The Applications of Folcisteine

Folcisteine, also referred to as N-acetylthioproline (ATCA), is recognized as a "plant stimulant" due to its distinctive capacity to enhance water and nutrient uptake in crops. Additionally, it is widely utilized in both pharmaceutical and agricultural applications.

Fig.1. Folcisteine

Synthetic Methods

Two primary synthetic routes are generally employed for the preparation of folcisteine.

Method 1: A mixture of cysteine, an inorganic base, and formaldehyde is reacted to generate the intermediate 4-carboxythiazolidine. This intermediate is subsequently treated with an acetylation reagent. The reaction mixture is then heated under reflux, followed by concentration and washing with water. Folcisteine is obtained in high yield after vacuum drying at 50–80 °C.^[1]

Method 2: L-Cysteine is reacted with an aqueous formaldehyde solution to yield L-thioproline. An acetylation reagent is then added directly to the same reaction vessel (one-pot synthesis). After the reaction reaches completion, activated carbon is introduced for decolorization. The target compound, folcisteine, is subsequently obtained through cooling-induced crystallization.^[2]

Pharmaceutical Applications

Folcisteine initially served as a pharmaceutical intermediate for protection against myocardial ischemia. Recently, researchers have discovered new functions for it.

Protection and repair following neural injury have consistently posed severe challenges for neuroscientists. Through years of dedicated efforts, numerous studies have confirmed that the nervous system possesses plasticity, manifested not only as a strong compensatory and adaptive capacity to various external stimuli but, more importantly, as an inherent ability to undergo structural and functional self-repair or reconstruction after injury. The realization of this process requires both the initiation of certain gene regulatory programs within neural cells and a highly complex local environment with specific conditions. In one example, Li Changxia disclosed a pharmaceutical formulation for neural repair involving the combined application of nodakenin and lobelin. Experimental results demonstrated that nodakenin and lobelin, within a ratio range of 15:1 to 20:1, promoted nerve regeneration and functional recovery in Balb/C mice with sciatic nerve injury. These findings indicate that nodakenin and lobelin exhibit a remarkable synergistic effect on neural repair within this specific ratio range.^[3]

Agricultural Applications

In agriculture, folcisteine functions as a biological stimulant that enhances biological activity, cytokines, and auxin. Its applications include regulating crop cell osmotic pressure, promoting seed germination, cell division, and elongation, reducing transplant shock, protecting chlorophyll, improving nutrient utilization, maintaining water and nutrient transport balance, extending the flowering period, increasing fruit setting rate and yield, delaying senescence, enhancing stress resistance, and reducing fruit drop.^[4]

Wan Cui disclosed a fertilizer synergist composed of a functional additive and a balanced stabilizer in a mass ratio of 1:1. The functional additive consists of folcisteine and DCPTA (2-(3,4-Dichlorophenoxy)triethylamine), while the balanced stabilizer comprises potassium acetate and potassium citrate. The mass ratio of lobeline to potassium acetate is 1:1, and the mass ratio of DCPTA to potassium citrate is 1:1. The mass fraction of lobeline in the fertilizer synergist is 5–20%, and that of DCPTA is 30–45%. This invention utilizes the functional additive and balanced stabilizer as core substances, which effectively promote crop absorption and utilization of nutrient elements, enhance plant nutrient assimilation efficiency, and are beneficial for both primary and secondary metabolism in plants.^[5]

Sudarshan Chemical Industries disclosed a sprayable synergistic aqueous solution for plant application comprising: folcisteine (ATCA) in the range of 4 to 10% by mass of the solution, folic acid in the range of 0.05 to 0.2% by mass of the solution, and chelated micronutrients providing effectively boron at 0.02% by mass of the solution, magnesium at 0.03%, manganese at 0.02%, zinc at 0.7%, and ammonium molybdate at 0.02% by mass of the solution, along with nitrogen at 4 to 6% by mass of the solution. The combination of micronutrients, nitrogen, folcisteine, and folic acid has a synergistic effect that significantly enhances the growth and yield attributes of tomatoes, as observed following the foliar application of the aqueous solution in accordance with the invention.^[6]

References

[1]Zhu, Donghai, A kind of method for preparing N-acetyl-DL-thioproline, CN104592083.

[2]Zhang, Yongchang, Process for preparation of folcisteine, CN102234252.

[3]Li Changxia, Application of medicine containing nodakenin in neural restoration, CN106361759.

[4]Han, Aohui. Physiological mechanism of sodium salicylate and folcisteine on alleviating salt stress in wheat seedlings, Scientific Reports (2023), 13(1), 22869.

[5]Wan Cui, Fertilizer synergist and its preparation method and application of improving fertilizer utilization rate, CN111763115.

[6]Sudarshan Chemical Industries Ltd, Sprayable plant nutraceutical comprising N-acetyl thiazolidine-4-carboxylic acid, folic acid, chelated micronutrients and nitrogen, IN2007MU01178.

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