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Methods The main influencing factors of Doi-SF-NPs were investigated by single factor experiments, and Box-Behnken design-response surface methodology (BBD-RSM) was employed to optimize prescription process of Doi-SF-NPs. Doi-SF-NPs was characterized by transmission electron microscopy (TEM) and Fourier transform infrared spectroscopy (FT-IR). Drug release behavior of Doi-SF-NPs in phosphate buffer saline solution with different pH values was investigated. MTT method and Annexin V/PI double staining method were used to investigate the inhibitory and proapoptotic effects of Doi-SF-NPs on PC3 cells, respectively. The nude mouse of prostate cancer was established, compared the concentrations of diosgenin and Doi-SF-NPs in tumor tissues, and then evaluated the tumor targeting ability of Doi-SF-NPs using the relative uptake rate and ratio of peak concentration. The nude mouse model of prostate cancer was divided into model (normal saline) group, positive control (cisplatin, 2.0 mg/kg) group, diosgenin (10 mg/kg) group, low-dose Doi-SF-NPs (5 mg/kg) group and high-dose Doi-SF-NPs (10 mg/kg) group, the in vivo anti-tumor effects of Doi-SF-NPs was compared with diosgenin. Safety evaluation of Doi-SF-NPs was also performed. Results Optimal prescription process of Doi-SF-NPs nanoparticles as follows: The mass ratio of silk fibroin to diosgenin was 11.94:1, the volume ratio of the organic phase to aqueous phase was 5.99:1, and the preparation time was 2.75 h. Average envelopment efficiency, drug loading, particle size and ζ potential were (84.07 ± 0.70)%, (6.41 ± 0.05)%, (164.29 ± 4.43) nm and (−23.01 ± 1.17) mV, respectively. Diosgenin formed Doi-SF-NPs with silk fibroin through hydrogen bonding. The appearance of Doi-SF-NPs was spherical nanoparticles. Doi-SF-NPs existed higher cumulative release in phosphate buffer solution of pH 5.5 and 6.0, which demonstrated that Doi-SF-NPs had obvious pH-sensitivity. MTT method results showed that IC50 of diosgenin and Doi-SF-NPs on PC3 cells were 72.44 and 55.68 μmol/L, respectively. Doi-SF-NPs more effectively induced apoptosis of PC3 cells than that of diosgenin. The relative uptake rate of Doi-SF-NPs in in tumor tissue was 3.23, and the peak concentration ratio was 2.60, which demonstrating that Doi-SF-NPs could significantly increase the accumulation in tumor tissue. Doi-SF-NPs (10 mg/kg) increased the tumor inhibition rate of diosgenin (10 mg/kg) from 29.47% to 66.18%. Doi-SF-NPs did not affect the major organs of tumor-bearing nude mouse, which showed that the safety of Doi-SF-NPs was high. Conclusion Doi-SF-NPs could improve the tumor targeting of diosgenin and significantly enhanced anti-tumor efficacy. Therefore, Doi-SF-NPs had the potential to be developed into an antitumor drug., authors=DONG Yanan1 , REN Shuqiang2 , SHI Yan3 , DONG Jiaojiao4 , WANG Fengyun1 , authorsList=DONG Yanan, REN Shuqiang, SHI Yan, DONG Jiaojiao, WANG Fengyun, authorCompany=1 Henan Vocational College of Applied Technology, Zhengzhou 450042, China; 目的 制备薯蓣皂苷元丝素蛋白纳米粒（diosgenin silk fibroin nanoparticles，Doi-SF-NPs），并进行理化性质、肿瘤靶向性和体内抗肿瘤作用评价。方法 单因素考察Doi-SF-NPs主要影响因素，采用Box-Behnken设计-响应面法（Box-Behnken design-response surface methodology，BBD-RSM）优化Doi-SF-NPs处方工艺。使用透射电子显微镜（transmission electron microscopy，TEM）和傅里叶变换红外光谱（Fourier transform infrared spectroscopy，FT-IR）法进行表征。考察Doi-SF-NPs在不同pH值磷酸盐缓冲液（PBS）中的释药行为。采用MTT法和Annexin V/PI双染法考察Doi-SF-NPs对人前列腺癌PC3细胞的生长抑制及促凋亡作用。建立前列腺癌荷瘤裸鼠模型，比较薯蓣皂苷元原料药和Doi-SF-NPs在肿瘤组织中质量浓度，采用相对摄取率和峰浓度比值考察Doi-SF-NPs肿瘤靶向性。将前列腺癌荷瘤裸鼠分为模型（生理盐水）组、阳性对照（顺铂，2.0 mg/kg）组、薯蓣皂苷元原料药（10 mg/kg）组及Doi-SF-NPs低、高剂量（5、10 mg/kg）组，比较Doi-SF-NPs体内抗肿瘤效果。评价Doi-SF-NPs安全性。结果 Doi-SF-NPs最佳处方：丝素蛋白与薯蓣皂苷元质量比为11.94∶1，有机相与水相体积比为5.99∶1，制备时间为2.75 h。Doi-SF-NPs平均包封率、载药量、粒径和ζ电位分别（84.07±0.70）%、（6.41± 0.05）%、（164.29±4.43）nm和（-23.01±1.17）mV。薯蓣皂苷元与丝素蛋白通过氢键络合作用形成Doi-SF-NPs。Doi-SF-NPs外貌呈类圆形纳米颗粒。Doi-SF-NPs在pH 5.5、6.0 PBS中累积释放度较高，具有明显的pH值敏感性。薯蓣皂苷元原料药和Doi-SF-NPs对PC3细胞半数抑制浓度（median inhibition concentration，IC₅₀）分别为72.44、55.68 μmol/L。Doi-SF-NPs比薯蓣皂苷元原料药更有效地诱导了PC3细胞凋亡。Doi-SF-NPs在肿瘤组织内相对摄取率为3.23，峰浓度比值为2.60，证明Doi-SF-NPs能明显增加肿瘤组织的蓄积量。Doi-SF-NPs（10 mg/kg）将薯蓣皂苷元原料药（10 mg/kg）抑瘤率由29.47%提高至66.18%。Doi-SF-NPs未对荷瘤裸鼠主要脏器产生影响，使用安全性高。结论 Doi-SF-NPs可提高薯蓣皂苷元肿瘤靶向性，显著提高了抗肿瘤药效，有望开发成抗肿瘤药物。, authors=董亚楠1 , 任书强2 , 石岩3 , 董娇娇4 , 王风云1 , authorsList=董亚楠, 任书强, 石岩, 董娇娇, 王风云, authorCompany=1 河南应用技术职业学院, 河南 郑州 450042; p -PDHA1轴影响谷氨酰胺代谢介导的前列腺癌研究[J]. 中草药, 2025, 56(4): 1254-1265.et al . Effect of diosgenin in suppressing viability and promoting apoptosis of human prostate cancer cells: An interplay with the G protein-coupled oestrogen receptor? [J]. Int J Mol Sci , 2024, 25(22): 12006.et al . pH-sensitive silk fibroin nanoparticles encapsulating β-hydroxyisovalerylshikonin for targeted pancreatic cancer therapy [J]. Curr Drug Deliv , 2025, 22(10): 1469-1480.J Polym Environ , 2026, 34(4): 92.et al . Supercritical fluid-assisted fabrication of indocyanine green-encapsulated silk fibroin nanoparticles for dual-triggered cancer therapy [J]. ACS Biomater Sci Eng , 2018, 4(10): 3487-3497.2 的合成、表征及其抗肿瘤性能[J]. 化学试剂, 2024, 46(10): 7-13.
中草药
|药剂与工艺
2026
, 57
(19) :
7587
-7601
薯蓣皂苷元丝素蛋白纳米粒的制备、表征及其对前列腺癌荷瘤裸鼠肿瘤的抑制作用
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董亚楠1 , 任书强2 , 石岩3 , 董娇娇4 , 王风云1
作者信息
1 河南应用技术职业学院, 河南 郑州 450042;
作者简介:
董亚楠: 董亚楠（1987—），女，硕士，副教授，研究方向为临床药学及基础医学。Tel:(0371)67592759 E-mail:dyn11212020@126.com
Preparation and characterization of diosgenin silk fibroin nanoparticles and their inhibitory effects on tumors in prostate cancer-bearing nude mice
DONG Yanan1 , REN Shuqiang2 , SHI Yan3 , DONG Jiaojiao4 , WANG Fengyun1
Affiliations
1 Henan Vocational College of Applied Technology, Zhengzhou 450042, China;
doi: 10.7501j.issn.0253-2670.2026.19.009
文章导航
目的 制备薯蓣皂苷元丝素蛋白纳米粒（diosgenin silk fibroin nanoparticles，Doi-SF-NPs），并进行理化性质、肿瘤靶向性和体内抗肿瘤作用评价。方法 单因素考察Doi-SF-NPs主要影响因素，采用Box-Behnken设计-响应面法（Box-Behnken design-response surface methodology，BBD-RSM）优化Doi-SF-NPs处方工艺。使用透射电子显微镜（transmission electron microscopy，TEM）和傅里叶变换红外光谱（Fourier transform infrared spectroscopy，FT-IR）法进行表征。考察Doi-SF-NPs在不同pH值磷酸盐缓冲液（PBS）中的释药行为。采用MTT法和Annexin V/PI双染法考察Doi-SF-NPs对人前列腺癌PC3细胞的生长抑制及促凋亡作用。建立前列腺癌荷瘤裸鼠模型，比较薯蓣皂苷元原料药和Doi-SF-NPs在肿瘤组织中质量浓度，采用相对摄取率和峰浓度比值考察Doi-SF-NPs肿瘤靶向性。将前列腺癌荷瘤裸鼠分为模型（生理盐水）组、阳性对照（顺铂，2.0 mg/kg）组、薯蓣皂苷元原料药（10 mg/kg）组及Doi-SF-NPs低、高剂量（5、10 mg/kg）组，比较Doi-SF-NPs体内抗肿瘤效果。评价Doi-SF-NPs安全性。结果 Doi-SF-NPs最佳处方：丝素蛋白与薯蓣皂苷元质量比为11.94∶1，有机相与水相体积比为5.99∶1，制备时间为2.75 h。Doi-SF-NPs平均包封率、载药量、粒径和ζ电位分别（84.07±0.70）%、（6.41± 0.05）%、（164.29±4.43）nm和（-23.01±1.17）mV。薯蓣皂苷元与丝素蛋白通过氢键络合作用形成Doi-SF-NPs。Doi-SF-NPs外貌呈类圆形纳米颗粒。Doi-SF-NPs在pH 5.5、6.0 PBS中累积释放度较高，具有明显的pH值敏感性。薯蓣皂苷元原料药和Doi-SF-NPs对PC3细胞半数抑制浓度（median inhibition concentration，IC₅₀）分别为72.44、55.68 μmol/L。Doi-SF-NPs比薯蓣皂苷元原料药更有效地诱导了PC3细胞凋亡。Doi-SF-NPs在肿瘤组织内相对摄取率为3.23，峰浓度比值为2.60，证明Doi-SF-NPs能明显增加肿瘤组织的蓄积量。Doi-SF-NPs（10 mg/kg）将薯蓣皂苷元原料药（10 mg/kg）抑瘤率由29.47%提高至66.18%。Doi-SF-NPs未对荷瘤裸鼠主要脏器产生影响，使用安全性高。结论 Doi-SF-NPs可提高薯蓣皂苷元肿瘤靶向性，显著提高了抗肿瘤药效，有望开发成抗肿瘤药物。
薯蓣皂苷元
/
丝素蛋白
/
纳米粒
/
Box-Behnken设计-响应面法
/
前列腺癌
/
肿瘤靶向
/
抗肿瘤
/
安全性评价
Objective To prepare diosgenin silk fibroin nanoparticles (Doi-SF-NPs) and evaluate their physicochemical properties, tumor targeting and in vivo anti-tumor effects . Methods The main influencing factors of Doi-SF-NPs were investigated by single factor experiments, and Box-Behnken design-response surface methodology (BBD-RSM) was employed to optimize prescription process of Doi-SF-NPs. Doi-SF-NPs was characterized by transmission electron microscopy (TEM) and Fourier transform infrared spectroscopy (FT-IR). Drug release behavior of Doi-SF-NPs in phosphate buffer saline solution with different pH values was investigated. MTT method and Annexin V/PI double staining method were used to investigate the inhibitory and proapoptotic effects of Doi-SF-NPs on PC3 cells, respectively. The nude mouse of prostate cancer was established, compared the concentrations of diosgenin and Doi-SF-NPs in tumor tissues, and then evaluated the tumor targeting ability of Doi-SF-NPs using the relative uptake rate and ratio of peak concentration. The nude mouse model of prostate cancer was divided into model (normal saline) group, positive control (cisplatin, 2.0 mg/kg) group, diosgenin (10 mg/kg) group, low-dose Doi-SF-NPs (5 mg/kg) group and high-dose Doi-SF-NPs (10 mg/kg) group, the in vivo anti-tumor effects of Doi-SF-NPs was compared with diosgenin. Safety evaluation of Doi-SF-NPs was also performed. Results Optimal prescription process of Doi-SF-NPs nanoparticles as follows: The mass ratio of silk fibroin to diosgenin was 11.94:1, the volume ratio of the organic phase to aqueous phase was 5.99:1, and the preparation time was 2.75 h. Average envelopment efficiency, drug loading, particle size and ζ potential were (84.07 ± 0.70)%, (6.41 ± 0.05)%, (164.29 ± 4.43) nm and (−23.01 ± 1.17) mV, respectively. Diosgenin formed Doi-SF-NPs with silk fibroin through hydrogen bonding. The appearance of Doi-SF-NPs was spherical nanoparticles. Doi-SF-NPs existed higher cumulative release in phosphate buffer solution of pH 5.5 and 6.0, which demonstrated that Doi-SF-NPs had obvious pH-sensitivity. MTT method results showed that IC50 of diosgenin and Doi-SF-NPs on PC3 cells were 72.44 and 55.68 μmol/L, respectively. Doi-SF-NPs more effectively induced apoptosis of PC3 cells than that of diosgenin. The relative uptake rate of Doi-SF-NPs in in tumor tissue was 3.23, and the peak concentration ratio was 2.60, which demonstrating that Doi-SF-NPs could significantly increase the accumulation in tumor tissue. Doi-SF-NPs (10 mg/kg) increased the tumor inhibition rate of diosgenin (10 mg/kg) from 29.47% to 66.18%. Doi-SF-NPs did not affect the major organs of tumor-bearing nude mouse, which showed that the safety of Doi-SF-NPs was high. Conclusion Doi-SF-NPs could improve the tumor targeting of diosgenin and significantly enhanced anti-tumor efficacy. Therefore, Doi-SF-NPs had the potential to be developed into an antitumor drug.
diosgenin
/
silk fibroin
/
nanoparticles
/
Box-Behnken design-response surface methodology
/
prostate cancer
/
tumor targeting
/
anti-tumor
/
safety evaluation
董亚楠, 任书强, 石岩, 董娇娇, 王风云.
薯蓣皂苷元丝素蛋白纳米粒的制备、表征及其对前列腺癌荷瘤裸鼠肿瘤的抑制作用.
中草药,
2026
, 57
(19)
: 7587
-7601
.
DOI: 10.7501j.issn.0253-2670.2026.19.009
DONG Yanan, REN Shuqiang, SHI Yan, DONG Jiaojiao, WANG Fengyun.
Preparation and characterization of diosgenin silk fibroin nanoparticles and their inhibitory effects on tumors in prostate cancer-bearing nude mice[J].
Chinese Traditional and Herbal Drugs ,
2026
, 57
(19)
: 7587
-7601
.
DOI: 10.7501j.issn.0253-2670.2026.19.009
2025年度河南省高等学校重点科研项目 (25B310010); 2024年度河南应用技术职业学院校级科研课题 (2024-KJ-69); 2025年度河南省科技攻关课题 (252102310468); 2026年度河南省科技攻关课题 (262102310551)
参考文献
引证文献
郑倩倩, 陈璐瑶, 汪涛. 中药有效成分防治前列腺癌的研究进展[J]. 西部中医药, 2024, 37(7): 83-87.p -PDHA1轴影响谷氨酰胺代谢介导的前列腺癌研究[J]. 中草药, 2025, 56(4): 1254-1265.et al . Effect of diosgenin in suppressing viability and promoting apoptosis of human prostate cancer cells: An interplay with the G protein-coupled oestrogen receptor? [J]. Int J Mol Sci , 2024, 25(22): 12006.et al . pH-sensitive silk fibroin nanoparticles encapsulating β-hydroxyisovalerylshikonin for targeted pancreatic cancer therapy [J]. Curr Drug Deliv , 2025, 22(10): 1469-1480.J Polym Environ , 2026, 34(4): 92.et al . Supercritical fluid-assisted fabrication of indocyanine green-encapsulated silk fibroin nanoparticles for dual-triggered cancer therapy [J]. ACS Biomater Sci Eng , 2018, 4(10): 3487-3497.2 的合成、表征及其抗肿瘤性能[J]. 化学试剂, 2024, 46(10): 7-13.
2026年第57卷第19期
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doi: 10.7501j.issn.0253-2670.2026.19.009
接收时间：2026-04-23
首发时间：2026-10-29
https://castjournals.cast.org.cn/joweb/zcy/CN/10.7501j.issn.0253-2670.2026.19.009
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2种不同金属材料的力学参数
科 属数 种数 占总种数比例 属 种数 占总种数比例 鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78 小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39 多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39 红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87 小菇属 Mycena 11 5.26 光柄菇属 Pluteus 5 2.39 红菇属 Russula 17 8.13 栓菌属 Trametes 5 2.39
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