lignans and herpetrione

The present study was designed to improve storage stability and oral bioavailability of Ganneng dropping pills (GNDP) by transforming lignans of Herpetospermum caudigerum (HL) composed of herpetrione (HPE) and herpetin (HPN) into nanosuspension (HL-NS), the main active ingredient of GNDP, HL-NS was prepared by high pressure homogenization and lyophilized to transform into solid nanoparticles (HL nanoparticles), and then the formulated HL nanoparticles were perfused into matrix to obtain NS-GNDP by melting method. For a period of 3 months, the content uniformity, storage stability and pharmacokinetics test in vivo of NS-GNDP were evaluated and compared with regular GNDP at room temperature. The results demonstrated that uniformity of dosage units of NS-GNDP was acceptable according to the criteria of Chinese Pharmacopoeia 2015J. Physical stability of NS-GNDP was investigated systemically using photon correlation spectroscopy (PCS), zeta potential measurement, and scanning electron microscopy (SEM). There was a slight increase in particles and PI of HL-NS re-dispersed from NS-GNDP after storage for 3 months, compared with new formulated NS-GNDP, which indicated a good redispersibility of the NS-GNDP containing HL-NS after storage. Besides, chemical stability of NS-GNDP was studied and the results revealed that HPE and HPN degradation was less when compared with that of GNDP, providing more than 99% of drug residue after storage for 3 months. In the dissolution test in vitro, NS-GNDP remarkably exhibited an increased dissolution velocity compared with GNDP and no distinct dissolution difference existed within 3 months. The pharmacokinetic study showed that HPE and HPN in NS-GNDP exhibited a significant increase in AUC

Topics: Animals; Benzofurans; Biological Availability; Cucurbitaceae; Drug Carriers; Drug Compounding; Drug Stability; Freeze Drying; Furans; Humans; Lignans; Male; Nanoparticles; Particle Size; Plant Extracts; Rats; Rats, Sprague-Dawley; Solubility

Herpetospermum caudigerum (HCD) is traditionally used for the treatment of liver diseases, cholic diseases, and dyspepsia as a well-known Tibetan medicine in China. The present study was designed to investigate the hepatoprotective effect of HCD and ascertain its active ingredients and possible mechanism.. Mice were orally administrated with different parts (seeds, testa and kernel) and fractions of HCD. The hepatoprotective activities of different parts (seeds, testa and kernel) and three fractions (petroleum ether fraction, ethyl acetate fraction and aqueous fraction) with different polarities of HCD and herpetrione (HPE) isolated from HCD were determined using a mouse model of CCl4-induced liver injury based on the analysis of serum ALT and AST activities and the changes of antioxidant parameters like malondialdehyde (MDA) content, glutathione (GSH) level, superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities in the liver. Moreover, the chemical analysis of different parts and fractions of HCD was later analyzed by HPLC.. Our results showed that the ethyl acetate fraction and HPE significantly alleviated liver injury as indicated by the decreased levels of serum ALT and AST and reduce the pathological tissue damage induced by CCl4. Moreover, they decreased the MDA content and increased the levels of SOD, GSH and GSH-Px. Chemical analysis indicated that the ethyl acetate fraction were rich in HPE.. The lignans extract of Herpetospermum caudigerum is effective for the prevention of CCl4-induced hepatic damage in mice and HPE may be partially responsible for the pharmacological effect of hepatoprotection. The hepatoprotective effect may be related to its free radical scavenging effect, inhibiting lipid peroxidation and increasing antioxidant activity.

Topics: Alanine Transaminase; Animals; Aspartate Aminotransferases; Carbon Tetrachloride; Chemical and Drug Induced Liver Injury; Cucurbitaceae; Furans; Glutathione; Glutathione Peroxidase; Lignans; Liver; Malondialdehyde; Mice; Phytotherapy; Plant Extracts; Protective Agents; Seeds; Superoxide Dismutase