α-倒捻子素 | 6147-11-1

• 物质功能分类: 生物化工 - 中草药成分
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 中文名称: α-倒捻子素
• 中文别名: a-倒捻子素；山竺提取物；罗汉果提取物；曼果斯廷；1,3,6-三羟基-7-甲氧基-2,8-双(3-甲基-2-丁烯基)-9H-氧杂蒽-9-酮
• 英文名称: α-mangostin
• 英文别名: alpha-Mangostin；mangostin；1,3,6-trihydroxy-7-methoxy-2,8-bis(3-methyl-2-butenyl)-9H-xanthen-9-one；1,3,6-trihydroxy-7-methoxy-2,8-bis(3-methyl-2-butenyl)-9H-xanthene-9-one；1,3,6-trihydroxy-7-methoxy-2,8-bis(3-methylbut-2-en-1-yl)-9H-xanthen-9-one；1,3,6-trihydroxy-7-methoxy-2,8-bis(3-methylbut-2-enyl)xanthen-9-one
• CAS: 6147-11-1
• 化学式: C₂₄H₂₆O₆
• 分子量: 410.467
• InChiKey: GNRIZKKCNOBBMO-UHFFFAOYSA-N

物化性质

• 熔点：
  180-182°C
• 沸点：
  640.1±55.0 °C(Predicted)
• 密度：
  1.265±0.06 g/cm3(Predicted)
• 溶解度：
  可溶于甲醇：1mg/mL，透明，淡黄色
• 最大波长(λmax)：
  346nm(MeOH)(lit.)
• 物理描述：
  Solid
• 颜色/状态：
  Faint yellow to yellow powder
• 蒸汽压力：
  9.44X10-15 mm Hg at 25 °C (est)
• 稳定性/保质期：

  Stable under normal temperatures and pressures.

• 分解：
  Nitrogen oxides, carbon monoxide, irritating and toxic fumes and gases, carbon dioxide, nitrogen.
• 聚合：
  Has not been reported.
• 解离常数：
  pKa1 = 3.68 (primary carbonyl); pKa2 = 7.69 (secondary carbonyl); pKa3 = 9.06 (tertiary carbonyl) (est)
• 碰撞截面：
  198.8 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

计算性质

• 辛醇/水分配系数(LogP)：
  6.3
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  96.2
• 氢给体数：
  3
• 氢受体数：
  6

ADMET

毒理性

• 相互作用

改变的膜完整性和炎症在心血管损伤中扮演关键角色。作者们研究了外源性给予alpha-山竹素对β-肾上腺素能儿茶酚胺诱导的心血管毒性的有益效果，特别关注了膜ATP酶、溶酶体水解酶以及炎症介质肿瘤坏死因子-α（TNF-α）和环氧合酶-2（COX-2）在白化大鼠中的表达。用异丙肾上腺素（150 mg/kg体重，ip）诱导大鼠2天，显著增加了血清和心脏溶酶体水解酶（β-D-葡萄糖苷酶、β-D-半乳糖苷酶、β-D-N-乙酰葡萄糖苷酶、酸性磷酸酶和组织蛋白酶-D）的活性。心脏中的钠、钙水平显著增加，而钾水平降低，同时伴随着膜结合磷酸酶（Na(+)-K(+) ATP酶、Ca(2+) ATP酶和Mg(2+) ATP酶）的异常活性，在给予ISO的大鼠心脏中观察到这些变化。通过Western印迹法评估心脏TNF-α和COX-2的表达。心脏TNF-α和COX-2的表达在ISO中毒的大鼠中显著升高。预先口服给予alpha-山竹素（200mg/kg体重）8天，显著减轻了这些异常，并使水平恢复到接近正常，与ISO中毒组大鼠相比。总之，alpha-山竹素通过有效减轻ISO诱导的氧化应激和细胞损伤，保持了心肌膜完整性，并减少了异常的TNF-α和COX-2表达。细胞正常化的恢复证明了alpha-山竹素的细胞保护作用。

Altered membrane integrity and inflammation play a key role in cardiovascular damage. /The authors/ investigated the salubrious effect of exogenously administered alpha-mangostin against beta-adrenergic cathecolamine-induced cardiovascular toxicity with special reference to membrane ATPases, lysosomal hydrolases and inflammatory mediators TNF-alpha and Cyclooxygenase-2 (COX-2) expressions in albino rats. Induction of rats with isoproterenol (150 mg/kg body wt, ip) for 2 days resulted in a significant increase in the activities of serum and cardiac lysosomal hydrolases (beta-d-glucuronidase, beta-d-galactosidase, beta-d-N-acetylglucosaminidase, acid phosphatase and cathepsin-D). A significant increase in cardiac levels of sodium, calcium with a decrease in the level of potassium paralleled by abnormal activities of membrane-bound phosphatases (Na(+)-K(+) ATPase, Ca(2+) ATPase and Mg(2+) ATPase) were observed in the heart of ISO-administered rats. Cardiac TNF-alpha and COX-2 expressions were assessed by Western blotting. Cardiac TNF-alpha and COX-2 expressions were significantly elevated in ISO-intoxicated rats. Pre-co-treatment with alpha-mangostin (200mg/kg body wt.) orally for 8 days significantly attenuated these abnormalities and restored the levels to near normalcy when compared to ISO intoxicated group of rats. In conclusion, alpha-mangostin preserves the myocardial membrane integrity and extenuates anomalous TNF-alpha and COX-2 expressions by mitigating ISO-induced oxidative stress and cellular damage effectively. Restoration of cellular normalcy accredits the cytoprotective role of alpha-mangostin.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

顺铂（CDDP）是一种化疗药物，会导致与氧化/硝化应激相关的肾毒性。α-芒果亭（α-M）是从山竹中提取的一种具有抗氧化和抗炎特性的氧杂蒽酮。本研究的目的是评估α-M对顺铂诱导的肾毒性的肾保护作用。α-M以每天12.5毫克/千克的剂量给药，连续10天（顺铂注射前7天和注射后3天）。在第7天，大鼠接受单次顺铂注射（7.5毫克/千克，腹腔注射）；3天后处死大鼠。α-M减轻了肾功能障碍、结构损伤、氧化/硝化应激、过氧化氢酶表达下降以及肿瘤坏死因子α和转化生长因子β的mRNA水平升高。总之，α-M对顺铂诱导的肾毒性的肾保护作用与减轻氧化/硝化应激、炎症和纤维化标志物以及保持过氧化氢酶活性有关。

Cisplatin (CDDP) is a chemotherapeutic agent that produces nephrotoxicity associated with oxidative/nitrosative stress. alpha-Mangostin (alpha-M) is a xanthone extracted from mangosteen with antioxidant and anti-inflammatory properties. The purpose of this study was to evaluate the renoprotective effect of alpha-M on the CDDP-induced nephrotoxicity. alpha-M was administered (12.5 mg/kg/day, i.g.) for 10 days (7 days before and 3 days after CDDP injection). On day 7, rats were treated with a single injection of CDDP (7.5 mg/Kg, i.p.); 3 days after the rats were killed. alpha-M attenuated renal dysfunction, structural damage, oxidative/nitrosative stress, decrease in catalase expression and increase in mRNA levels of tumour necrosis factor alpha and transforming growth factor beta. In conclusion the renoprotective effect of alpha-M on CDDP-induced nephrotoxicity was associated with the attenuation in oxidative/nitrosative stress and inflammatory and fibrotic markers and preservation of catalase activity.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

来自 Garcinia mangostana L. 树皮中的 alpha-Mangostin 被发现对耐万古霉素的肠球菌（VRE）和耐甲氧西林的金黄色葡萄球菌（MRSA）具有活性，其最小抑菌浓度（MIC）分别为6.25和6.25至12.5微克/毫升。我们的研究表明，alpha-Mangostin 与庆大霉素（GM）对 VRE 有协同作用，以及 alpha-Mangostin 与盐酸万古霉素（VCM）对 MRSA 有协同作用。进一步的研究显示，alpha-Mangostin 与市售抗生素如氨苄西林和米诺环素之间存在部分协同作用。这些发现表明，单独使用 alpha-Mangostin 或与 GM 联合对抗 VRE，以及与 VCM 联合对抗 MRSA 可能有助于控制 VRE 和 MRSA 感染。

alpha-Mangostin, isolated from the stem bark of Garcinia mangostana L., was found to be active against vancomycin resistant Enterococci (VRE) and methicillin resistant Staphylococcus aureus (MRSA), with minimum inhibitory concentration (MIC) values of 6.25 and 6.25 to 12.5 ug/mL, respectively. Our studies showed synergism between alpha-mangostin and gentamicin (GM) against VRE, and alpha-mangostin and vancomycin hydrochloride (VCM) against MRSA. Further studies showed partial synergism between alpha-mangostin and commercially available antibiotics such as ampicillin and minocycline. These findings suggested that alpha-mangostin alone or in combination with GM against VRE and in combination with VCM against MRSA might be useful in controlling VRE and MRSA infections.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 立即急救：确保已经进行了充分的中和。如果患者停止呼吸，请开始人工呼吸，最好使用需求阀复苏器、球囊阀面罩设备或口袋面罩，按训练操作。如有必要，执行心肺复苏。立即用缓慢流动的水冲洗受污染的眼睛。不要催吐。如果患者呕吐，让患者向前倾或将其置于左侧（如果可能的话，头部向下），以保持呼吸道畅通，防止吸入。保持患者安静，维持正常体温。寻求医疗帮助。 /毒物A和B/

/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 基本治疗：建立专利气道（如有需要，使用口咽或鼻咽气道）。如有必要，进行吸痰。观察呼吸不足的迹象，如有需要，辅助通气。通过非循环呼吸面罩以10至15升/分钟的速度给予氧气。监测肺水肿，如有必要，进行治疗……。监测休克，如有必要，进行治疗……。预防癫痫发作，如有必要，进行治疗……。对于眼睛污染，立即用水冲洗眼睛。在运输过程中，用0.9%的生理盐水（NS）持续冲洗每只眼睛……。不要使用催吐剂。对于摄入，如果患者能吞咽、有强烈的干呕反射且不流口水，则用温水冲洗口腔，并给予5毫升/千克，最多200毫升的水进行稀释……。在去污后，用干燥的无菌敷料覆盖皮肤烧伤……。/毒药A和B/

/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险品标志：
  T
• 安全说明：
  S45
• 危险类别码：
  R25
• WGK Germany：
  1,2
• 海关编码：
  2932999099
• 危险品运输编号：
  UN 2811 6.1 / PGIII
• RTECS号：
  ZD6122420
• 危险性防范说明：
  P501,P273,P270,P264,P301+P312+P330
• 危险性描述：
  H302,H413
• 储存条件：
  2-8°C

制备方法与用途

概述

α-倒捻子素是从山竹子中提取的一种氧杂蒽酮类化合物，源于天然山竹子的有效成分。它具有安全无毒及悠久食用历史等特点，为深入研究α-倒捻子素作为药物提供了理论和应用基础。

生物活性

α-倒捻子素（alpha-MangOSa href=https://www.molaid.com/MS_19470 target="_blank">STin）是一种具有广泛生物活性的膳食呫吨酮，包括抗氧化、抗过敏、抗病毒、抗菌、抗炎及抗癌作用。它也是IDH1突变体（如IDH1-R132H）的抑制剂，Ki值为2.85 μM。

靶点

α-倒捻子素对IDH1-R132H表现出选择性抑制效果，但不抑制IDH1。它以竞争性方式抑制α-酮戊二酸（α-KG）与IDH1-R132H的结合，并在IDH1 (+/R132H) MCF10A细胞中促进5-甲基胞嘧啶和组蛋白H3精氨酸三甲基化位点的去甲基化。在用α-倒捻子素处理的细胞中，细胞增殖以剂量依赖性方式显著减少。α-倒捻子素还增加Bax（促凋亡）、裂解 caspase-3、裂解 caspase-9 和裂解-PARP 的水平。

此外，它显著抑制光诱导的视网膜色素上皮细胞退化及200 μM H₂O₂诱导的RPE细胞凋亡。H₂O₂诱导的活性氧（ROS）生成和光诱导的丙二醛（MDA）生成也被α-倒捻子素抑制。

体内研究

α-倒捻子素通过减少p53表达，降低TAA_DMSO治疗后的肝纤维化风险。与单独使用DMSO相比，在用α-倒捻子素处理后，血清中转氨酶（AST和ALT）的水平显著下降。

化学性质

α-倒捻子素是一种白色结晶粉末，可溶于甲醇、乙醇及DMSO等有机溶剂。它来源于藤黄科山竹壳、罗汉果及山竺。

用途

α-倒捻子素具有治疗腹泻、疟疾、抗炎、抗溃疡以及抗白血病和败血症的作用，可用于含量测定/鉴定/药理实验等。其药理活性包括抗氧化、抗炎、抗菌及抗癌作用。

反应信息

• 作为反应物：
  描述：

  α-倒捻子素 在 sodium hydride 、 乙硫醇 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 5.0h， 以54%的产率得到gamma-倒捻子素
  参考文献：
  名称：

  作为磷酸甘油酸变位酶 1 抑制剂的 1,3,6,7-四羟基呫吨酮衍生物的设计、合成和生物学评价

  摘要：

  磷酸甘油酸变位酶 1 (PGAM1) 是癌症治疗的一个有希望的目标。在此，我们发现 α-mangostin 和 γ-mangostin 表现出中等的 PGAM1 抑制活性，IC 50 分别为 7.2 μM 和 1.2 μM。基于 α-芒果苷，设计、合成了一系列 1,3,6,7-四羟基呫吨酮衍生物，并在体外评估了其对 PGAM1 的抑制作用。还清楚地描述了这种新化合物的显着构效关系（SAR）和新的结合模式。该研究为进一步优化具有 1,3,6,7-四羟基呫吨酮骨架的 PGAM1 抑制剂或新型抑制剂的从头设计提供了有价值的信息。

  DOI：

  10.1016/j.bmcl.2021.127820
• 作为产物：
  描述：

  2,4-二苄氧基苯甲醛 在 palladium on activated charcoal 盐酸 、 四氯化碳 、 sodium periodate 、 四氧化锇 、 正丁基锂 、 溴 、 仲丁基锂 、 甲酸铵 、 potassium carbonate 、 间氯过氧苯甲酸 、 三苯基膦 、 2-碘酰基苯甲酸 作用下， 以 四氢呋喃 、 甲醇 、 乙醚 、 二氯甲烷 、 氯仿 、 水 、 二甲基亚砜 、 N,N-二甲基甲酰胺 、 丙酮 、 甲苯 为溶剂， 生成 α-倒捻子素
  参考文献：
  名称：

  第一个直接合成的α-芒果，酸性鞘磷脂酶的有效抑制剂

  摘要：

  α倒捻子素的全合成图1A已经实现。通过使用PPh 3 -CCl 4条件进行了构建黄酮骨架的关键环化反应。讨论了1a和二苯甲酮中间体16对酸性鞘磷脂酶的抑制活性。

  DOI：

  10.1016/s0040-4039(01)02137-2
• 作为试剂：
  描述：

  花生四烯酸 在 cyclooxygenase-1 、 α-倒捻子素 作用下， 反应 0.17h， 生成 地诺前列酮
  参考文献：
  名称：

  Inhibition of cyclooxygenase and prostaglandin E2 synthesis by γ-mangostin, a xanthone derivative in mangosteen, in C6 rat glioma cells

  摘要：

  The fruit hull of mangosteen, Garcinia mangostana L., has been used for many years as a medicine for treatment of skin infection, wounds, and diarrhea in Southeast Asia. In the present study, we examined the effect of gamma-mangostin, a tetraoxygenated diprenylated xanthone contained in mangosteen, on arachidonic acid (AA) cascade in C6 rat glioma cells. gamma-Mangostin had a potent inhibitory activity of prostaglandin E-2 (PGE(2)) release induced by A23187, a Ca2+ ionophore. The inhibition was concentration-dependent, with the IC50 value of about 5 muM. gamma-Mangostin had no inhibitory effect on A23187-induced phosphorylation of p42/p44 extracellular signal regulated kinase/mitogen-activated protein kinase or on the liberation of [C-14]-AA from the cells labeled with [C-14]-AA. However, gamma-mangostin concentration-dependently inhibited the conversion of AA to PGE(2) in microsomal preparations, showing its possible inhibition of cyclooxygenase (COX). In enzyme assay in vitro, gamma-mangostin inhibited the activities of both constitutive COX (COX-1) and inducible COX (COX-2) in a concentration-dependent manner, with the IC50 values of about 0.8 and 2 muM, respectively. Lineweaver-Burk plot analysis indicated that gamma-mangostin competitively inhibited the activities of both COX-1 and -2. This study is a first demonstration that gamma-mangostin, a xanthone derivative, directly inhibits COX activity. (C) 2002 Elsevier Science Inc. All rights reserved.

  DOI：

  10.1016/s0006-2952(01)00810-3

文献信息

• Semisynthesis and Biological Evaluation of Xanthone Amphiphilics as Selective, Highly Potent Antifungal Agents to Combat Fungal Resistance
  作者：Shuimu Lin、Wan Ling Wendy Sin、Jun-Jie Koh、Fanghui Lim、Lin Wang、Derong Cao、Roger W. Beuerman、Li Ren、Shouping Liu

  DOI：10.1021/acs.jmedchem.7b01348

  日期：2017.12.28

  New efficient antifungal agents are urgently needed to treat drug-resistant fungal infections. Here, we designed and synthesized a series of cationic xanthone amphiphilics as antifungal agents from natural α-mangostin to combat fungal resistance. The attachment of cationic residues on the xanthone scaffold of α-mangostin resulted in interesting antifungal agents with a novel mode of action. Two lead

  迫切需要新型有效的抗真菌剂来治疗耐药性真菌感染。在这里，我们设计和合成了一系列阳离子x吨两亲性化合物，它们是从天然α-Mangostin中作为抗真菌剂来对抗真菌的抵抗力。阳离子残基在α-芒果的黄酮酮骨架上的附着产生了具有新颖作用方式的有趣的抗真菌剂。两种先导化合物（1和2）对多种真菌病原体均显示出有效的抗真菌活性，其中包括耐药性白色念珠菌，曲霉和镰刀菌。菌株，对哺乳动物细胞的细胞毒性和溶血活性低。两种化合物均可通过直接破坏真菌细胞膜而迅速杀死真菌，并避免产生耐药性。另外，化合物1在真菌性角膜炎的鼠模型中显示出有效的体内抗真菌活性。据我们所知，以前尚未报道基于膜的基于黄酮的抗真菌剂。这些结果表明，化合物1和2可能是治疗耐药性真菌感染的有前途的候选药物。
• Nonpeptidic Amphiphilic Xanthone Derivatives: Structure–Activity Relationship and Membrane-Targeting Properties
  作者：Jun-Jie Koh、Hanxun Zou、Shuimu Lin、Huifen Lin、Rui Ting Soh、Fang Hui Lim、Wee Luan Koh、Jianguo Li、Rajamani Lakshminarayanan、Chandra Verma、Donald T. H. Tan、Derong Cao、Roger W. Beuerman、Shouping Liu

  DOI：10.1021/acs.jmedchem.5b01500

  日期：2016.1.14

  explored the effects of the structures on their membrane-targeting properties. The SAR analysis successfully identified 3a with potent MICs (1.56–3.125 μ/mL) and lower hemolytic activity (80.2 μg/mL for 3a versus 19.7 μg/mL for 2c). Compound 3a displayed a membrane selectivity of 25.7–50.4. Thus, 3a with improved HC50 value and promising selectivity could be used as a lead compound for further structural

  我们最近报道了一种高效的非肽类蒽酮2c（AM-0016）的生物启发性合成，它具有针对MRSA的有效抗菌活性。在本文中，我们报告了一系列非肽两亲性蒽酮衍生物的详尽的结构-活性关系（SAR）分析，以试图鉴定出具有更低溶血活性和更大膜选择性的更有效的化合物。在这项研究中分析了四十六种两亲性蒽酮衍生物，并根据间隔物长度，阳离子部分，亲脂性链和三臂功能化将其结构分为四类。我们评估和探索了结构对其膜靶向性能的影响。SAR分析成功识别出3a具有有效的MIC（1.56-3.125μ/ mL）和较低的溶血活性（3a的溶血活性为80.2μg / mL，而2c的溶血活性为19.7μg/ mL ）。化合物3a的膜选择性为25.7-50.4。因此，具有提高的HC 50值和有希望的选择性的3a可用作进一步治疗MRSA感染的结构优化的先导化合物。
• Controlled Release of Nitric Oxide And Drugs From Functionalized Macromers And Oligomers
  申请人：Bezwada Rao S.

  公开号：US20120035259A1

  公开（公告）日：2012-02-09

  The present invention provides NO and, optionally, drug releasing macromers and oligomers wherein the drug molecule and NO releasing moiety are linked an absorbable macromer or oligomeric chain susceptible to hydrolytic degradation and wherein the macromer or oligomer comprises of repeat units derived from safe and biocompatible molecules such as glycolic acid, lactic acid, caprolactone and p-dioxanone. Furthermore, the present invention relates to controlled release of nitric oxide (NO) and/or drug molecule from a NO and drug releasing macromer or oligomer. Moreover, the present invention also relates to medical devices, medical device coatings and therapeutic formulations comprising of nitric oxide and drug releasing macromers and oligomers of the present invention.

  本发明提供了一氧化氮(NO)和可选的药物释放的大分子和寡聚物，其中药物分子和一氧化氮释放部分通过可吸收的大分子或可水解降解的寡聚物链连接，并且大分子或寡聚物由来自诸如乙醇酸、乳酸、己内酰胺和对二恶烷等安全且生物相容的分子的重复单元组成。此外，本发明还涉及从一氧化氮和/或药物分子释放的大分子或寡聚物控制释放一氧化氮(NO)。此外，本发明还涉及包含本发明的一氧化氮和药物释放大分子和寡聚物的医疗器械、医疗器械涂层和治疗方法。
• ABSORBABLE BRANCHED POLYESTERS AND POLYURETHANES
  申请人：Bezwada Biomedical, LLC

  公开号：US20140142199A1

  公开（公告）日：2014-05-22

  The present invention relates to the discovery of a new class of hydrolysable isocyanates, hydrolysable branched polyols and branched absorbable polyesters and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, stents, highly porous foam, reticulated foam, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers can have a controlled hydrolytic degradation profile.

  本发明涉及一种新型可水解异氰酸酯、可水解支链多元醇及其制备的支链可吸收聚酯和聚氨酯的发现。由此得到的可吸收聚合物可用于药物输送、支架、高孔隙率泡沫、网状泡沫、组织工程、组织粘合剂、防止粘连、骨蜡制剂、医疗设备涂层、表面改性剂以及其他可植入医疗设备。此外，这些可吸收聚合物可以具有受控的水解降解特性。
• Functionalized drugs and polymers derived therefrom
  申请人：Bezwada S. Rao

  公开号：US20060172983A1

  公开（公告）日：2006-08-03

  Compounds selected from: where DRUG-OH, DRUG-COOH and DRUG-NH 2 are biologically active compounds; each X is independently selected from —CH 2 COO— (glycolic acid moiety), —CH(CH 3 )COO— (lactic acid moiety), —CH 2 CH 2 OCH 2 COO— (dioxanone moiety), —CH 2 CH 2 CH 2 CH 2 CH 2 COO— (caprolactone moiety), —(CH 2 ) y COO—, where y is 2-4 or 6-24 and —(CH 2 CH 2 O) z CH 2 COO—, where z is 2-24; each Y is independently selected from —COCH 2 O— (glycolic ester moiety), —COCH(CH 3 )O— (lactic ester moiety), —COCH 2 OCH 2 CH 2 O— (dioxanone ester moiety), —COCH 2 CH 2 CH 2 CH 2 CH 2 O— (caprolactone ester moiety), —CO(CH 2 ) m O—, where m is 2-4 or 6-24 and —COCH 2 O(CH 2 CH 2 O) n — where n is between 2-24; R′ is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; and p is 1-6. Multi-functional compounds and drug dimers, oligomers and polymers are also disclosed.

  从中选择的化合物：其中DRUG-OH，DRUG-COOH和DRUG-NH2是生物活性化合物；每个X独立地从— COO—（乙二酸基团），—CH(CH3)COO—（乳酸基团），— O COO—（二氧杂环己酮基团），— COO—（己内酯基团），—(CH2)yCOO—中选择，其中y为2-4或6-24和—( O)z COO—，其中z为2-24；每个Y独立地从—CO O—（乙二酸酯基团），—COCH( )O—（乳酸酯基团），—CO O O—（二氧杂环己酮酯基团），—CO O—（己内酯酯基团），—CO( )mO—，其中m为2-4或6-24和—CO O( O)n—，其中n为2-24；R′为氢，苄基或烷基，烷基可以是直链或支链；p为1-6。还披露了多功能化合物和药物二聚体、寡聚体和聚合物。