10-Hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: 10-Hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
• 化学式: C₂₉H₃₈O₄
• 分子量: 450.6
• InChiKey: KQJSQWZMSAGSHN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  33
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.66
• 拓扑面积：
  74.6
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Method of treating refractory rheumatoid arthritis associated with p53 mutation
  申请人：Macau University of Science and Technology

  公开号：US10688105B2

  公开（公告）日：2020-06-23

  A method for treating a subject suffering from refractory rheumatoid arthritis includes the step of administering an effective amount of a quinonemethide triterpenoid or a pharmaceutically tolerable salt, solvate or anhydrate thereof to the subject. Also is a method for inducing autophagy in a synovial fibroblast, and a method of inducing calcium mobilization in a synovial fibroblast. Further a pharmaceutical composition includes an effective dose of a quinonemethide triterpenoid and an anti-arthritis compound. The quinonemethide triterpenoid is suitable to treat refractory rheumatoid arthritis (RA) in particular ABC-protein-dependent RA and apoptosis-deficient RA. The quinonemethide triterpenoid also possesses significant inhibitory effects on the growth of synovial fibroblasts, in particular modulating the calcium homeostasis in multidrug-resistant rheumatoid arthritis synovial fibroblasts.

  一种治疗患有难治性类风湿性关节炎的受试者的方法，包括向受试者施用有效量的喹烯酮三萜类化合物或其药学上可耐受的盐、溶液剂或水合物。还有一种诱导滑膜成纤维细胞自噬的方法，以及一种诱导滑膜成纤维细胞钙动员的方法。还有一种药物组合物包括有效剂量的喹烯酮三萜类化合物和抗关节炎化合物。喹烯酮三萜类化合物适用于治疗难治性类风湿性关节炎（RA），尤其是ABC蛋白依赖型RA和细胞凋亡缺陷型RA。喹烯酮三萜类化合物还对滑膜成纤维细胞的生长具有显著的抑制作用，特别是能调节耐多药类风湿关节炎滑膜成纤维细胞的钙平衡。
• TREATMENT OF SUBJECTS WITH MULTIDRUG-RESISTANT CANCER
  申请人：Macau University of Science and Technology

  公开号：US20170128394A1

  公开（公告）日：2017-05-11

  A quinonemethide triterpenoid is administered to subjects with multidrug-resistant cancer, in particular a cancer with enhanced expression and/or functional activity of ABC transporter proteins such as P-glycoprotein and/or an apoptosis-deficient, in particular p53-, Bax- or Bak-deficient, cancer, i.e. specific subgroups of subjects with cancer. The quinonemethide triterpenoid is suitable to treat cancer allowing for an accumulation of cytotoxic or therapeutic compounds in the cells while having exceptionally increased cytotoxic activity towards the multidrug-resistant cancer cells and while allowing for an increased activity of chemotherapeutic compounds. Methods for specifically targeting cancer cells with multidrug-resistance and methods for potentiating the activity of a chemotherapeutic compound in those cancer cells are also disclosed. A kit including a quinonemethide triterpenoid and a chemotherapeutic compound is also provided.
• COMPOUNDS, COMPOSITIONS, METHODS, AND USES FOR TREATING LEPTIN RESISTANCE, OBESITY, DIABETES MELLITUS AND METABOLIC SYNDROME
  申请人：Hurt Clarence

  公开号：US20210324031A1

  公开（公告）日：2021-10-21

  Novel leptin and leptin-fusion protein-small molecule drug conjugates are disclosed, where conjugation takes place through the use of cleavable and non-cleavable linkers. The small molecules chemically linked to the protein carrier are imported into the specific leptin-responsive target tissue or cell through receptor-mediated endocytosis and released from the carrier protein through enzymatic cleavage of the linker-drug moiety or through lysosomal degradation of the carrier protein. Free drug then act to modify leptin receptor-triggered biochemical pathways that are altered in conditions of leptin-resistance. Drug will correct altered pathway allowing resensitization of receptor signaling. This can greatly aid in the resolution of pathologies either initiated at the onset of leptin resistance or exacerbated by it.