ABSTRACT
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.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Cell Proliferation/drug effects , Drugs, Chinese Herbal/pharmacology , Prostate-Specific Antigen/genetics , Prostatic Neoplasms/genetics , Receptors, Androgen/genetics , Cell Line, Tumor , Humans , Male , Prostate-Specific Antigen/metabolism , Prostatic Neoplasms/drug therapy , Prostatic Neoplasms/metabolism , Prostatic Neoplasms/physiopathology , Receptors, Androgen/metabolism , Signal Transduction/drug effectsABSTRACT
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.
Subject(s)
Asteraceae/chemistry , Lactones/isolation & purification , Plant Extracts/isolation & purification , Sesquiterpenes/isolation & purification , China , Lactones/chemistry , Mass Spectrometry , Molecular Conformation , Nuclear Magnetic Resonance, Biomolecular , Optical Rotation , Plant Extracts/chemistry , Plant Roots/chemistry , Rhizome/chemistry , Sesquiterpenes/chemistry , Spectrophotometry, InfraredABSTRACT
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.
Subject(s)
Cytokines/metabolism , Drugs, Chinese Herbal/pharmacology , Isodon , Th1 Cells/metabolism , Th2 Cells/metabolism , Animals , Diterpenes, Kaurane , Drugs, Chinese Herbal/isolation & purification , Female , Interferon-gamma/metabolism , Interleukin-2/metabolism , Interleukin-4/metabolism , Interleukin-5/metabolism , Isodon/chemistry , Male , Mice , Mice, Inbred BALB C , Plants, Medicinal/chemistry , Tumor Necrosis Factor-alpha/metabolismABSTRACT
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.
Subject(s)
Asteraceae , Phytotherapy , Plant Extracts/chemistry , Humans , Magnetic Resonance Spectroscopy , Mass Spectrometry , Naphthalenes/chemistry , Plant Roots , Polycyclic Sesquiterpenes , Rhizome , Sesquiterpenes/chemistry , Spectrophotometry, InfraredABSTRACT
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.
Subject(s)
Asteraceae/chemistry , Sesquiterpenes/chemical synthesis , Animals , Hepatocytes/drug effects , Light , Magnetic Resonance Spectroscopy , Mice , Molecular Structure , Oxidation-Reduction , Plant Roots/chemistry , Sesquiterpenes/metabolism , Sesquiterpenes/pharmacology , Sesquiterpenes/radiation effects , Singlet OxygenABSTRACT
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.
Subject(s)
Asteraceae/chemistry , Furans/isolation & purification , Lignans/isolation & purification , Furans/chemistry , Furans/pharmacology , HIV Reverse Transcriptase/antagonists & inhibitors , Lignans/chemistry , Lignans/pharmacology , Magnetic Resonance SpectroscopyABSTRACT
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.
Subject(s)
Furans/isolation & purification , Rehmannia/chemistry , Animals , Furans/chemistry , Furans/pharmacology , Immune System/drug effects , Mice , Platelet Aggregation Inhibitors/pharmacologyABSTRACT
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.
Subject(s)
Huperzia , Phytotherapy , Triterpenes/chemistry , Humans , Magnetic Resonance Spectroscopy , Plant Components, Aerial , Plant RootsABSTRACT
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.
Subject(s)
Asteraceae , Phytotherapy , Plant Extracts/chemistry , Sesquiterpenes/chemistry , Humans , Oxidation-Reduction , Plant Roots , RhizomeABSTRACT
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.
Subject(s)
Asteraceae/chemistry , Naphthalenes/chemistry , Naphthalenes/isolation & purification , Crystallography, X-Ray , Plant Extracts/chemistry , Plant Roots/chemistry , Spectrum AnalysisABSTRACT
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).
