Reparative and toxicity-reducing effects of liposome-encapsulated saikosaponin in mice with liver fibrosis

Saikosaponin d (SSd), a primary active component of the Chinese herb Bupleurum falcatum, has antitumor and antiliver fibrosis effects. However, the toxicity of SSd at high doses can induce conditions such as metabolic disorders and hemolysis in vivo, thus hampering its clinical use. The present study investigated the toxicity-reducing effects of liposome encapsulation of pure SSd and the therapeutic action of SSd-loaded liposomes (Lipo-SSd) in liver fibrosis in vitro and in vivo. Lipo-SSd (diameter, 31.7 ± 7.8 nm) was prepared at an entrapment efficiency of 94.1%. After 10-day incubation, a slow release profile of 56% SSd from Lipo-SSd was observed. The IC50 of SSd on hepatic stellate cells was approximately 2.9 μM. Lipo-SSd exhibited much lower cytotoxicity than did pure SSd. In the in vivo toxicity assay, Lipo-SSd significantly increased mice survival rate and duration compared with pure SSd at the same dose. These in vitro and in vivo data indicate that liposomal encapsulation can reduce the cytotoxicity of SSd. The histopathological analysis results demonstrated that in mice with thioacetamide-induced liver fibrosis, Lipo-SSd exerted more obvious fibrosis- and inflammation-alleviating and liver tissue-reparative effects than did pure SSd; these effects are potentially attributable to the sustained release of SSd. In conclusion, Lipo-SSd fabricated here have antiliver fibrosis effects and lower toxicity compared with that of pure SSd.

Differential Effects of Saikosaponins A, B2, B4, C and D on Alcohol and Chocolate Self-Administration in Rats

Aims Treatment with saikosaponin A (SSA)—an ingredient of the medicinal herb, Bupleurum falcatum—has been reported to suppress several addictive-like behaviors, including morphine, cocaine, alcohol and chocolate self-administration in male rats. The aim of this investigation was to investigate whether saikosaponins of B. falcatum other than SSA affect alcohol and chocolate self-administration in rats. Methods Ovariectomized female Sardinian alcohol-preferring (sP) and Wistar rats were trained to self-administer alcohol (15%, v/v) and a chocolate solution [5% (w/v) Nesquik® in water], respectively, under fixed ratio schedules of reinforcement. The following saikosaponins were compared to SSA: saikosaponin D (SSD; epimer of SSA), saikosaponin C (SSC), saikosaponin B2 (SSB2) and saikosaponin B4 (SSB4). All saikosaponins were tested acutely at the doses of 0, 0.25, 0.5 and 1 mg/kg (i.p.). Results Treatment with SSA and SSD resulted in highly similar, marked reductions in alcohol self-administration; SSC failed to alter lever-responding for alcohol, while SSB2 and SSB4 produced intermediate reductions. Only SSA and SSD reduced chocolate self-administration, with SSC, SSB2 and SSB4 being ineffective. Conclusions The wide spectrum of efficacy of saikosaponins in reducing alcohol and chocolate self-administration suggests that even relatively small structural differences are sufficient to produce remarkable changes in their in vivo pharmacological profile. Together, these results confirm that roots of B. falcatum may be an interesting source of compounds with anti-addictive potential.

Vegetation characteristics of the Gubinsko-Troekurovskie Heights (Samara Region)

In the flora of Gubinsko-Troekurovskie heights (Samara Region) the authors identified 467 species of vascular plants, including 26 rare species: Adonanthe vernalis , Astragalus zingeri , Bupleurum falcatum , Catabrosella humilis , Clausia aprica , Cotoneaster laxiflorus , Crataegus volgensis , Ephedra distachya , Ferula caspica , Fritillaria ruthenica , Galatella angustissima , Gentiana cruciata , Hedysarum grandifolium , Iris aphylla , Iris pseudacorus , Iris pumila , Jurinea ledebourii , Jurinea multiflora , Koeleria sclerophylla , Linum perenne , Polygala sibirica , Pulsatilla patens , Scabiosa isetensis , Stipa korshinskyi , Stipa pennata , Thymus zheguliensis . Bunchgrass real steppes with the domination of Stipa capillata and Cleistogenes squarrosa develop on flatter areas. Bunchgrass real steppes with domination of Stipa pennata , Stipa lessingiana and Helictotrichon desertorum are also formed on the gentle slopes (angle less than 30). Calciphyte legumes real steppes with domination of Astragalus tenuifolius , mixed grass real steppes ( Potentilla glaucescens , Centaurea carbonata ) and semi-shrubs real steppe ( Ephedra distachya , Onosma volgensis , Thymus zheguliensis ) develop on steep slopes (angle more than 30). Strong erosion steep slopes often contribute to the preservation and maintenance of the populations of many rare species for the Samara Region.