Tissue Distribution, Excretion, and Interaction With Human Serum Albumin of Total Bioflavonoid Extract From Selaginella doederleinii.

Selaginella doederleinii Hieron is a traditional Chinese medicinal herb widely used to treat different cancers. Previously, we showed that the total bioflavonoid extract of S. doederleinii (TBESD) exhibits anti-carcinogenic activities both in vitro and in vivo. However, the plasma protein binding and pharmacokinetics parameters of TBESD remain unclear. To investigate plasma protein binding, tissue distribution, and excretion of TBESD, rats were administered a single dose of TBESD (600 mg/kg) intragastrically and tissue distribution and excretion of TBESD components were determined by rapid high-performance liquid chromatography and tandem mass spectrometry. TBESD binding to human serum albumin (HSA) was assessed by fluorescence spectroscopy. TBESD components amentoflavone, delicaflavone, robustaflavone, 2″,3″-dihydro-3',3‴-biapigenin, and 3',3‴-binaringenin were rapidly absorbed and distributed in various tissues, mostly in the lungs, kidneys, and ovaries, without long-term accumulation. The excretion of bioflavonoids occurred mostly via the intestinal tract and constituted 30% of the administered dose up to 48 h. Spectral analysis indicated that TBESD had a dynamic quenching effect on HSA by binding to one HSA site through hydrophobic interactions and hydrogen bond formation. This is the first comprehensive report on the tissue distribution, excretion, and plasma protein binding of TBESD. This study provides important information on TBESD pharmacokinetics necessary for its further development into a therapeutic form for clinical applications.

Curcumin analog L3 alleviates diabetic atherosclerosis by multiple effects.

L3, an analog of curcumin, is a compound isolated from a traditional Chinese medicine Turmeric. In this paper, we aims to explore the efficacy of L3 on diabetic atherosclerosis and the related mechanism. The effect of L3 was studied on glucose and lipid metabolism, antioxidant status, atherosclerosis-related indexes and pathological changes of main organs in the mice model of diabetes induced by streptozotocin and high-fat diet. The results showed that L3 treatment could meliorate dyslipidemia and hyperglycemia, reduce oxidative stress, enhance the activity of antioxidases, increase the nitric oxide level in plasma and aortic arch, decrease the production of reactive oxygen species in pancreas and lectin-like oxidized low-density lipoprotein receptor-1 expression in aortic arch, and meliorate the fatty and atherosclerotic degeneration in aortic arch, thereby preventing the development of diabetes and its complications. These results suggested that L3 can alleviate the diabetic atherosclerosis by multiple effects. This study provided scientific basis for the further research and clinical application of L3.

Anti-proliferation and anti-angiogenesis of curcumin-K30 solid dispersion.

OBJECTIVE: To evaluate the anti-proliferation and anti-angiogenesis effect of curcumin-K30 solid dispersion (Cur-K30) on tumors in vivo. METHODS: Growth inhibition rates of the tumor cells was measured with MTT method. Tumor inhibition was detected by tumors transplanted subcutaneously in mice treated with Cur-K30 [50, 100, and 200 mg/(kg · d)]. The expressions of CD34 and vascular endothelial growth factor (VEGF) were assessed by immunohistochemical study, and analyzed by Imageproplus software. RESULTS: Cur-K30 had inhibitory effect on different tumor cell lines in a dose dependent manner with IC50 values from 6.6 to 12.12 µg/mL. The in vivo study showed that the inhibitory rates of the 200 mg/(kg · d) Cur-K30 group on H22, B16, and SW480 were 43.2%, 53.1%, and 59.8%, respectively, which were all much higher than the inhibitory rates of curcumin suspension group with the same dose. Compared with the control group, the expression of CD34 and VEGF in SW480 tumors was down-regulated in the 200 mg/(kg · d) Cur-K30 group (P <0.01). CONCLUSION: The proliferation inhibition of Cur-K30 is higher than curcumin in vivo, and the most significant effect is obtained in SW480 tumors transplanted subcutaneously in nude mice. Down-regulation of VEGF and decreased microvascular density may contribute to the anti-tumor effect of Cur-K30.