Lignans-rich extract from Herpetospermum caudigerum alleviate physical fatigue in mice / 中国结合医学杂志

<p><b>OBJECTIVE</b>To ascertain anti-fatigue constituents and mechanisms of Herpetospermum caudigerum.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>Compared with the control group, the lignans extract (ethyl acetate fraction) of Herpetospermum caudigerum and HPE could signifificantly 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.</p><p><b>CONCLUSIONS</b>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.</p>

Experimental study on herpetrione nanosuspension against hepatitis B virus in Vitro and in Vivo / 中国药学杂志

OBJECTIVE: To evaluate the anti-hepatitis B virus (HBV) activity of herpetrione nanosuspension (PEDX-NS) both in vitro and in vivo. METHODS: HepG2 2.2.15 cells and duck hepatitis B virus (DHBV) infected ducks as in vitro and in vivo models were used to compare the anti-HBV activity of PEDX-NS and PEDX coarse suspension (PEDX-CS). RESULTS: In the HepG2 2.2.15 cell, PEDX-NS effectively suppressed the secretion of the HBV antigens (HBsAg and HBeAg) in a dose-dependent manner with significant difference from PEDX-CS (P<0.05 or P<0.01). In the in vivo evaluation, PEDX-NS with high dose (100 mg·kg-1) and middle dose (60 mg·kg-1) significantly reduced the serum HBV DNA level (P<0.05 or P<0.01) and the effect was better than that of PEDX-CS (P<0.05 or P<0.01). CONCLUSION: The result revealed that PEDX-NS exhibits anti-HBV activity both in vitro and in vivo and its effect was superior to that of PEDX-CS. The mechanism is probably that the small particle size of PEDX-NS provides a large specific surface area that resulted in better absorption in vivo, thus enhancing its anti-HBV activity.

Preparation of herpetrione nanosuspensions and preliminary study on its pharmacokinetics / 中国药学杂志

OBJECTIVE: To prepare herpetrione nanosuspension (PEDX-NS) and evaluate its pharmacokinetics in rats. METHODS: PEDX-NS was prepared by high pressure homogenization technology, and its morphology and mean diameter were determined. An HPLC method was employed to determine the concentration of herpetrione(PEDX), the index component of PEDX-NS, in plasma, and the bioavailability of the nanosuspension was compared with the reference formulation after oral administration in Wistar rats. RESULTS: The particles in the nanosuspension observed by scanning electron microscopy were irregular spheres, and the mean particle size of PEDX-NS was (238.6 ± 1.9)nm. Its pharmacokinetic process calculated with DAS2.0 software was fitted to a two-compartment model. The AUG was 25.19 μg · h · mL-1 and the pmax was 11.64 μg · mL-1, which were 2.47 and 2.63 times of the reference formulation, respectively (P < 0.01). CONCLUSION: It is feasible to prepare PEDX-NS by high pressure homogenization technology, and PEDX-NS can improve the bioavailability of PEDX notablely.