丙酮萃取姜黄中含姜黄素油树脂的动力学、热力学行为及其生物利用度

A. Kunyima, J. C. Kuburhanwa, H. M. Kaseya, M. Kunyima
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引用次数: 0

摘要

背景:为什么姜黄素这种神奇的两亲性化合物,具有非常非凡的治疗潜力(因为可以与生物体中的许多靶点发生反应),在生物体中的生物利用度很弱,并且代谢成活性非常弱或无活性的化合物?如何实质性地提高其生物利用度,从而提高其在生物体中的吸收,以便将其纳入药物制造中,而不管其纳米颗粒是如何引起进一步的注意的?目的:研究姜黄素在体外的动力学和热力学行为或与其他化合物共同给药的反应,以了解如何增加其在体内的吸收,因为生物利用度需要姜黄素的水溶性(亲水性),而姜黄素分子是天然疏水的。目的:因此,我们的目标是更好地了解天然姜黄素在生物体中的吸收,而不诉诸于纳米颗粒中的化学转化,这是额外的努力。方法:以丙酮为溶剂,利用KUNYIMA第一定律对姜黄(Curcuma Longa L.)中含有姜黄素的油树脂进行了动力学和热力学研究,丙酮可通过催化加氢(H2,Ni)或化学还原(LiAlH4)在类水溶剂丙烯-2-醇中还原。结果:测定了含姜黄素的油树脂在250 rpm(圆/ min)和500 rpm (k= 0.1520±0.0005)min-1条件下在封闭体系中27,5℃、恒压丙酮中提取的弱总动力学常数。结论:昆依马第一定律为从姜黄中提取含姜黄素的油树脂的动力学和热力学研究提供了可能。动力学常数是测定含有姜黄素的油树脂溶解度的一种方法,因此也是测定姜黄素在给定溶剂中的溶解度的一种方法,本文所讨论的溶剂是乙醇和丙酮。结果表明,动力学常数与溶剂溶解度成反比,可以作为测定姜黄素提取吸热或放热行为的参数。姜黄素在乙醇和丙酮中的体外吸热行为,通过磁搅拌增加,表明其生物利用度较弱,因此姜黄素的生物利用度较弱。本实际研究的挑战是提高我们对姜黄中含姜黄素的油树脂的体外提取动力学和热力学的理解,以预测其生物利用度仍然较弱,从而有效地验证其作用。提高生物利用度将通过改进姜黄素的配方或通过新的给药途径来实现。姜黄素类似物的概念也是促进其作用的一种方式。这种现象在类水溶剂中越放热,所涉及的化合物就越具有生物可利用性。本研究通过含姜黄素的油树脂提取的吸热行为和较弱的整体动力学常数揭示了姜黄素在丙酮中的酮型优势和姜黄素(姜黄素)缺乏生物利用度。丙酮中熵的变化毫不奇怪地显示了萃取后系统的扰动。比较了姜黄素在丙酮和乙醇中作为类水溶剂的动力学常数值,发现姜黄素在丙酮中的溶解度较好,动力学常数较弱。姜黄素预示着充满希望的未来。
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Kinetic and Thermodynamic Behavior of Extraction of Oleoresin Containing Curcuminoids from Turmeric (Curcuma longa L.) in Acetone and Their Bioavailability
Background: Why this miraculous and amphiphilic compound, the curcumin, which has a very extraordinary therapeutic potential (because can react with many targets in the organism), has a weak bioavailability in the organism and is metabolized in compounds having very weak activity or inactive compounds?. How to improve substantially its bioavailability and therefore its absorption in the organism in order to allow its incorporation in making of pharmaceuticals regardless of its nanoparticles of which obtention is furthermore hardworking? Aim: It seems indicated to search the response in the kinetic and thermodynamic behavior of this compound or in its co-administration with the other compounds in vitro in order to understand how to increase its absorption in vivo because bioavailability entails hydrosolubility (hydrophile) of curcuminoids of which the molecules are naturally hydrophobes. Objective: So our objective is to make better our understanding of the absorption of natural curcuminoids in the organism without resorting to chemical transformation in nanoparticles that is additionally hardworking. Methodology: In this paper, kinetic and thermodynamic study of extraction of oleoresin containing curcuminoids from Turmeric (Curcuma Longa L.), using KUNYIMA’s first law, has been performed in acetone that can be reduced in propan-2-ol which is water-like solvent by catalytic hydrogenating (H2,Ni ) or by chemical reduction (LiAlH4). Results: The weak global kinetic constant of extraction of oleoresin containing curcuminoids has been determined at 250 rpm (round per minute) and found the same at 500 rpm (k= 0.1520 ± 0.0005) min-1 for temperature of 27,5°C and constant pressure in acetone in closed system. Conclusion: Kunyima’s first law has made possible the kinetic and thermodynamic study of extraction of oleoresin containing curcuminoids from Turmeric. Kinetic constant is a measure of solubility of oleoresin containing curcuminoids and therefore a measure of solubility of curcuminoids in a given solvent, ethanol and acetone being concerned in this paper as solvents. Results show that kinetic constant is inversely proportional to solubility of solvent and it can be a parameter abling the determination of the endothermic or exothermic behavior of extraction of curcuminoids. The endothermic behavior of curcuminoids hereby determined in ethanol and acetone in vitro, increased by magnetic stirring, suggests their weak bioavailability and therefore the weak bioavailability of curcumin. The challenge of this actual research is to improve our understanding of kinetics and thermodynamics of extraction of oleoresin containing curcuminoids from Turmeric in vitro in order to presage their bioavailability still weak for an efficient validated action. The increase of bioavailability will be done whether through improved formulations of curcumin or through new pathways of administration. The conception of curcumin analogous is also a way to promote its effects. More the phenomenon is exothermic in water-like solvents, more the involved chemical compound is bioavailable. The study revealed the predominance of keto form of curcumin in acetone and the lack of bioavailability of curcumin (curcuminoids) through the endothermic behavior of extraction of oleoresin containing curcuminoids and through the weak global kinetic constant. The variation of entropy in acetone has shown without surprise the disturbance of the system after extraction. The values of kinetic constants in acetone and ethanol as water-like solvents have been compared and showed the great solubility of curcuminoids in acetone evidenced by the weak kinetic constant compared to that in ethanol. Curcumin predicts anyway hopeful future.
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