新闻:佛罗里达州斯克里普斯的科学家开发出新型复合逆转脂

StephenW

http://www.medhelp.org/posts/Hepatitis-B/Scripps-Florida-Scientists-Develop-New-Compound-that-Reverses-Fatty-Liver-Disease/show/1870439
News Release   

    Scripps Florida Scientists Develop New Compound that Reverses Fatty Liver Disease    JUPITER, FL, December 19, 2012 – Scientists from the Florida campus of The Scripps Research Institute (TSRI) have developed the first synthetic compound that can reverse the effects of a serious metabolic condition known as fatty liver disease. True to its name, the disease involves an abnormal buildup of fat in the liver.
The compound—known as SR9238—is the first to effectively suppress lipid or fat production in the liver, eliminating inflammation and reversing fat accumulation in animal models of fatty liver disease. The new compound also significantly lowered total cholesterol levels,although precisely how that occurred remains something of a mystery.
“We’ve been working on a pair of natural proteins called LXRα and LXRβ that stimulate fat production in the liver, and we thought our compound might be able to successfully suppress this process,” said Thomas Burris, a professor at TSRI who led the study, which was recently published in an online edition of the journal ACS Chemical Biology. “Once the animals were put on the drug, we were able to reverse the disease after a single month with no adverse side effects—while they ate a high-fat diet.”
Fatty liver, which often accompanies obesity and type 2 diabetes, frequently leads to more serious conditions including cirrhosis and liver cancer. The condition affects some 10 to 24 percent of the general population, according to a 2003 study in GUT, an international journal of gastroenterology and hepatology.
Burris and his colleagues designed SR9238 so that it would be quickly metabolized in the liver to minimize migration of the drug into the bloodstream, which could lead to side effects.
In the study, mice were fed a high-fat diet for 14 weeks prior to treatment with SR9238. After one month of treatment, the scientists found that the liver’s fat-producing genes were repressed and fat expression in the liver was reduced up to 90 percent.
In addition, the scientists observed an 80 percent reduction of the enzyme responsible for producing cholesterol (3-Hydroxy-3-methylglutaryl coenzyme A Reductase)—the same enzyme targeted by statins.
Markers for liver damage were down as well, which suggests the compound may also have the potential to treat alcohol-related fatty liver damage.
The first author of the study, “A Liver Selective LXR Inverse Agonist that Suppresses Hepatic Steatosis” is Kristine Griffett of TSRI. Other authors include Laura A. Solt, Bahaa El-Dien M. El‐Gendy and Theodore M.Kamenecka, also of TSRI. For more information on the paper, see http://pubs.acs.org/doi/abs/10.1021/cb300541g
The work was supported by the State of Florida.
About The Scripps Research Institute
The Scripps Research Institute (TSRI) is one of the world's largest independent, not-for-profit organizations focusing on research in the biomedical sciences. Over the past decades, TSRI has developed a lengthy track record of major contributions to science and health, including laying the foundation for new treatments for cancer, rheumatoid arthritis, hemophilia, and other diseases.The institute employs about 3,000 people on its campuses in La Jolla, CA, and Jupiter, FL, where its renowned scientists—including three Nobel laureates—work toward their next discoveries. The institute's graduate program, which awards PhD degrees in biology and chemistry, ranks among the top ten of its kind in the nation. For more information, see www.scripps.edu.

StephenW

新闻发布
佛罗里达州斯克里普斯的科学家开发出新型复合逆转脂肪肝疾病

2012年12月19日，佛罗里达州朱庇特 - 从佛罗里达州校园的斯克里普斯研究所（TSRI）的科学家们开发出第一个人工合成的化合物，可以扭转一个严重的代谢状况的影响，被称为脂肪肝疾病。正如它的名字，疾病是不正常的脂肪堆积在肝脏。

化合物SR9238被称为是第一个能有效地抑制脂质或脂肪在肝脏中生产，消除炎症和扭转脂肪堆积在脂肪肝疾病的动物模型。新的化合物也显着降低总胆固醇水平，但正是如何发生仍是一个谜。

“我们一直在说：”一对天然蛋白质称为LXRα和LXRβ，刺激脂肪在肝脏中生产，我们认为我们的化合物可能是能够成功地抑制这个过程中，在TSRI教授托马斯·伯里斯，谁领导了研究，最近发表在ACS化学生物学“杂志网络版。 “一旦动物的药物，我们能逆转病情后，单月没有副作用的影响，而他们吃高脂肪的饮食。”

往往伴随着肥胖和2型糖尿病，脂肪肝，往往会导致更严重的疾病，包括肝硬化和肝癌。条件影响的总人口约10％至24％，根据2003年的研究中GUT，国际胃肠病学和肝病学杂志。

伯里斯和他的同事们设计的SR9238，因此，这将迅速在肝脏代谢的药物，以尽量减少迁移到血液中，这可能导致副作用。

在这项研究中，老鼠被喂食高脂肪的饮食14周，治疗SR9238前。治疗一个月后，科学家们发现，肝脏的脂肪产生的基因被抑制脂肪在肝脏的表达减少高达90％。

此外，科学家们观察到降低了80％的酶负责的制造胆固醇（3  - 羟基-3  - 甲基戊二酰辅酶A还原酶）的他汀类药物的目标相同的酶。

肝损害的标记，这表明该化合物可能也有潜在的治疗酒精性脂肪肝损害。

第一作者的研究中，“A肝选择性的LXR反相激动剂，抑制肝细胞脂肪变性”和Kristine Griffett TSRI。“其他作者包括劳拉A. SOLT，巴哈丁EL演M. EL-Gendy和Theodore M. Kamenecka，也TSRI。有关的文件的更多信息，请参阅http://pubs.acs.org/doi/abs/10.1021/cb300541g
这项工作是由佛罗里达州的支持。

关于斯克里普斯研究所

斯克里普斯研究所（TSRI）是世界上最大的独立的，不以营利为目的的组织在生物医学科学重点研究之一。在过去的几十年里，TSRI科学和健康的重大贡献，包括癌症，类风湿关节炎，血友病，和其他疾病的新的治疗方法奠定了基础制定了一个长期的跟踪记录。在其著名的科学家，包括三位诺贝尔奖得主，他们的努力下发现，该研究所在其校园在加州La Jolla，木星，佛罗里达州，员工约3,000人。该研究所的研究生课程的奖励，生物学和化学的博士学位，其在全国位居前十的行列。有关详细信息，请参阅www.scripps.edu。

StephenW

希望
1。对人类也是有效的;
2。也能控制B型肝炎