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Jatrogricaine A (1), a new diterpenoid possessing a 5/6/6/4 carbon ring system, together with eight known diterpenoids (2-9) were isolated from the stems of Jatropha podagrica. Their structures were elucidated by extensive spectroscopic methods and the absolute configuration of 1 was determined by single crystal X-ray diffraction analysis. All compounds were evaluated for their anti-inflammatory activities in vitro, and compound 3 showed significant inhibitory effects against nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW264.7 macrophage cells with an IC50 of 13.44 ± 0.28 μmol·L-1, being comparable to the positive control, quercetin (IC50 17.00 ± 2.10 μmol·L-1).

Six new cassaine diterpenoids (1, 3–7), along with three known ones (2, 8–9) were isolated from the seeds of Erythrophleum fordii. Their structures were elucidated by extensive spectroscopic methods and acid hydrolysis. Compound 2 was tested to be the most potent one and showed more sensitive activities on MCF-7 and A549 cancer cells with IC50 values of 3.66 ± 1.20 and 2.87 ± 0.46 μM, respectively. Furthermore, compound 2 reduced the number of cell colonies significantly in a dose-dependent manner in the colony formation assay and triggered apoptosis of MCF-7 cell.

Objective To compare the clinical efficacy difference between comprehensive ying needling therapy and intramuscular injection with ribavirin for mumps. Methods One hundred patients with mumps were randomly divided into comprehensive ying needling therapy group (group A, 52 cases) and western medicine group (group B, 48 cases), then 8 cases were eliminated and drop out from group A and 4 cases were eliminated and drop out from group B respectively, actual inclusion 44 cases in group A 44 cases in group B. Point bloodletting was performed at parotid gland (腮腺Sāixian) and Threeshang acupoints of the patients in group A for once every other day, treatment for 7 days was considered as 1 course of treatment, and 2 courses were needed. Intramuscular injection with ribavirin was given to the patients in group B for twice a day, treatment for 7 days was considered as 1 course, and 2 courses were needed. The parotid gland swelling score, fever score, orifice parotid duct swelling score, score of difficulty in opening mouth and the clinical efficacy of the patients in the two groups were compared before and after treatment. Results The cured and markedly effective rate in group A was 90.9% (40/44), which was superior to 68.2% in group B (30/44) (P Conclusion The curative effect of comprehensive ying needling therapy for treatment of mumps was superior to that of conventional western medicine therapy.

Objective To compare the clinical efficacy between electroacupuncture combined with heat-sensitive moxibustion and western medicine for treatment of premature ovarian failure. Methods Eighty patients were randomly divided into an electroacupuncture combined with heat-sensitive moxibustion group (group A, n=40) and a western medicine group (group B, n=40). Zigōng ( EX-CA 1), Xuehâi ( SP 10), Gānshū ( BL 18) and Shenshū ( BL 23) were selected in group A, and acupuncture combined with heat-sensitive moxibustion were carried out. Climen was taken orally in group B. The score changes of menstrual cycle, tidal fever and sweatiness, emotional excitement, soreness and weakness of waist and knees, dizziness and tinnitus, as well as the cured and markedly effective rate of the patients in the two groups before and after two courses of treatment were compared. Results The cured and markedly effective rate of group A was 72.5% (29/40), which was superior to that of group B (37.5%, 15/40) (P Conclusion The efficacy of electroacupuncture combined with heat-sensitive moxibustion is superior to that of conventional western medicine in treatment of premature ovarian failure.

In the present study, two new diterpenoid lactones, 3-deoxy-andrographoside (1) and 14-deoxy-15-methoxy-andrographolide (2), were isolated from the aerial parts of Andrographis paniculata. Their structures were elucidated by combination of NMR, MS, and chemical methods. The configurations of 1 and 2 were established based on the analysis of ROESY data and single crystal X-ray diffraction experiment.

Two novel monoterpenoid indole alkaloids (MIAs), gelsechizines A-B (1-2), along with four known ones (3-6) were isolated from the fruits of Gelsemium elegans. Compound 1 features a new carbon skeleton with two additional carbon atoms forming a 4-methylpyridine unit. Their structures with absolute configurations were elucidated by NMR, MS, X-ray diffraction and electronic circular dichroism (ECD) calculations. Compounds 1-3 showed significant anti-inflammatory effects in vivo and in vitro, which may be related to the inhibition of the trecruitment of neutrophils and macrophages as well as the secretion of TNF-α and IL-6. Preliminary structure-activity relationship analysis revealed that the β-N-acrylate moiety plays an important role in the anti-inflammatory effect.

A novel polyvinylidene fluoride (PVDF) membrane, i.e. Ag/TiO 2 /PVDF composite membrane, was prepared via the blending/photo reduction combined method in this paper. And the influence of Ag/TiO 2 embedment on the surface property of PVDF membrane was discussed, including the surface hydrophilicity and visible-light response activity. ATR/FTIR characterization certified that amount of hydroxyl group ( OH) was formed on the PVDF membrane surface owing to the embedment of Ag/TiO 2. The results suggested that the increased hydrophilicity of PVDF membrane can be achieved through the addition of Ag/TiO 2 nanoparticles because the surface hydroxyl group ( OH) had great contribution to membrane hydrophilicity. The increased hydrophilicity was also demonstrated by the contact angle measurement. In a word, Ag/TiO 2 improved the surface hydrophilicity of PVDF membrane in contrast with virgin PVDF membrane. Besides, Ag/TiO 2 nanoparticle provided PVDF membrane with an enhanced visible-light response activity. Ag/TiO 2 /PVDF composite membrane showed excellent activity on degradation of methylene blue (MB) and inactivation of bacterial under visible-light illumination. I hope this research can provide a new way for PVDF surface modification.

One new stenine-type alkaloid, tuberostemonine D ( 1 ), together with five known stenine-type alkaloids ( 2 – 6 ) and two known stemoninine-type alkaloids ( 7 and 8 ), were isolated from the roots of Stemona tuberosa . Their structures were elucidated by extensive spectroscopic methods (IR, UV, MS, 1D and 2D NMR), and the structure of 1 was further confirmed by X-ray diffraction analysis. First simultaneous isolation of stenine- and stemoninine-type alkaloids not only added a new chemical type and increased the chemical diversity of Stemona tuberosa , but also provided chemotaxonomic clues for the close relationship between genera Stemona and Stichoneuron , and favored retaining them in the same family.

Five new sesquiterpenoids Nardosinanone A–E (1–5), were isolated from the extract of Nardostachys chinensis, and their structures were determined by extensive spectroscopic analysis. Compound 1 featured a nardosinane sesquiterpenoid with an unusual tricyclic skeleton. Compounds 2–4 were new nardosinane sesquiterpenoids bearing a rare 10,11-epoxy group. The absolute configurations were determined by single-crystal X-ray diffraction analysis, ECD calculation method, the CD analysis of the in situ formed [Rh2(OCOCF3)4] complex, and the CD data analysis based on the octane rule of cyclohexanone.

In this paper, we provide some fuzzy extensions to the well-known K–K–M–S theorem and Zhou’s open K–K–M–S theorem. As an application, we will use one of these results to give a proof for the fuzzy extension to the well-known Scarf’s core existence theorem, which can be used to give another proof for the non-emptiness of the fuzzy core of a pure exchange economy introduced by Florenzano.

Venenum Bufonis, a traditional Chinese medicine, is widely used in the treatment of liver cancer in modern Chinese medical practices. In our search for anti-hepatoma constituents in Venenum Bufonis, bufotalin, bufalin, telocinobufagin and cinobufagin were obtained. Bufotalin was the most potent active compound among these four bufadienolides, and it exerted stronger inhibitory effect on the viability of doxorubicin-induced multidrug resistant liver cancer cells (R-HepG2) than that of their parent cells HepG2. Structure-activity relationship analysis indicated that the acetyl group linked to C-16 of bufadienolides might be useful for increasing anti-hepatoma activity. Further mechanistic studies revealed that bufotalin treatment induced cell cycle arrest at G(2)/M phase through down-regulation of Aurora A, CDC25, CDK1, cyclin A and cyclin B1, as well as up-regulation of p53 and p21. Bufotalin treatment also induced apoptosis which was accompanied by decrease in mitochondrial membrane potential, increases in intracellular calcium level and reactive oxygen species production, activations of caspase-9 and -3, cleavage of poly ADP-ribose polymerase (PARP) as well as changes in the expressions of bcl-2 and bax. It was also found that the inhibition of Akt expression and phosphorylation was involved in apoptosis induction, and specific Akt inhibitor LY294002 or siRNA targeting Akt can synergistically enhanced bufotalin-induced apoptosis. In vivo study showed that bufotalin significantly inhibited the growth of xenografted R-HepG2 cells, without body weight loss or marked toxicity towards the spleen. These results indicate that bufotalin has a promising potential to become a novel anti-cancer agent for the treatment of liver cancer with multidrug resistance.

Angiogenesis is crucial for carcinogenesis and other angiogenic processes. Arenobufagin, one of the major components of toad venom, is a traditional Chinese medicine used for cancer therapy. It inhibits cell growth in several cancer cell lines. However, little is known about arenobufagin's anti-angiogenic activity. In this study, we showed that arenobufagin inhibited vascular endothelial growth factor (VEGF)-induced viability, migration, invasion and tube formation in human umbilical vein endothelial cells (HUVECs) in vitro. Arenobufagin also suppressed sprouting formation from VEGF-treated aortic rings in an ex vivo model. Furthermore, we found that arenobufagin blocked angiogenesis in a matrigel plugs assay. Computer simulations suggested that arenobufagin interacted with the ATP-binding sites of VEGFR-2 by docking. In addition, arenobufagin inhibited VEGF-induced VEGFR-2 auto-phosphorylation and suppressed the activity of VEGFR-2-mediated signaling cascades. Taken together, our findings demonstrate that arenobufagin is a specific inhibitor of VEGF-mediated angiogenesis.

Three new C-3 dehydrated bufadienolides were isolated from the venom of Bufo bufo gargarizans. Their structures were elucidated as 5β,12β-12,14-dihydroxy-11-oxobufa-3,20,22-trienolide (1), 5β,12β-12,14-dihydroxy-11-oxobufa-2,20,22-trienolide (2), and 5β,12α-12,14-dihydroxy-11-oxobufa-2,20,22-trienolide (3) on the basis of extensive spectroscopic analysis, especially 1D NMR and 2D NMR data. In addition, all three compounds were tested for their cytotoxic activities against A549 and HepG2 cancer cell lines. Compounds 2 and 3 showed significant cytotoxicities with IC50 values less than 10 μmol/L on both cancer cells.