Lei Yang,Zhenghai Zhang,Jian Hou,Xin Jin,Zhongcheng Ke,Dan Liu,Mei Du,Xiaobing Jia,Huixia Lv
Ginsenoside compound K (CK) is one of the effective ingredients in antitumor composition of ginsenoside. However, the poor water solubility and significant efflux have limited the widespread clinical use of CK. In this study, preparation of novel CK-loaded d -alpha-tocopheryl polyethylene glycol 1,000 succinate/poly(ethylene glycol)-poly(ε-caprolactone) mixed micelles (CK-M) is discussed to solve the above problems. Particle size, zeta potential, and morphology were characterized using dynamic light scattering and transmission electron microscopy. CK-M are spherical shaped with an average particle size of 53.07±1.31 nm with high drug loading of 11.19%±0.87% and entrapment efficiency of 94.60%±1.45%. Water solubility of CK was improved to 3.78±0.09 mg/mL, which was ~107.35 times higher than free CK. A549 and PC-9 cells were used to evaluate in vitro cytotoxicity and cellular uptake. IC 50 values of CK-M in A549 and PC-9 cells (24 h) were 25.43±2.18 and 18.35±1.90 μg/mL, respectively. Enhanced cellular uptake of CK-M was observed in both cells. Moreover, CK-M promoted tumor cell apoptosis, inhibited tumor cell invasion, metastasis, and efflux through regulation of Bax, Bcl-2, matrix metalloproteinase-2, Caspase-3, and P-glycoprotein. In vivo imaging indicated that CK-M has excellent tumor targeting effect within 24 h, and the relative tumor inhibition rate of CK-M was 52.04%±4.62% compared with control group ( P <0.01). Thus, CK-M could be an appropriate delivery agent for enhanced solubility and antitumor effect of CK.
Mingyue Zhao,Xin Liu,Yuzhu Hou,Tongtong Yang,Jiaquan Xu,Rui Su
The levels of l-arginine and asymmetric dimethylarginine (ADMA) and the amount of the nitric oxide (NO) production have recently been linked to breast cancer and pharmaceutical effect evaluation. Herein, a method combining electrochemistry and high-resolution mass spectrometry (HRMS) was established and used to study NO metabolism and its modulation by ginsenoside compound K (CK) in breast cancer cells. Platinum nanoparticles-decorated fluorine tin oxide was employed as an electrochemical sensor for in situ detection of NO release, while HRMS was used for the analysis of the NO-related metabolites. Through the combination of the electrochemical and HRMS results, decreases in arginine and NO and increases in ADMA and ornithine were observed after modulation by CK, and two highly correlated metabolic pathways including arginine and proline metabolism and vascular smooth muscle contraction were found. This method offers a new strategy for fast evaluation of pharmaceutical efficacy based on NO metabolism.
Chinese herb hydrogel has outstanding values in wound treatment. Tremendous effort is dedicated to developing functional and intelligent Chinese herb hydrogels for accelerating healing process. Herein, a novel multifunctional bilayer Chinese herb hydrogel patch for wound healing is presented. The patches are composed of a Ginsenoside compound K (GCK)-integrated chitosan inverse opal scaffold layer and a Bletilla striata polysaccharide (BP) hydrogel filler layer. As the photothermal conversion capacity of BP can trigger faster degradation of its hydrogel layer under near-infrared (NIR) light, the encapsulated BP can be controllably released to wound area and exhibit photothermal antibacterial and antioxidant effects. Besides, the inverse opal scaffold layer shows great mechanical property and moisturizing performance, and its released GCK can promote angiogenesis for long term therapeutic effects. Attractively, due to responsive structural color, the patch is endowed with self-reporting performance, which can real-time visually monitor the drug release degree. Taking advantages of these properties, the patches have been demonstrated to achieve satisfying therapeutic effects for in vivo wound treatment. Therefore, we believe that the proposed Chinese herb hydrogel patches are valuable as multifunctional patches for clinical treatment.
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