Optimization of supercritical CO2 extraction for sauchinone and in vitro antitumor activity of Saururi Herba supercritical extract / 中成药

AIM To optimize the supercritical CO2 extraction of sauchinone and to evaluate the in vitro antitumor activity of Saururi Herba supercritical extract.METHODS With extraction pressure,extraction temperature,extraction time,entrainer (ethanol) concentration and entrainer amount as influencing factors,together with extraction rate of sauchinone as an evaluation index,orthogonal test was used for optimizing the extraction.Then MTT was applied to determining the extract's inhibitory effect on human multidrug-resistant hepatocellular carcinoma cell line (7721/Adm).RESULTS The optimal conditions were determined to be 30 MPa for extraction pressure,50 ℃ for extraction temperature,2 h for extraction time,95％ for ethanol concentration,and one time for ethanol amount,the average extraction rate of sauchinone was 0.173％.The obtained extract significantly inhibited the proliferation of 7721/Adm cells (IC50 =50.08 μg/mL),demonstrating a stronger activity than that of ethanol extract (ICs0 =150.59 μg/mL).CONCLUSION This stable and feasible method is appropriate for sauchinone extraction,and the supercritical CO2 extract from Saururi Herba shows a strong in vitro antitumor activity.

The Therapeutic Effect of Sauchinone on Inflammatory Arthritis in Mice

OBJECTIVE: Rheumatoid arthritis (RA) is a chronic inflammatory disease, mainly involving joints and bones. Sauchinone is an anti-inflammatory agent isolated from Saururus chinensis, which was used in oriental medicine. The aim of this study was to evaluate the therapeutic effect of sauchinone on inflammatory arthritis and underlying mechanism of anti-arthritic effect. METHODS: Mice with collagen induced arthritis (CIA) was intraperitoneally injected with sauchinone (20 mg/kg) or vehicle. The clinical and histological evaluations were performed with arthritis scoring and hematoxylin-eosin staining, respectively. CD4+ interleukin (IL) 17+ T cells were determined under Th17 skewing condition treated with sauchinone. To evaluate the effect of sauchinone on osteoclastogenesis, mice bone marrow macrophages (BMMs) and human peripheral blood mononuclear cells (PBMCs) were cultured with macrophage-colony stimulating factor and receptor activator of nuclear factor-κB ligand in the absence or presence of sauchinone. RESULTS: Sauchinone significantly attenuated the inflammatory arthritis in CIA mice both clinically and histologically. The proportion of Th17 cells were decreased with treatment with sauchinone in vivo and in vitro. The expressions of Th17 cell markers (IL-17 and retinoic acid receptor-related orphan receptor gamma t) and B cell markers (activation-induced cytidine deaminase) were downregulated in the presence of sauchinone. Sauchinone also suppressed the formation of tartrate-resistant acid phosphatase positive cells from mice BMMs and human PBMCs, and the expression of osteoclastogenic markers. CONCLUSION: Sauchinone alleviates inflammatory arthritis in mice through inhibition of Th17 differentiation and osteoclastogenesis. Sauchinone, one of traditional herbal medicine, could be a therapeutic candidate for the treatment of RA.

Natural Products for Chemoprevention of Breast Cancer

Breast cancer is the primary cause of cancer death in women. Although current therapies have shown some promise against breast cancer, there is still no effective cure for the majority of patients in the advanced stages of breast cancer. Development of effective agents to slow, reduce, or reverse the incidence of breast cancer in high-risk women is necessary. Chemoprevention of breast cancer by natural products is advantageous, as these compounds have few side effects and low toxicity compared to synthetic compounds. In the present review, we summarize natural products which exert chemopreventive activities against breast cancer, such as curcumin, sauchinone, lycopene, denbinobin, genipin, capsaicin, and ursolic acid. This review examines the current knowledge about natural compounds and their mechanisms that underlie breast cancer chemopreventive activity both in vitro and in vivo. The present review may provide information on the use of these compounds for the prevention of breast cancer.

Protective Effect of Sauchinone Against Regional Myocardial Ischemia/Reperfusion Injury: Inhibition of p38 MAPK and JNK Death Signaling Pathways

Sauchinone has been known to have anti-inflammatory and antioxidant effects. We determined whether sauchinone is beneficial in regional myocardial ischemia/reperfusion (I/R) injury. Rats were subjected to 20 min occlusion of the left anterior descending coronary artery, followed by 2 hr reperfusion. Sauchinone (10 mg/kg) was administered intraperitoneally 30 min before the onset of ischemia. The infarct size was measured 2 hr after resuming the perfusion. The expression of cell death kinases (p38 and JNK) and reperfusion injury salvage kinases (phosphatidylinositol-3-OH kinases-Akt, extra-cellular signal-regulated kinases [ERK1/2])/glycogen synthase kinase (GSK)-3beta was determined 5 min after resuming the perfusion. Sauchinone significantly reduced the infarct size (29.0% +/- 5.3% in the sauchinone group vs 44.4% +/- 6.1% in the control, P < 0.05). Accordingly, the phosphorylation of JNK and p38 was significantly attenuated, while that of ERK1/2, Akt and GSK-3beta was not affected. It is suggested that sauchinone protects against regional myocardial I/R injury through inhibition of phosphorylation of p38 and JNK death signaling pathways.