Covering: 1998 to July 2010 Since 1998, a great number of bufadienolides have been reported from plants, animals and plant cell suspensions, as well as from fungi and bacteria cultures. This review summarizes both new bufadienolides and those obtained from new sources, together with data regarding the antitumor activity of bufadienolide derivatives.

Hirudo (Shuizhi in Chinese) is an important Chinese medicine, which possesses many therapeutic properties for the treatment of the cerebral hemorrhage and other thrombosis‐related diseases. The phytochemical investigation gave more than 51 compounds including pteridines, phosphatidylcholines, glycosphingolipids, and sterols, as well as some bioactive peptides from the Shuizhi derived from three animal species recorded in the current Chinese Pharmacopoeia. The pharmacological studies on the Shuizhi have revealed various activities such as anticoagulation, antithrombosis, antiatherosclerosis, antiplatelet aggregation, antitumor and anti‐inflammatory as well as hemorheology improvement, and protective effects against cerebral ischemia‐reperfusion injury. However, some important issues based on the traditional uses of Shuizhi are still not clear. The aim of the present review is to provide comprehensive knowledge on the ethnopharmacology, phytochemistry, and pharmacological activities of Shuizhi. It will provide a potential guidance in exploring main active compounds of Shuizhi and interpreting the action mechanism for the further research.

Hyperuricemia (HUA) is a kind of metabolic disease with high incidence that still needs new countermeasures. Apigenin has uric-lowering and kidney-protective activities, but how apigenin attenuates HUA and renal injury remains largely unexploited. To this end, an acute HUA mouse model was established by intraperitoneal injection of potassium oxazinate and oral administration with hypoxanthine for 7 consecutive days. Apigenin intervention decreased serum uric acid (UA), creatinine (CRE), blood urea nitrogen (BUN), interleukin-1β (IL-1β), interleukin-6 (IL-6), tumor necrosis factor (TNF-α), interleukin-18 (IL-18), liver xanthine oxidase (XOD), and urine protein levels, and increased serum interleukin-10 (IL-10) and urine UA and CRE levels in HUA mice. Moreover, administration of apigenin to HUA mice prevented renal injury, decreased renal glucose transporter 9 (GLUT9) and urate anion transporter 1 (URAT1) levels, and increased renal organic anion transporter 1 (OAT1). These alterations were associated with an inhibition of IL-6, phospho-janus kinase 2 (P-JAK2), phospho-signal transducer, and activator of transcription 3 (P-STAT3), and suppression of cytokine signaling 3 (SOCS3) expression in the kidneys. Additionally, the molecular docking results showed that apigenin had strong binding capacity with UA transporters and JAK2 proteins. In summary, apigenin could improve UA metabolism and attenuate renal injury through inhibiting UA production, promoting excretion, and suppressing the JAK2/STAT3 signaling pathway in HUA mice. The results suggest that apigenin may be a suitable drug candidate for management of HUA and its associated renal injury.

Lonicera japonica flos is widely used as a pharmaceutical resource and a commonly-employed ingredient in healthy food, soft beverages and cosmetics in China. Sometimes, sulfur fumigation is used during post-harvest handling. In this study, a comprehensive comparison of the chemical profile between sun-dried and sulfur-fumigated samples was conducted by HPLC fingerprints and simultaneous quantification of nine constituents, including secologanic acid, along with another eight usually-analyzed markers. Secologanic acid was destroyed, and its sulfonates were generated, whereas caffeoylquinic acids were protected from being oxidized. The residual sulfur dioxide in sulfur-fumigated samples was significantly higher than that in sun-dried samples, which might increase the potential incidence of toxicity to humans. Meanwhile, compared with sun-dried samples, sulfur-fumigated samples have significantly stronger antioxidant activity, which could be attributed to the joint effect of protected phenolic acids and flavonoids, as well as newly-generated iridoid sulfonates.

The qualitative and quantitative analyses by HPLC and LC-DAD-MS/MS were conducted for the quality consistency evaluation of Compound Kushen Injection (CKI). For fingerprint analysis, 8 peaks were selected as the characteristic peaks in the HPLC chromatograms of 27 different batches of CKI samples and their similarities were more than 0.90, except the four samples. For the typical HPLC profile, peak identification was carried out by HPLC and LC-MS/MS analyses and as a result, 21 chromatographic peaks were identified or characterized based on the comparison of retention time and UV spectra with authentic compounds as well as by summarized MS fragmentation rules. Six of these identified compounds, including oxymatrine, oxysophocarpine, N-methylcytisine, matrine, sophocarpine, and trifolirhizin, were simultaneously determined and the results showed that the total amounts of six marker compounds were variable, to some extent, which was deduced to be related to the quality of the crude materials and the manufacturing process employed. Supplemental materials are available for this article. Go to the publisher's online edition of the Journal of Liquid Chromatography & Related Technologies to view the supplemental file.