Simulated digestion of dried leaves of Artemisia annua consumed as a treatment (pACT) for malaria.
Simulated digestion of dried leaves of Artemisia annua consumed as a treatment (pACT) for malaria.
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DOI：
10.1016/j.jep.2013.11.043
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发表时间：
2014-02-03
影响因子：
5.4
通讯作者：
Towler, Melissa J.
中科院分区：
文献类型：
--
作者：
Weathers, Pamela J.;Jordan, Nikole J.;Lasin, Praphapan;Towler, Melissa J.
青蒿素(AN)由青蒿素(Artemisia Annua)生产，青蒿素是一种中草药，长期以来被用作治疗发烧的茶汤；它也是目前有效治疗疟疾的青蒿素联合疗法(ACTS)的关键成分。最近，我们发现，产青蒿素并含有青蒿素协同作用的黄酮类化合物的整个植物的干燥叶子似乎比ACT口服治疗疟疾更有效，成本更低；然而，人们对消化如何影响干燥叶子中青蒿素和类黄酮类化合物的释放知之甚少。在目前的研究中，我们使用模拟的消化系统来确定青蒿素和黄酮类化合物在吸收到血液之前是如何释放的。不同的给药方式和主食与干叶联合消化，以考察它们对青蒿素和黄酮类化合物生物利用度的影响。在口腔、胃和肠道阶段结束时回收消化物质，分离成固体和液体部分，并提取用于测定青蒿素和总黄酮类化合物。添加蔗糖、各种食用油和大米并不能减少青蒿素在肠液中的释放量，但与未包埋的干叶相比，黄酮类的释放量增加近一倍。用羟甲基纤维素或明胶胶囊包埋干燥叶后，青蒿素的释放量减少了50%，但黄酮类的释放量没有变化。在小米或玉米粉存在下，青蒿素的释放量有所下降，但类黄酮的释放量没有变化。对缺乏青蒿素的突变体青蒿素的使用表明，植物基质在确定青蒿素在消化过程中如何受到影响方面是至关重要的。这项研究提供的证据表明，青蒿素和类黄酮类化合物如何受到口服植物的消化和饮食成分的影响，提供治疗作用的口服植物，以及通过干燥的叶子提供的青蒿素如果以片剂形式提供而不是胶囊形式提供，可能更具生物利用度。
Artemisinin (AN) is produced by Artemisia annua, a medicinal herb long used as a tea infusion in traditional Chinese medicine to treat fever; it is also the key ingredient in current artemisinin-based combination therapies (ACTs) effective in treating malaria. Recently we showed that dried leaves from the whole plant A. annua that produces artemisinin and contains artemisinin-synergistic flavonoids seems to be more effective and less costly than ACT oral malaria therapy; however little is known about how digestion affects release of artemisinin and flavonoids from dried leaves. In the current study we used a simulated digestion system to determine how artemisinin and flavonoids are released prior to absorption into the bloodstream. Various delivery methods and staple foods were combined with dried leaves for digestion in order to investigate their impact on the bioavailability of artemisinin and flavonoids. Digestate was recovered at the end of the oral, gastric, and intestinal stages, separated into solid and liquid fractions, and extracted for measurement of artemisinin and total flavonoids. Compared to unencapsulated digested dried leaves, addition of sucrose, various cooking oils, and rice did not reduce the amount of artemisinin released in the intestinal liquid fraction, but the amount of released flavonoids nearly doubled. When dried leaves were encapsulated into either hydroxymethylcellulose or gelatin capsules, there was >50% decrease in released artemisinin but no change in released flavonoids. In the presence of millet or corn meal, the amount of released artemisinin declined, but there was no change in released flavonoids. Use of a mutant A. annua lacking artemisinin showed that the plant matrix is critical in determining how artemisinin is affected during the digestion process. This study provides evidence showing how both artemisinin and flavonoids are affected by digestion and dietary components for an orally consumed plant delivered therapeutic and that artemisinin delivered via dried leaves would likely be more bioavailable if provided as a tablet instead of in a capsule.
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影响因子：
3.8
作者：
Hollman, PCH
通讯作者：
Hollman, PCH
影响因子：
3.8
作者：
Kean, Ellie G.;Bordenave, Nicolas;Ferruzzi, Mario G.
通讯作者：
Ferruzzi, Mario G.
影响因子：
8.1
作者：
Peters, Catrina M.;Green, Rodney J.;Janle, Elsa M.;Ferruzzi, Mario G.
通讯作者：
Ferruzzi, Mario G.
DOI：
10.1007/s11101-010-9166-0
发表时间：
2011-06
期刊：
Phytochemistry reviews : proceedings of the Phytochemical Society of Europe
影响因子：
--
作者：
Weathers PJ;Arsenault PR;Covello PS;McMickle A;Teoh KH;Reed DW
通讯作者：
Reed DW
影响因子：
5.1
作者：
Xu, MC;Shi, ZQ;He, BL
通讯作者：
He, BL