CAS: 11079-53-1; Hyperforin

该化合物是一种自然产生的多酚化合物,主要见于称为St. John's Wort 的超生性激素,它具有生物活性成分的作用,有助于植物的药用特性,特别是在治疗中度和中度抑郁方面.希伯林展示了一种复杂的结构,其特点是双环系统和多种功能组合在一起,有助于其药理效应.已知它是一种选择性的血清素和无肾上腺再摄入抑制剂,提高了大脑...

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    专利号:WO-2019190945-A1
    优先权日:2018-03-29
    标 题 :Biosynthesis of olivetolic acid
    发明人:GONZALEZ RAMON; TAN ZAIGAO; CLOMBURG JAMES M
    权利人:UNIV RICE WILLIAM M
    摘要:We present a biosynthetic approach to engineer novel microbes, such as Escherichia coli , for the production of olivetolic acid and other aromatic polyketides, as well as various downstream products that can be made therefrom. We engineered an E. coli strain that synthesizes olivetolic acid from a principle carbon source in vivo by expressing olivetolic acid synthase and olivetolic acid cyclase with the required modules of a β-oxidation reversal for hexanoyl-CoA generation. Further, we engineered an E. coli strain that synthesizes olivetolic acid which integrated additional auxiliary enzymes for increasing both hexanoyl-CoA and malonyl-CoA, enabling the synthesis of about 75 mg/L olivetolic acid and a productivity of 9.3 mg/hr olivetolic acid produced per gram dry weight of cells.

    专利号:US-2025066826-A1
    优先权日:2023-08-21
    标 题 :Artificial synthesis method for malonyl-coenzyme a (coa) and use thereof
    发明人:TAN ZAIGAO; LIU TIANGANG; LI JIAN
    权利人:UNIV SHANGHAI JIAOTONG
    摘要:An artificial synthesis method for malonyl-CoA and use thereof are provided. By means of heterologous expression of an aminotransferase and a malonyl-CoA reductase, an artificial synthesis pathway for synthesizing malonyl-CoA by using β-alanine (β-ala) as a precursor is constructed as follows: firstly, under catalysis of a transaminase, β-ala transfers amino groups to α-ketonic acid (such as pyruvic acid, oxaloacetic acid, or α-ketoglutaric acid, etc.), to form an intermediate product 3-oxopropanoate and a corresponding amino acid; the 3-oxopropanoate generates malonyl-CoA under the action of the malonyl-CoA reductase. This pathway addresses the defects of the natural malonyl-CoA synthesis pathway, such as low carbon utilization, consumption of energy substance ATP, release of greenhouse gas CO 2 , and strict regulation of pathway enzymes, a pyruvate dehydrogenase (PDH) and an acetyl-CoA carboxylase (ACC), thereby achieving high yielding of products using malonyl-CoA as a precursor, including flaviolin, octanoic acid, phloroglucinol, pentadecaheptaene, natamycin, and spinosad.

    专利号:WO-2008071173-A1
    优先权日:2006-12-12
    标题 :Preparations for inhibiting prostaglandin e2 synthesis
    发明人:WERZ OLIVER; KOEBERLE ANDREAS
    权利人:UNIV EBERHARD KARLS; WERZ OLIVER; KOEBERLE ANDREAS
    摘要:The present invention relates to preparations of acylphloroglucinols, in particular hyperforin and myrtucommulone and derivatives thereof, the provision of these preparations for the therapeutic treatment of inflammatory diseases, painful and feverous conditions and cancer diseases which are accompanied by increased activity of the inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) or increased prostaglandin E2 synthesis, and also the appertaining methods.

    专利号:US-7854946-B1
    优先权日:2007-05-31
    标题:Anti-inflammatory and anti-HIV compositions and methods of use
    发明人:HILLWIG MATTHEW LEE
    权利人:UNIV IOWA STATE RES FOUND INC
    摘要:The metabolic fingerprint and anti-inflammatory activity and anti-HIV activity of H. gentianoides is disclosed. High performance liquid chromatography (HPLC) analysis shows that H. gentianoides contains a family of compounds, including some not previously observed in other Hypericum species. H. gentianoides extracts and fractions from these extracts reduce prostaglandin E2 synthesis in mammalian macrophages and inhibit HIV in infected HeLa cells. The present invention provides extracts and fractions thereof from H. gentianoides for use in pharmaceutical compositions and methods for the treatment or inhibition of inflammation, prostaglandin E-mediated disease, disorder or condition, a cyclooxygenase-mediated disease, disorder or condition, or an HIV infection.

    专利号:US-9321713-B2
    优先权日:2011-06-03
    标 题:Hyperforin analogs, methods of synthesis, and uses thereof
    发明人:SHAIR MATTHEW D; SPARLING BRIAN A; MOEBIUS DAVID
    权利人:SHAIR MATTHEW D; SPARLING BRIAN A; MOEBIUS DAVID; HARVARD COLLEGE
    摘要:The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisioned useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.

    专利号:US-10202326-B2
    优先权日:2014-10-21
    标题:Polyprenylated phloroglucinol compounds as potent P-glycoprotein inducers
    发明人:BHARATE SANDIP; KUMAR AJAY; BHARATE JAIDEEP; JOSHI PRASHANT; WANI ABUBAKAR; MUDUDUDDLA RAMESH; SHARMA ROHIT; VISHWAKARMA RAM
    权利人:COUNCIL SCIENT IND RES
    摘要:The present invention relates to the polyprenylated phloroglucinol compounds of formulae I and II. The present invention also provides synthesis and p-glycoprotein induction activity of the alkyl- and acyl-polyprenylated phloroglucinol compounds. Further, use of the compounds as p-glycoprotein inducers and methods of treatment of Alzheimer's disease using compounds of the invention are also provided.
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    主要参考文献


    1: Li XX, Yan Y, Zhang J, Ding K, Xia CY, Pan XG, Shi YJ, Xu JK, He J, Zhang WK. Hyperforin: A natural lead compound with multiple pharmacological activities. Phytochemistry. 2023 Feb;206:113526. doi: 10.1016/j.phytochem.2022.113526. Epub 2022 Nov 26. 33(3):565-580.e7. doi: 10.1016/j.cmet.2021.02.007.
    12:635076. doi: 10.3389/fimmu.2021.635076.
    4: Bouron A. Cellular neurobiology of hyperforin. Phytother Res. 2023 Nov 14. doi: 10.1002/ptr.8063. Epub ahead of print. 67(20):2201-7. doi: 10.1016/j.phytochem.2006.08.017. Epub 2006 Sep 14.

    合成参考文献


    参考文献:10.2165/11530120-000000000-00000
    摘要:Canning S, Waterman M, Orsi N, Ayres J, Simpson N, Dye L. The efficacy of Hypericum perforatum (St John's wort) for the treatment of premenstrual syndrome: a randomized, double-blind, placebo-controlled trial. CNS Drugs. 2010 Mar;24(3):207–25. doi: 10.2165/11530120-000000000-00000.
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