-3,10-quinone (1), together with three known compounds, have been isolated from the ethanolic extract of the fruit bodies of Bulgaria inquinans, and their structures elucidated on the basis of the spectral data and comparison with the literature.