Department of Chemical Engineering, College of Engineering, Northeastern University, Boston, MA 02115, USA.
Department of Agronomy and Plant Breeding, Faculty of Engineering and Agriculture, Science and Research Branch, IA University, Tehran, Iran.
Int J Nanomedicine. 2020 Apr 28;15:2935-2945. doi: 10.2147/IJN.S223796. eCollection 2020.
New anticancer agents that rely on natural/healthy, not synthetic/toxic, components are very much needed.
Ricinoleyl hydroxamic acid (RHA) was synthesized from castor oil and hydroxylamine using Lipozyme TL IM as a catalyst. To optimize the conversion, the effects of the following parameters were investigated: type of organic solvent, period of reaction, amount of enzyme, the molar ratio of reactants and temperature. The highest conversion was obtained when the reaction was carried out under the following conditions: hexane as a solvent; reaction period of 48 hours; 120 mg of Lipozyme TL IM/3 mmol oil; HA-oil ratio of 19 mmol HA/3 mmol oil; and temperature of 40°C. The cytotoxicity of the synthesized RHA was assessed using human dermal fibroblasts (HDF), and its application towards fighting cancer was assessed using melanoma and glioblastoma cancer cells over a duration of 24 and 48 hours.
RHA was successfully synthesized and it demonstrated strong anticancer activity against glioblastoma and melanoma cells at as low as a 1 µg/mL concentration while it did not demonstrate any toxicity against HDF cells.
This is the first report on the synthesis of RHA with great potential to be used as a new anticancer agent.
非常需要新的抗癌药物，这些药物依赖于天然/健康的、非合成/有毒的成分。
蓖麻油和羟胺用脂肪酶 TL IM 作为催化剂合成了蓖麻醇酰羟胺（RHA）。为了优化转化率，考察了以下参数的影响：有机溶剂的种类、反应时间、酶的用量、反应物的摩尔比和温度。当反应在以下条件下进行时，得到了最高的转化率：己烷作为溶剂；反应时间为 48 小时；120mg 脂肪酶 TL IM/3mmol 油；HA-油摩尔比为 19mmolHA/3mmol 油；温度为 40°C。用人真皮成纤维细胞（HDF）评估了合成的 RHA 的细胞毒性，并在 24 和 48 小时的时间内用黑色素瘤和神经胶质瘤癌细胞评估了其抗癌应用。
成功合成了 RHA，它在低至 1μg/ml 的浓度下对神经胶质瘤和黑色素瘤细胞表现出很强的抗癌活性，而对 HDF 细胞没有显示出任何毒性。
这是首次报道用具有很大潜力的 RHA 作为一种新的抗癌药物进行合成。
