超高效液相色谱法测定波棱瓜子中Herpetrione的含量

目的用超高效液相色谱法测定波棱瓜子中Herpetrione的含量。方法采用Waters ACQUITY UPLC BEHC18色谱柱(2.1 mm×50 mm,1.7μm),流动相为乙腈-0.1%磷酸溶液(21∶79),流速为0.5 ml/min,柱温:30℃,检测波长:240 nm。结果 Herpetrione在0.0095～0.1520μg范围内线性关系良好,其回归方程为:Y=2.68×106X-278.98,r=0.9999;平均回收率为99.57%,RSD为1.15%。结论该方法操作简单,准确性和重复性好,建立了波棱瓜子的一种快速准确的含量检测方法。

Herpetrione纳米混悬剂的制备及药动学初步研究

目的本实验制备了herpetrione纳米混悬剂(PEDX-NS),并进行了大鼠体内药动学研究。方法采用高压均质法制备herpetrione纳米混悬剂,考察纳米混悬剂的形态及粒径分布。以herpetrione(PEDX)为指标成分,采用HPLC测定大鼠灌胃给药后的血药浓度,用DAS2.0药动学软件计算药动学参数。结果制得的纳米混悬剂呈不规则球形,平均粒径为(238.6±1.9)nm,多分散度指数为(0.183±0.017)。herpetrione在大鼠体内动力学行为符合二室模型。herpetrione纳米混悬剂药-时曲线下面积(AUC)为25.19μg.h.mL-1,达峰浓度(ρmax)为11.64μg.mL-1,与参比药herpetrione普通混悬剂(PEDX-S)相比,分别提高了2.47倍和2.63倍(P<0.01)。结论高压均质法制备herpetrione纳米混悬剂工艺简单可行,herpetrione纳米混悬剂能显著提高药物体内生物利用度。

Insight into the in vivo fate of intravenous herpetrione amorphous nanosuspensions by aggregation-caused quenching probes

Intravenous nanosuspensions are attracted growing attention as a viable strategy for development of intravenous formulations of poorly water-soluble drugs.However,only few information about the biological fate of intravenous nanosuspensions is currently known,especially amorphous nanosuspensions are not reported yet.In this study,the in vivo fate of herpetrione(HPE)amorphous nanosuspensions following intravenous administration was explored by using an aggregation-caused quenching(ACQ)probe and HPLC methods.The ACQ probe is physically embedded into HPE nanoparticles via anti-solvent method to form HPE hybrid nanosuspensions(HPE-HNSs)for bioimaging.HPE-HNSs emit strong and stable fluorescence,but fluorescence quenches immediately upon the dissolution of HPE-HNSs,confirming the selfdiscrimination of HPE-HNSs.Following intravenous administration of HPE-HNSs,integral HPE-HNSs and HPE show similar degradation and biodistribution,with rapid clearance from blood circulation and obvious accumulation in liver and lung.Due to the slower dissolution and enhanced recognition by reticuloendothelial system,450 nm HPE-HNSs accumulate more in liver,lung and spleen than that of 200 nm HPE-HNSs.These results demonstrate that integral HPE-HNSs determine the in vivo performance of HPEHNSs.This study provides insight into the in vivo fate of intravenous amorphous nanosuspensions.

Formation mechanism of herpetrione self-assembled nanoparticles based on p H-driven method

The self-assembled nanoparticles(SAN)formed during the decoction process of traditional Chinese medicine(TCM)exhibit non-uniform particle sizes and a tendency for aggregation.Our group found that the p H-driven method can improve the self-assembly phenomenon of Herpetospermum caudigerum Wall.,and the SAN exhibited uniform particle size and demonstrated good stability.In this paper,we analyzed the interactions between the main active compound,herpetrione(Her),and its main carrier,Herpetospermum caudigerum Wall.polysaccharide(HCWP),along with their self-assembly mechanisms under different p H values.The binding constants of Her and HCWP increase with rising p H,leading to the formation of Her-HCWP SAN with a smaller particle size,higher zeta potential,and improved thermal stability.While the contributions of hydrogen bonding and electrostatic attraction to the formation of Her-HCWP SAN increase with rising p H,the hydrophobic force consistently plays a dominant role.This study enhances our scientific understanding of the self-assembly phenomenon of TCM improved by p H driven method.

Lignans-Rich Extract from Herpetospermum caudigerum Alleviate Physical Fatigue in Mice

Objective: To ascertain anti-fatigue constituents and mechanisms of Herpetospermum caudigerum. Methods: The 80% ethanol extracts of Herpetospermum caudigerum were partitioned with chloroform, ethyl acetate and n-butanol, respectively. Male Kunming mice were divided into 13 groups with 16 mice in each group: a control group fed with water, 9 groups treated with 3 fractions of Herpetospermum caudigerum(chloroform fraction, ethyl acetate fraction and n-butanol fraction) at dose of 80, 160 and 320 mg/kg for the low-dose group, medium-dose group and high-dose group, 3 herpetrione(HPE) treated groups fed with HPE at dose of 15, 30, and 60 mg/kg for the low-dose group, medium-dose group and high-dose group. All animals were treated once per day for 30 days. Anti-fatigue activity was assessed through the forced swimming test and serum biochemical parameters including blood lactic acid(BLA), blood urea nitrogen(BUN), malondialdehyde(MDA), hepatic glycogen(HG), lactic dehydrogenase(LDH), superoxide dismutase(SOD) and glutathione peroxidase(GPx) determined following the recommended procedures provided by the commercial kits. Results: Compared with the control group, the lignans extract(ethyl acetate fraction) of Herpetospermum caudigerum and HPE could significantly prolonged the exhaustive swimming time(P<0.05 or P<0.01), and also increased the HG levels(P<0.05 or P<0.01) and the activities of antioxidant enzymes(SOD, GPx and LDH, P<0.05 or P<0.01); BLA and MDA levels were decreased considerably in lignans extract and HPE treated groups(P<0.05 or P<0.01). HPE also could significantly decrease the BUN contents compared with the control group(P<0.05). The chloroform and n-butanol fraction showed no effect on swimming time and biochemical parameters. Conclusions: The lignans extract had antifatigue activities and HPE may be partly responsible for the anti-fatigue effects of Herpetospermum caudigerum. The possible mechanisms of anti-fatigue activity were related to the decrease of BUN and BLA, the increase of the HG storage and protecting corpuscular membrane by preventing lipid oxidation via modifying several enzyme activities.