Kooperativer Bibliotheksverbund

Berlin Brandenburg

and
and

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
Filter
  • Diterpenes
Type of Medium
Language
Year
  • 1
    Language: English
    In: Marine Drugs, 01 December 2017, Vol.15(12), p.382
    Description: In this paper, we reviewed natural compounds isolated from octocorals belonging to the genus Pachyclavularia, including 20 cembrane-, 39 briarane-, and eight briarellin-related diterpenoids, and one secosterol. The chemical constituents of these 68 secondary metabolites, and their names, structures, and bioactivities, along with studies of their biological activities, are summarized in this review. Based on the literature, many of these compounds possess bioactivities, including anti-inflammation properties, cytotoxicity, and ichthyotoxicity, suggesting that they may have the potential to be developed into biomedical agents for treatment.
    Keywords: Pachyclavularia ; Octocoral ; Cembrane ; Briarane ; Briarellin ; Secosterol ; Bioactivity ; Pharmacy, Therapeutics, & Pharmacology
    E-ISSN: 1660-3397
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 2
    Language: English
    In: Bioorganic & Medicinal Chemistry Letters, 01 June 2015, Vol.25(11), pp.2421-2424
    Description: There are many reports for andrographolide modification regarding antitumor effects. Transformation of the five-membered lactone ring to furan aromatic ring still results in compounds with good cytotoxicity. To determine further the importance of the five-membered lactone ring and to obtain better lead compounds, we transformed the five-membered lactone ring in andrographolide. New types of -labdane diterpene derivatives were made, whose cytotoxic activities were measured in vitro. Preliminary SAR was summarized and two compounds, and , with good cytotoxic activity were obtained, which have the potential to be developed into new antitumor drugs.
    Keywords: Andrographolide ; Ent-Labdane Diterpene ; SAR ; Cytotoxic Activity ; Medicine ; Chemistry ; Anatomy & Physiology
    ISSN: 0960-894X
    E-ISSN: 1464-3405
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 3
    Language: English
    In: Life Sciences, 2011, Vol.89(23), pp.886-895
    Description: Histone modifications play central epigenetic roles in regulating the entire genome of the cell and cell proliferation. Herein, we investigated the effects of the natural compound, 16-hydroxycleroda-3,13-dien-15,16-olide (PL3), on the expressions of histone-modifying enzymes, and examined how it induces apoptosis in leukemia K562 cells. Cell proliferation was determined by an MTT assay, and histone-modifying enzyme gene expressions were investigated by a quantitative real-time PCR. Protein expressions were analyzed by a Western blot analysis. The histone H3K27 distribution was observed with immunofluorescence staining. To verify polycomb repressive complex 2 (PRC2) complex downstream gene expressions, a gene-expression array was performed to determine gene regulations. PL3 induced apoptosis and modulated many histone-modifying enzymes, especially the two PRC2 components, enhancer of zeste homolog 2 (EZH2) and suppressor of zeste 12 homolog (Suz12). Genes repressed by PRC2 were shown to be reactivated by PL3. Of these, 10 genes targeted by the PRC2 complex were identified, and expressions of 10 pro-/antiapoptotic genes were significantly regulated; these effects may have contributed to PL3-induced apoptosis in K562 cells. Regulation of other histone-modifying enzymes, including Aurora B, may also be involved in cell-cycle regulation. Our data suggest that the induction of apoptosis by PL3 might partly occur through both a reduction in PRC2-mediated gene silencing and the reactivation of downstream tumor suppressor gene expressions. PL3 acts as a novel small-molecule histone modulator, which can potentially contribute to cancer chemotherapy singly or as a combined medication.
    Keywords: 16-Hydroxycleroda-3,13-Dien-15,16-Olide ; Apoptosis ; Histone Modulator ; Prc2 Complex ; Histone Modification ; Sciences (General) ; Biology
    ISSN: 0024-3205
    E-ISSN: 1879-0631
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 4
    Language: English
    In: Phytochemistry, November 2016, Vol.131, pp.124-129
    Description: Phytochemical investigation of the ethanolic extract of led to isolation of gramaderins A–D, together with thirteen known compounds. All isolates were assayed for their anti-inflammatory activities. Consequently, 5,7-dihydroxy-3,6,3′,4′,5′-pentamethoxyflavone and 5,3′-dihydroxy-3,6,7,4′,5′-pentamethoxyflavone showed significant bioactivities by inhibiting superoxide anion generation. 8-Acetoxy-pentadeca-1,9 ,14-trien-4,6-diyne-3-ol also demonstrated potent inhibition on elastase release. The gramaderins A/C ( -alkyl linked -lactone) and gramaderins B/D ( -alkyl linked -lactone) co-exist in this plant material, of which the latter derivatives are few in nature. Gramaderins C/D possess a special linear dilactone diterpene skeleton, which never been reported. Phytochemical investigation of the ethanolic extract of led to the isolation of gramaderins A–D. Gramaderins C and D possess a linear dilactone diterpene skeleton.
    Keywords: Grangea Maderaspatana ; Asteraceae ; Diterpenes ; Anti-Inflammatory ; Botany
    ISSN: 0031-9422
    E-ISSN: 1873-3700
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 5
    Language: English
    In: Free Radical Biology and Medicine, 01 August 2011, Vol.51(3), pp.641-657
    Description: Defects in apoptotic pathways confer resistance to tubulin-binding agents via downregulation of caspases or overexpression of antiapoptotic factors, urging the need for novel agents acting on an alternative pathway. The purpose of this study was to investigate whether induction of ROS can induce caspase-independent cell death in breast cancer cells and thereby enhance the activity of paclitaxel. Here, we report that gelomulide K acts as a caspase-independent cell death-inducing agent that synergizes with paclitaxel in breast cancer cells and has low toxicity in normal cells. Treatment with gelomulide K induced PARP-1 hyperactivation, AIF nuclear translocation, and cytoprotective autophagy. These effects were associated with increased ROS production and a decrease in cellular GSH levels in cancer cells. Furthermore, pretreatment with NAC, a precursor of intracellular GSH, effectively abrogated gelomulide K-induced caspase-independent cell death and autophagy, suggesting that ROS-mediated downstream signaling is essential to the anticancer effects of gelomulide K. Additionally, in a xenograft model, gelomulide K induced PARP-1 activation and reduced tumor growth. In terms of structure–activity relationships, analysis not only showed a correlation between ROS levels and drug activity but also highlighted the importance of the 8,14-epoxy group. Taken together, our results show that enhancement of paclitaxel activity can be achieved with gelomulide K and that the structurally relevant pharmacophore provides important insight into the development of new caspase-independent cell death-inducing agents.
    Keywords: Ros ; Caspase-Independent Cell Death ; Parp-1 ; Breast Cancer ; Free Radicals ; Biology ; Anatomy & Physiology
    ISSN: 0891-5849
    E-ISSN: 1873-4596
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 6
    In: Organic & Biomolecular Chemistry, 2011, Vol.9(3), pp.834-844
    Description: New eunicellin-base diterpenoids, klysimplexins I–T ( 1–12 ), were isolated from a cultured soft coral Klyxum simplex . Their structures were elucidated by spectroscopic methods, particularly in 1D and 2D NMR experiments. The absolute stereochemistry of 4 was determined by Mosher's method. Compounds 9 and 12 have been shown to exhibit cytotoxicity toward a limited panel of cancer cell lines. Compounds 2–6 , 10 and 11 were found to display significant in vitro anti-inflammatory activity in LPS-stimulated RAW264.7 macrophage cells by inhibiting the expression of the iNOS protein. Compounds 10 and 11 also could effectively reduce the level of COX-2 protein.
    Keywords: Chemistry;
    ISSN: 1477-0520
    E-ISSN: 1477-0539
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 7
    Language: English
    In: Toxicology, 2011, Vol.285(1), pp.72-80
    Description: ► Natural product PL3 induced cancer cell apoptosis and cell cycle arrest. ► PL3 targeted and de-regulated PI3K pathway activities. ► De-activated PI3K pathway caused Aurora B degradation and spindle dysfunction. ► PL3 could reverse the drug-resistance of Bcr-ABL T315I-positive cells to Imatinib. The PI3K-AKT pathway and Aurora kinase play essential roles in such cellular processes as cell survival, angiogenesis, and differentiation, and are usually expressed at maximum levels during cancer cell proliferation. The present study investigated the effect of the natural compound, 16-hydroxycleroda-3,13-dien-15,16-olide (PL3), on regulating the PI3K-AKT pathway and Aurora B, which led to cancer cell apoptosis. PL3 acts as a PI3K inhibitor by influencing cell survival, signaling transduction, and cell cycle progression. It was observed that PL3 targeted and induced dephosphorylation of the PI3K pathway, degradation of Aurora B and mitotic-related gene expressions, and sequentially shut down the cell cycle. This eventually resulted in cell death. As Aurora B was downregulated, spindle dysfunction and destruction of the G /M phase checkpoint resulted in DNA-damaged cells undergoing apoptosis. Moreover, PL3 also resensitized T315I-mutated Bcr-ABL BA/F3 cells to improve the cytotoxicity of Imatinib in Imatinib-resistant cell line. Taken together, PL3 can perturb the PI3K-AKT pathway and Aurora B resulting in gene silencing and cell cycle disturbance. It was demonstrated that PL3 acted like a novel small-molecule PI3K modulator, thereby potentially contributing to cancer chemotherapy and combination medication.
    Keywords: 16-Hydroxycleroda-3,13-Dien-15,16-Olide ; Aurora B ; Pi3k ; Mitotic Block ; Apoptosis ; Pharmacy, Therapeutics, & Pharmacology ; Public Health
    ISSN: 0300-483X
    E-ISSN: 1879-3185
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 8
    Language: English
    In: Bioorganic & Medicinal Chemistry Letters, 01 March 2012, Vol.22(5), pp.1922-1925
    Description: A series of tetracyclic diterpenoids bearing α-methylenelactone group were synthesized from stevioside. Some of them exhibited significant cytotoxicity against all the six tumor cell lines with the IC values ranging from 0.09 to 5.71 μM. A series of tetracyclic diterpenoids bearing the α-methylenelactone group have been synthesized and screened for their in vitro anti-tumor activities against six human cancer cell lines. The results showed that compounds , and exhibited significant cytotoxicity superior to the positive control doxorubicin hydrochloride against MDA-MB-231, K562 and HepG2 cell lines. In particular, compound was identified as the most promising anticancer agent against HepG2 cells with IC value of 0.09 μM.
    Keywords: Tetracyclic Diterpenoids ; Steviol ; Isosteviol ; Α-Methylenelactone ; Anti-Tumor Activity ; Medicine ; Chemistry ; Anatomy & Physiology
    ISSN: 0960-894X
    E-ISSN: 1464-3405
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 9
    Language: English
    In: Marine drugs, 09 August 2016, Vol.14(8)
    Description: Two new cubitanoids, nanoculones A and B (1 and 2), and three new cembranoids, nanolobols A-C (3-5), as well as six known compounds, calyculone I (6), sinulariuol A (7), sinulariols C, D, H, and J (8-11), were isolated from the soft coral Sinularia nanolobata, collected off the coast of the eastern region of Taiwan. Their structures were elucidated on the basis of extensive spectroscopic analysis. Cytotoxicity of compounds 1-11 was evaluated. The nitric oxide (NO) inhibitory activity of selected compounds was further measured by assay of lipopolysaccharide (LPS)-stimulated NO production in activated RAW264.7 cells. The results showed that none of 1-11 exhibited cytotoxicity against the tested cancer cell lines, whereas compound 8 was found to significantly reduce NO production.
    Keywords: Sinularia ; Cubitane ; Nanoculones A and B ; Nanolobols A–C ; Anthozoa -- Chemistry ; Antineoplastic Agents -- Chemistry ; Diterpenes -- Pharmacology ; Nitric Oxide -- Metabolism
    E-ISSN: 1660-3397
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 10
    Language: English
    In: Planta Medica, 2015, Vol.81(12/13)
    In: Planta Medica, 2015, Vol.81(12/13), pp.1017-1028
    Description: Aconite species have played an important role in human history. Aconitum species have been used worldwide as poisons as well as remedies. Their potential in targeting several ailments such as pain, rheumatism, and lethargy has been recognized by Western, Chinese, and Indian health care practitioners. Aconite use in herbal preparations has declined, especially in Europe and the United States, in the first half of the twentieth century due to several reported toxicity cases. The situation has changed with the application of new technologies for the accurate analysis of its toxic components and the development of efficient detoxification protocols. Some Asian countries started small clinical trials to evaluate the potency and safety of different marketed aconite preparations. The current review summarizes therapeutic uses of aconite preparations in China, Taiwan, India, and Japan. It also highlights clinical trial results with special emphasis on their limitations. Modern drugs and pharmacopoeial preparations derived from aconite are also discussed.
    Keywords: aconitum ; Ranunculaceae ; Fuzi ; Monkshood ; Traditional chinese medicine ; Ayurvedic medicine
    ISSN: 0032-0943
    E-ISSN: 1439-0221
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. Further information can be found on the KOBV privacy pages