[Effect of compound Chinese traditional medicine PC-SPES II in inhibiting proliferation of human prostate cancer cell LNCaP and on expressions of AR and PSA].

To investigate the effect of compound Chinese traditional medicine PC-SPES II I in inhibiting proliferation of human prostate cancer cell LNCaP based on the androgen receptor (AR) signaling pathway. The effect of PC-SPES II on LNCaP cell proliferation was detected by MTT assay. According to the findings, at the mass concentration of 180-1 440 mg x L(-1), PC-SPES II significantly inhibited the proliferation of LNCaP cells; the IC50 of PC-SPES II at 24 h and 48 h were 311.48, 199.01 mg x L(-1), respectively. The flow Cytometry detection showed 240 mg x L(-1) PC-SPES II arrested cells in G2/M phase, and an obvious apoptotic peak appeared before G0/G1 peak and rose over time. Meanwhile, Hoechst 33258 staining revealed apoptotic cellular morphology. Annexin V-FITC/PI staining manifested an increase in apoptotic cell ratio at the PC-SPES II concentration of 480 mg x L(-1) in a dose dependent manner. The prostate specific antigen (PSA) secretion of LNCaP cells was tested by PSA ELISA kit. Besides, compared with 25 mg x L(-1) Bic, 480 mg x L(-1) PC-SPES II significantly reduced the cell secretion of PSA. The AR and PSA mRNA and protein expressions were detected by qRT-PCR and Western blot. According to the results, after the induction of LNCaP cells with synthetic androgen 25 µg x L(-1) R1881, 240-480 mg x L(-1) PC-SPES II notably down-regulated the AR and PSA mRNA and protein expressions and inhibited the translocation of AR from cytoplasm to nucleus. In summary, PC-SPES II significantly can inhibit the in vitro proliferation of LNCaP cells and arrest cell cycle arrest in G2/M phase. Its mechanism may be associated with the down-regulation of the AR and PSA expressions and the inhibition of AR nuclear translocation.

A novel bieremophilanolide from Ligularia lapathifolia.

A new bieremophilanolide was isolated from the roots and rhizomes of Ligularia lapathifolia. Its structure was established as 8,8'-bi-3beta-angeloyloxy-eremophil-7(11)-en-12,8alpha(14beta,6alpha)-diolide (1) by IR, MS, 1D, and 2D NMR experiments.

[Effect of glaucocalyxin A on level of Th1/Th2 type cytokines in mice].

OBJECTIVE: To research the effect of glaucocalyxin A (GLA) on the level of Th1/Th2 type cytokines in mice. METHOD: By using flow cytometer with CBA software to detect Th1/Th2 type cytokines. RESULT: GLA had insighificant inhibitory effects on Th1 and Th2 cytokines (IL-2, IFN-gamma,TNF-alpha, IL-4 and IL-5) induced by ConA, in which more potential on cytokines from Th1 than those of from Th2 were displayed. However, GLA could produce inhibition on IL-2, IFN-gamma and TNF-alpha and acceleration on IL-4 and IL-5. CONCLUSION: Immunosuppressive effect of GLA is related to the influence the level of Th1/Th2 type cytokines.

New eremophilane-type sesquiterpenes from Ligularia hodgsonii.

Four new eremophilanlides (1- 4) together with a known sesquiterpene were isolated from the roots and rhizomes of Ligularia hodgsonii. The structures of these new compounds were established as 6beta-(2'-methylbutanoyloxy)-10beta-acetoxy-3 beta, 8beta-dihydroxyeremophil-7(11)-en-8,12-olide (1), 6beta,10 beta-dihydroxyeremophil-7(11)-en-8alpha,12-olide (2), 3beta-acetoxy-6,9-dien-8-oxoeremophil-12-nor-11-ketone (3), and 3beta-acetoxy-6alpha, 8alpha-dihydroxyeremophil-7(11), 9-dien-8,12-olide (4) by means of mass, IR and NMR spectroscopy.

Sensitized photooxidation of furanoeremophilane with singlet oxygen and their biogenetic relationship.

In an attempt to explore the biogenetic relationship of furanoeremophilane derivatives and eremophilan-8alpha,12-olides, produced in Ligularia and their structure-activity relationship, we studied the photosensitized oxidation of furanoeremophilane-type sesquiterpenes. Under the condition of several solvents solution Irradiation with a 200 W incandescent lamp of furanoeremophilan-14beta,6alpha-olide isolated from Ligularia vellerea, in various solutions with methylene blue, rose bengal, toluidine blue and safranine T gave several products. The products were isolated by chromatographic procedure and their structures were elucidated as eremophilan-14beta,6alpha,8alpha,12-diolide derivatives by NMR, IR and MS methods. A reaction mechanism has been proposed.

A new pinoresinol-type lignan from Ligularia kanaitizensis.

A new pinoresinol-type Lignan, 9alpha-angloyloxypinoresinol (1), was isolated from the roots and rhizomes of Ligularia kanaitizensis (Franch.) Hand.-Mazz, in addition to a known compound, 9alpha-hydroxypinoresinol (2). The structure of this new lignan (1) was established on the basis of 1D and 2D NMR experiments. Anti-HIV-1 RT biological assay showed that 1 was inhibitory to HIV-1 RT.

A novel bis-furan derivative, two new natural furan derivatives from Rehmannia glutinosa and their bioactivity.

A novel bis-furan derivative and two new natural furan derivatives were isolated from the CHCl3 extracts of the dried roots of Rehmannia glutinosa (Gaerth) Lilosch. Their structures were identified as 1,5-bis(5-methoxymethyl)furan-2-yl-penta-1,4-dien-3-one 1, (E)-4-(5-(methoxymethyl)furan-2-yl)but-3-en-2-one 2 and (E)-4-(5-(hydroxymethyl)furan-2-yl)but-3-en-2-one 3 on the basis of spectral data. Moreover, biological assay showed that 1 (10 microg/mL) and 3 (10 microg/mL) can promote immune activity, 2 (100 microg/mL) and 3 (100 microg/mL) inhibit immune activity and 1 can inhibit blood platelet aggregation.

Serratane-type triterpenoids from Huperzia serrata.

Sixteen serratane-type triterpenoids including three new compounds, 14beta,15beta-epoxyserratan-3beta,21beta,29-triol (1), serrat-14-en-3beta,21beta,29-triol (2) and serrat-14-en-3alpha,21beta,24,29-tetraol (3), were isolated from the whole plant of Huperzia serrata (Thunb) Trev. The structures of these new compounds (1-3) were elucidated on the basis of spectral analysis.

New eremophilane-type sesquiterpenes from Ligularia lapathifolia.

Seven new eremophilanolides were isolated from the roots and rhizomes of Ligularia lapathifolia. Their structures were established as 3beta-angeloyloxy-8beta H-eremophil-7(11)-ene-12,8alpha (14beta, 6alpha)-diolide, 3beta-angeloyloxy-8beta-hydroxyeremophil-7(11)-ene-12,8alpha(14beta,6alpha)-diolide,3beta-angeloyloxy-8beta-methoxyeremophil- 7(11)-ene-12,8alpha(14beta,6alpha)-diolide,3beta-angeloyloxy-8beta-ethoxyeremophil-7(11)-ene-12, 8alpha (14beta,6alpha)-diolide, 3beta-angeloyloxy-10beta- hydroxyeremophil-8(9),7(11)-diene-12,8(14beta,6alpha)-diolide, 3beta-angeloyloxy-8,12-expoy-12alpha-hydroxy-8beta-methoxyeremophil-7(11)-en-14beta,6alpha-olide and 3beta-angeloyloxyeremophilan-7,11-dien-14beta,6alpha-olide, by means of spectroscopic analyses. Moreover, application of a photooxygenation reaction on 7 resulted in the generation of 2 with an alpha,beta-unsaturated gamma-lactone moiety. This biomimetic transformation supports a biogenetic pathway proposed for 2.

Two new norsesquiterpenes from Ligularia lapathifolia.

Two new norsesquiterpenes were isolated from the extracts of the roots and rhizomes of Ligularia lapathifolia (Franch.) Hand.-Mazz. Their structures were identified as 2-acetyl-3a-methyl-5-(2-methyl-but-2-enoyloxy)-3a,4,5,6,7,7a-hexahydro-H-indene-4-carboxylic acid (1) and 2-acetyl-8a-methyl-2-(2-methyl-but-2-enoyloxy)-6-oxo-1,2,3,4,4a,5,6,8a-octahydro-naphthalene-1-carboxylic acid (2), respectively, on the basis of spectral data and for 1 by single-crystal X-ray analysis.

Two new guaianolides and a new daucene derivative from Sinodielsia yunnanensis.

From the roots and rhizomes of Sinodielsia yunnanensis, three new sesquiterpenes were isolated and their structures were established as 5alpha,6beta- H-1(10),3,7(11)-guaiatrien-12,6alpha-olide ( 1), 5alpha,6beta,7beta- H-1(10),3-guaiadien-12,6alpha-olide ( 2) and 5beta-hydroxy-10alpha- O-angeloyl-3-oxodauc-8-ene ( 3) by means of spectroscopic analyses and single-crystal X-ray experiment (for compound 1).