Breast cancer is one of the most common cancers and the leading cause of cancer-related deaths among women due to the diagnostic delay and failure of treatment.1 Despite the significant progress made in developing the...Breast cancer is one of the most common cancers and the leading cause of cancer-related deaths among women due to the diagnostic delay and failure of treatment.1 Despite the significant progress made in developing therapeutic strategies for breast cancer,effective treatment of breast cancer,particularly aggressive triple-negative breast cancer,remains lacking.Angiogenesis is a crucial risk factor for breast cancer metastasis and a predictor of poor prognosis.Thus,developing novel agents capable of suppressing tumor angiogenesis offers a promising approach for breast cancer treatment.Oridonin,the major active ingredient of the traditional Chinese medicinal herb,exhibits anti-cancer activity by inhibiting tumor-induced angiogenesis.2 Nevertheless,the therapeutic potential of oridonin is limited due to its rapid plasma clearance and limited potency.Various novel oridonin analogues have been designed and chemically synthesized by modifying their A,B,and D rings to achieve an agent with better anti-cancer efficacy and lower toxicity than oridonin.3 Chick embryo chorioallantoic membrane(CAM)and yolk sac membrane(YSM)models were commonly utilized to study tumor-induced angiogenesis.To discover the promising anti-angiogenic agents,we screened novel oridonin analogues synthesized in-house using the CAM and YSM models.展开更多
β-Cyclodextrin( β-CyD) is cyclic oligosaccharide of a glucopyranose, containing a relatively hydrophobic central cavity and hydrophilic outer surface. However, the usefulness of β-CyD is limited owing to its low aq...β-Cyclodextrin( β-CyD) is cyclic oligosaccharide of a glucopyranose, containing a relatively hydrophobic central cavity and hydrophilic outer surface. However, the usefulness of β-CyD is limited owing to its low aqueous solubility whereas we found that its apparent high solubility was evident in some injectable solvents including 2-pyrrolidone(PYR), Nmethyl pyrrolidone(NMP) and dimethyl sulfoxide(DMSO). Therefore, in the present study, the physicochemical properties of the 30–60% w/w β-CyD in PYR, NMP and DMSO were investigated such as viscosity, water resistant, matrix formation rate and syringeability. The higher the concentration of β-CyD resulted in the increased viscosity and the higher force and energy of syringeability. β-CyD in PYR gave the highest viscosity which contributed to the lowest syringeability while β-CyD in DMSO exhibited the highest syringeability. The β-CyD in DMSO and NMP exhibited the higher rate of matrix formation. β-CyD in PYR showed the highest water resistant for phase separation while β-CyD in NMP gave the faster de-mixing rate compared to that from PYR. The difference in physicochemical properties of β-CyD dried ppts studied by scanning electron microscope(SEM), differential scanning calorimetry(DSC), X-ray diffraction(XRD), Fourier-transform infrared spectroscopy(FT-IR) and thermogravimetric analysis(TGA) revealed that there was partial complexation of β-CyD with respective solvents. Both solution and precipitate characteristic properties will be useful for using β-CyD in further investigation as matrix material dissolved in the injectable vehicles as the in situ forming gel for periodontitis treatment.展开更多
基金supported by the Basic and Applied Basic Research Project of Guangdong Province,China(No.2023A1515010459 to C.L.Q.)Key Team of Basic and Clinical Research on Tumor Immunotherapy of Guangdong Pharmaceutical University(No.2024ZZ10 to X.L.)+2 种基金the Project of Administration of Traditional Chinese Medicine of Guangdong Province,China(No.20251209 to C.L.Q.20242048 to P.T.)Dr.Jia Zhou has no connections with the above-mentioned funding resources in China,and is partly supported by the John D.Stobo,M.D.Distinguished Chair Endowment Fund,and Edith&Robert Zinn Chair in Drug Discovery Endowment Fund at the University of Texas Medical Branch in the United States.
文摘Breast cancer is one of the most common cancers and the leading cause of cancer-related deaths among women due to the diagnostic delay and failure of treatment.1 Despite the significant progress made in developing therapeutic strategies for breast cancer,effective treatment of breast cancer,particularly aggressive triple-negative breast cancer,remains lacking.Angiogenesis is a crucial risk factor for breast cancer metastasis and a predictor of poor prognosis.Thus,developing novel agents capable of suppressing tumor angiogenesis offers a promising approach for breast cancer treatment.Oridonin,the major active ingredient of the traditional Chinese medicinal herb,exhibits anti-cancer activity by inhibiting tumor-induced angiogenesis.2 Nevertheless,the therapeutic potential of oridonin is limited due to its rapid plasma clearance and limited potency.Various novel oridonin analogues have been designed and chemically synthesized by modifying their A,B,and D rings to achieve an agent with better anti-cancer efficacy and lower toxicity than oridonin.3 Chick embryo chorioallantoic membrane(CAM)and yolk sac membrane(YSM)models were commonly utilized to study tumor-induced angiogenesis.To discover the promising anti-angiogenic agents,we screened novel oridonin analogues synthesized in-house using the CAM and YSM models.
文摘β-Cyclodextrin( β-CyD) is cyclic oligosaccharide of a glucopyranose, containing a relatively hydrophobic central cavity and hydrophilic outer surface. However, the usefulness of β-CyD is limited owing to its low aqueous solubility whereas we found that its apparent high solubility was evident in some injectable solvents including 2-pyrrolidone(PYR), Nmethyl pyrrolidone(NMP) and dimethyl sulfoxide(DMSO). Therefore, in the present study, the physicochemical properties of the 30–60% w/w β-CyD in PYR, NMP and DMSO were investigated such as viscosity, water resistant, matrix formation rate and syringeability. The higher the concentration of β-CyD resulted in the increased viscosity and the higher force and energy of syringeability. β-CyD in PYR gave the highest viscosity which contributed to the lowest syringeability while β-CyD in DMSO exhibited the highest syringeability. The β-CyD in DMSO and NMP exhibited the higher rate of matrix formation. β-CyD in PYR showed the highest water resistant for phase separation while β-CyD in NMP gave the faster de-mixing rate compared to that from PYR. The difference in physicochemical properties of β-CyD dried ppts studied by scanning electron microscope(SEM), differential scanning calorimetry(DSC), X-ray diffraction(XRD), Fourier-transform infrared spectroscopy(FT-IR) and thermogravimetric analysis(TGA) revealed that there was partial complexation of β-CyD with respective solvents. Both solution and precipitate characteristic properties will be useful for using β-CyD in further investigation as matrix material dissolved in the injectable vehicles as the in situ forming gel for periodontitis treatment.
