Mutactimycin,a new anthracycline antibiotic,consists of 5 components: mutac-timycin A,B,C,D and 7-deoxymutactimycinone A. Mutactimycin components differ from each other in suppressing proliferation and inducing differ...Mutactimycin,a new anthracycline antibiotic,consists of 5 components: mutac-timycin A,B,C,D and 7-deoxymutactimycinone A. Mutactimycin components differ from each other in suppressing proliferation and inducing differentiation of human erythroleukemia K-562 cells. Determined by benzidine staining, the percentage of K-562 cells with hemoglobin expression was86% by mutactimycin C. The peak percentage of benzidine positive cells appeared on day 5 or 6.The differentiated cells were partially reversed after drug removal.The induced cells lost the clonogenicity in soft-agar. The kinetics of differentiation induced by mutactimycin C, in comparison with other known anthracycline antibiotics,was similar to that by doxorubicin, epirubicin anddaunorubicin. Mutactimycin C was more active than aclarubicin A. The structure-activity relationship for mutactimycin components suggested that the substituting groups on C_3, C_11, and the saccharide on C_7 might be important for their activities.展开更多
OBJECTIVE: To explore the laws governing the distribution ofTraditional Chinese Medicine (TCM) syndrome elements (SEs) of senile diabetes (SD) and their relationship to relevant factors. METHODS: An investigation of p...OBJECTIVE: To explore the laws governing the distribution ofTraditional Chinese Medicine (TCM) syndrome elements (SEs) of senile diabetes (SD) and their relationship to relevant factors. METHODS: An investigation of patients who met the inclusion criteria was conducted by trained doctors, using case report forms. All related data were collected, including body mass index, glycated hemoglobin, illness course, complications, symptoms, and tongue and pulse manifestation. The SEs of each patient were judged by three qualified associate chief physicians independently. RESULTS: The main SEs of SD are Yin deficiency, Qi deficiency, blood stasis, and phlegm turbidity. Yindeficiency, Qi deficiency, blood stasis, and phlegm turbidity are most commonly seen among 4-SE combinations. Yang deficiency is typically related to illness course and BMI, phlegm turbidity to hypertension and hyperlipidemia, excessive heat to diabetic microangiopathy, and blood stasis to illness course and diabetic macroangiopathy. CONCLUSION: SD pathogenesis has a deficiency in origin and excess in superficiality. Deficiency syndrome mainly manifests as deficiency of both Qi and Yin, and concurrently in Yang deficiency. Excess syndrome is characterized by blood stasis and phlegm turbidity. SEs analysis provides a basis for the prevention and treatment of SD with TCM and lays the foundation for objectively evaluating multicentric clinical research for SD inTCM.展开更多
Cancer is still one of the important diseases that threatens the health of people. Multidrug resistance(MDR) is the main factor that leads to the failure of cancer chemotherapy. Thus, MDR diagnosis could facilitate th...Cancer is still one of the important diseases that threatens the health of people. Multidrug resistance(MDR) is the main factor that leads to the failure of cancer chemotherapy. Thus, MDR diagnosis could facilitate the monitoring of the therapy process and realization of efficient treatment of tumors. In this study, we have tried to use a new tetrathiafulvalene(TTF) derivative(TTF-(COONBu4)2) to sensitively recognize the MDR through the multi-signal responsive strategy. The relevant electrochemical and spectroscopic studies demonstrate the specific binding behavior of TTF-(COONBu4)2 with P-glycoprotein(P-gp) as well as drug-resistant leukemia cells. Especially due to the over-expression of specific components of P-gp on the plasma membranes of drug resistant cells, the electrochemical and hydrophilic/hydrophobic features of drug resistant-leukemia cells are apparently different from those of other kinds of leukemia cells. Meanwhile, Fourier transform infrared spectroscopic study illustrates that the most intense vibration band of TTF moieties in the 1400–1600 cm-1 range is almost smeared out upon binding to P-gp, and the binding of TTF-(COONBu4)2 to P-gp may also lead to changes in protein secondary structure and backbone. This observation may advance the development of the new TTF agent for the promising clinical diagnosis and monitoring of MDR of tumors with the aim of successful chemotherapy for human cancer.展开更多
文摘Mutactimycin,a new anthracycline antibiotic,consists of 5 components: mutac-timycin A,B,C,D and 7-deoxymutactimycinone A. Mutactimycin components differ from each other in suppressing proliferation and inducing differentiation of human erythroleukemia K-562 cells. Determined by benzidine staining, the percentage of K-562 cells with hemoglobin expression was86% by mutactimycin C. The peak percentage of benzidine positive cells appeared on day 5 or 6.The differentiated cells were partially reversed after drug removal.The induced cells lost the clonogenicity in soft-agar. The kinetics of differentiation induced by mutactimycin C, in comparison with other known anthracycline antibiotics,was similar to that by doxorubicin, epirubicin anddaunorubicin. Mutactimycin C was more active than aclarubicin A. The structure-activity relationship for mutactimycin components suggested that the substituting groups on C_3, C_11, and the saccharide on C_7 might be important for their activities.
基金Supported by The Special Scientific Research Program of State Administration of Traditional Chinese Medicine: Methodological Evaluation of Treating Type 2 Diabetes with Syndrome Differentiation Methods Based on Three Stages In TCM(No. 06-07LP42)
文摘OBJECTIVE: To explore the laws governing the distribution ofTraditional Chinese Medicine (TCM) syndrome elements (SEs) of senile diabetes (SD) and their relationship to relevant factors. METHODS: An investigation of patients who met the inclusion criteria was conducted by trained doctors, using case report forms. All related data were collected, including body mass index, glycated hemoglobin, illness course, complications, symptoms, and tongue and pulse manifestation. The SEs of each patient were judged by three qualified associate chief physicians independently. RESULTS: The main SEs of SD are Yin deficiency, Qi deficiency, blood stasis, and phlegm turbidity. Yindeficiency, Qi deficiency, blood stasis, and phlegm turbidity are most commonly seen among 4-SE combinations. Yang deficiency is typically related to illness course and BMI, phlegm turbidity to hypertension and hyperlipidemia, excessive heat to diabetic microangiopathy, and blood stasis to illness course and diabetic macroangiopathy. CONCLUSION: SD pathogenesis has a deficiency in origin and excess in superficiality. Deficiency syndrome mainly manifests as deficiency of both Qi and Yin, and concurrently in Yang deficiency. Excess syndrome is characterized by blood stasis and phlegm turbidity. SEs analysis provides a basis for the prevention and treatment of SD with TCM and lays the foundation for objectively evaluating multicentric clinical research for SD inTCM.
基金supported by the National Natural Science Foundation of China(81325011)the National High Technology Research&Development Program of China(2012AA022703)+1 种基金the National Basic Research Program of China(2010CB732404)the Major Science&Technology Project of Suzhou(ZXY2012028)
文摘Cancer is still one of the important diseases that threatens the health of people. Multidrug resistance(MDR) is the main factor that leads to the failure of cancer chemotherapy. Thus, MDR diagnosis could facilitate the monitoring of the therapy process and realization of efficient treatment of tumors. In this study, we have tried to use a new tetrathiafulvalene(TTF) derivative(TTF-(COONBu4)2) to sensitively recognize the MDR through the multi-signal responsive strategy. The relevant electrochemical and spectroscopic studies demonstrate the specific binding behavior of TTF-(COONBu4)2 with P-glycoprotein(P-gp) as well as drug-resistant leukemia cells. Especially due to the over-expression of specific components of P-gp on the plasma membranes of drug resistant cells, the electrochemical and hydrophilic/hydrophobic features of drug resistant-leukemia cells are apparently different from those of other kinds of leukemia cells. Meanwhile, Fourier transform infrared spectroscopic study illustrates that the most intense vibration band of TTF moieties in the 1400–1600 cm-1 range is almost smeared out upon binding to P-gp, and the binding of TTF-(COONBu4)2 to P-gp may also lead to changes in protein secondary structure and backbone. This observation may advance the development of the new TTF agent for the promising clinical diagnosis and monitoring of MDR of tumors with the aim of successful chemotherapy for human cancer.
