Phosphatidylcholines,soya is an essential phospholipid from soybean for cell formation, growth, and death.[1] It is always used in the preparation of liposomes.[2] Soya lecithin origin phosphatidylcholine (Soya PC) was identified as a natural TLR4 antagonist by the computational study.[3]
In vitro, fibroblasts display sensitivity toward the soybean phosphatidylcholine liposomes with an IC50 of 150 μM. Because of the lesser efficency with these liposomes bind to cells, in vitro experiment it shown that phosphatidylcholine liposomes produced no detectable growth inhibitory effects (IC50 > 400 lM) . soya-phosphatidylcholines liposomes present in abundance linoleic acid, which as an essential fatty acid normally obtained from external sources, resulting in the proliferation of the broblasts seen at concentrations below 50 μM and the reduction in cell proliferation occurring at soya-phosphatidylcholines phospholipid concentrations above 50 μM.[2] In vitro, treatment with 10 and 50 μM soya-phosphatidylcholines liposomes, there exsits an increase in the number of fibroblasts per well comparedto the control group, while at phospholipid concentrations exceeding 100μM, a clear inhibitory effect was observed.[4]
In vivo experiment it demonstrated that treatment with 5 mg/kg and 10 mg/kg Soya phosphatidylcholines significantly decreased the respiration rate whereas, tidal volume and airflow rate were found to be significantly increased compared to asthmatic rats. In the meanwhile, the total leukocytes and differential leukocytes count, eosinophils, lymphocytes in the blood of asthmatic rats also showed significantly decreased after treatment with 5 mg/kg and 10 mg/kg Soya PC. In vivo test it indicated that serum triglyceride level was obviously decreased in soya phosphatidylcholines (5 mg/kg and 10 mg/kg) treated asthmatic rats, however, treatment with 5 mg/kg and 10 mg/kg Soya phosphatidylcholines did not show the modulation in serum glucose and cholesterol level in asthmatic rats.
参考文献:
[1]. Chiang YP, et al. Sphingomyelin synthases 1 and 2 exhibit phosphatidylcholine phospholipase C activity. J Biol Chem. 2021 Dec;297(6):101398.
[2]. Berrocal MC, et al. Comparison of the effects of dimyristoyl and soya phosphatidylcholine liposomes on human fibroblasts. Drug Deliv. 2000 Jan-Mar;7(1):37-44.
[3]. Thakur VR, et al. An anti-asthmatic activity of natural Toll-like receptor-4 antagonist in OVA-LPS-induced asthmatic rats. Clin Exp Pharmacol Physiol. 2018 Nov;45(11):1187-1197.
[4]. Berrocal MC, et al. Aging of soya-PC liposomes containing vitamin E reverses the stimulating effects of freshly prepared liposomes on growth of fibroblasts in culture. Drug Deliv. 1998;5(4):243-50.
Phosphatidylcholines,soya 是大豆中细胞形成、生长和死亡所必需的磷脂。[1]常用于脂质体的制备。[2] 大豆卵磷脂来源的磷脂酰胆碱 (Soya PC) 经计算研究确定为天然 TLR4 拮抗剂。[3]
在体外，成纤维细胞对大豆磷脂酰胆碱脂质体表现出敏感性，IC50 为 150 μM。由于这些脂质体与细胞结合的效率较低，体外实验表明磷脂酰胆碱脂质体没有产生可检测的生长抑制作用 (IC50 > 400 μM)。大豆磷脂酰胆碱脂质体富含亚油酸，亚油酸作为一种必需脂肪酸，通常从外部来源获得，导致成纤维细胞在浓度低于 50 μM 时增殖，而大豆磷脂酰胆碱磷脂浓度高于 50 时细胞增殖减少μM.[2] 在体外，用10和50μM大豆磷脂酰胆碱脂质体处理，与对照组相比，每孔成纤维细胞数量增加，而当磷脂浓度超过100μM时，观察到明显的抑制作用。[4]
体内实验表明，与哮喘大鼠相比，用 5 mg/kg 和 10 mg/kg 大豆磷脂酰胆碱处理可显着降低呼吸率，而潮气量和气流率显着增加。同时，用5mg/kg和10mg/kg Soya PC处理后，哮喘大鼠血液中的总白细胞和白细胞分类计数、嗜酸性粒细胞、淋巴细胞也有显着下降。体内试验表明，大豆磷脂酰胆碱（5mg/kg和10mg/kg）治疗哮喘大鼠血清甘油三酯水平明显降低，而5mg/kg和10mg/kg大豆磷脂酰胆碱治疗没有表现出调节作用对哮喘大鼠血糖和胆固醇水平的影响。
| Cell experiment [1]: | |
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Cell lines |
Human fibroblasts |
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Preparation Method |
Human fibroblasts were incubated for 72 h with low (50 μM) and high (200 μM) concentrations of large, unilamellar (LUV) soya-phosphatidylcholines liposomes in the presence and absence of vitamin E (soya-phosphatidylcholines:vitamin E; 10:0.5). |
|
Reaction Conditions |
50 μM and 200 μM, 72h |
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Applications |
No significant changes in cell viability were observed between untreated fibroblasts and those incubated with 50 μM soya-phosphatidylcholines liposomes. In contrast, a marked loss of cells was apparent at a concentration of 200 μM soya-phosphatidylcholines liposomes which was reversible by the addition of vitamin E. |
| Animal experiment [2]: | |
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Animal models |
Male Wistar albino rats (200-250 g) |
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Preparation Method |
Treatment of soya phosphatidylcholines (5 mg/kg/d and 10 mg/kg/d, i.p.) and dexamethasone (2.5 mg/kg/d, i.p.) were started from the 28th day of study till the end of the study in respective groups. At the end of the experiment, lung function parameters, total and differential leukocytes count in blood and BALf; inflammatory cytokines (IL-4, IL-5, and IL-13) and metabolic parameters (glucose, cholesterol, and triglyceride) in serum were measured in all the rats. Histopathological examination of lungs was performed in all rats. |
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Dosage form |
5 mg/kg/d and 10 mg/kg/d, i.p. |
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Applications |
The results displayed lung function parameters, total and differential leukocytes count in blood and BALf; inflammatory cytokines (IL-4, IL-5, and IL-13) and triglyceride shown significantly decreased, but serum glucose and cholesterol level has no change. |
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参考文献: [1]. Berrocal MC, et al. Vitamin E improves the uptake of unsaturated soya lecithin liposomes by human fibroblasts in vitro. J Microencapsul. 1998 May-Jun;15(3):347-59. [2]. Thakur VR, et al. An anti-asthmatic activity of natural Toll-like receptor-4 antagonist in OVA-LPS-induced asthmatic rats. Clin Exp Pharmacol Physiol. 2018 Nov;45(11):1187-1197. |
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