Pharmacokinetic comparisons of two different combinations of Shaoyao-Gancao Decoction in rats: competing mechanisms between paeoniflorin and glycyrrhetinic acid.

ETHNOPHARMACOLOGICAL RELEVANCE: Shaoyao-Gancao Decoction (SGD), a well-known traditional Chinese medicine prescription, is a combination of Radix Paeoniae Alba (Paeonia lactiflora Pall, root) and Glycyrrhizae uralensis (Glycyrrhiza uralensis Fisch., root and rhizome, honeyed) for spasmolysis and emergency pain relief. Paeoniflorin (PF) and glycyrrhetinic acid (GA) are two typical active components of SGD for pain relief. AIM OF THE STUDY: To study comparative pharmacokinetics of ten bioactive compounds in SGDs with two different combinations of RP and GU, and therefore to investigate the herb-herb interaction mechanisms of Shaoyao-Gancao Decoction for better spasmolysis and emergency pain relief in rats. MATERIALS AND METHODS: Herbal IR macro-fingerprinting was implemented to provide the full chemical fingerprints of RP, GU and SGD decoctions and to investigate the variation rule of the full chemical profile of SGDs with various combinations of RP and GU. A specifically developed HPLC-MS/MS assay coupled with protein precipitation method was employed to determine the plasma concentrations of the ten analytes. Male Wistar rats were orally administered with SGD1 (RP:GU, 1:1 (w/w)) and SGD2 ((RP:GU, 4:1 (w/w)) equivalent to 9.5 g/kg body weight of GU. RESULTS: Full chemical fingerprints of RP, GU and SGDs with various combinations of RP and GU were provided in the form of IR macro-fingerprints. Except for liquiritin, there were statistically significant differences (p<0.05 or p<0.01) of these analytes between SGD1 and SGD2 in in vivo pharmacokinetic study. Compared with the results when oral administrated with SGD1, six glycosides (PF, albiflorin, oxypaeoniflorin, isoliquiritin, ononin, and glycyrrhizin) exhibited higher systematic exposure levels (AUC0-t) and slower elimination rates (CL) whereas two glycones (GA and isoliquiritigenin) were the reverse when administrated with SGD2. CONCLUSIONS: Increasing the amount of RP attenuated the inhibitory effect of GA via competing being consumed by intestinal bacteria (or ß-glucosidase) to reduce the conversion amount of glycyrrhizin to GA and subsequently to afford significantly higher bioavailability and longer efficacy of PF, glycyrrhizin, albiflorin, oxypaeoniflorin, isoliquiritin, and ononin, leading to better spasmolysis and emergency pain relief.

[Study on different proportion formulas of activating blood circulation by FTIR].

Fourier transform spectroscopy (FTIR) and two-dimensional correlation spectroscopy were used to analyze different compatibility forms of sargentgloryvine stem, radix paeoniae rubra and cortex moutan in order to study the FTIR spectra of different proportion formulas. The results indicate that different proportion formulas have distinct change regularity in FTIR spectra, second derivative spectra and synchronous 2D. Key components of sargentgloryvine stem's characteristic absorption band are 1 610, 1 518 and 1 446 cm(-1) which are characteristic absorption band of aromatic material, and in the original formula, that shows stronger peak than others, suggesting that original formula can make the best of composition of drug action. In the different proportion formulas, 1 614 cm(-1) is nearer to 1 610 cm(-1), which is sargentgloryvine stem's characteristic absorption band, than to 1 706 cm(-1), illustrating that sargentgloryvine stem is more influential formula than others. According to identification and ascription of characteristic absorption band, it was initially revealed that different proportion of drug dosage can affect pharmacodynamic action of integral formula.

[Analysis and comparison of daxueteng and their extracts by FTIR].

The present study is to compare and analyze Sargentodora cuneata (oliv) Rehd. etwils herbs, the aqueous, anthraquinone extracts and residue in Jiang Xi and An Hui quickly and undamagedly by Fourier transform infrared spectroscopy(FTIR) and two-dimensional correlation spectroscopy. In the spectra of DaXueTeng, there are two strong peak areas at about 1400-1620 cm(-1) and 1000-1200 cm(-1), and it was concluded that DaXueTeng contains much glycoside and anthraquinone. Anthraquinone extracts only exhibit strong peaks of 1400-1620 cm(-1) which were stronger than that of 1000-1200 cm(-1), and this illustrated that this method was adapted to extracting anthraquinone; then aqueous only show powerful peaks of 1000-1200 cm(-1), so the authors know that the craftwork was suitable for extracting glycoside; finally, the authors also found that the residue of DaXueTeng contained much calcium oxalate. All of these illustrated that FTIR could not only analyze and identify traditional Chinese medicine (TCM) and extract components, but also discriminate contents of different extracts of TCM. The authors developed the new method to analyze and evaluate the DaXueTeng and their pharmacodynamic extracts successfully.

Beneficial effect of HHI-I on cerebral microcirculation, blood-brain barrier in rats and anti-hypoxic activity in mice.

OBJECTIVE: To investigate the effect of HHI-I (I) on the cerebral microcirculation, the blood-brain barrier permeability in rats and anti-hypoxic activity in mice. METHODS: (1) The blood microcirculation of the brain in rats was investigated by laser Doppler flowmetry with the probes laid on the cerebral pia mater or inserted into the brain parenchyma. (2) The protective action of HHI-I against the brain microcirculation disturbance induced by intravenous injection of high-molecular dextran (10%, 9 mL/kg) was observed. (3) The protective effect of HHI-I against lethal hypoxia in mice was observed with a hypoxic chamber containing 5% oxygen. (4) The disruption of the blood-brain barrier (BBB) permeability in rats was caused by phenylephrine-induced hypertension, and the effect of intravenous injection of HHI-I on the BBB permeability was determined using Evans blue as the marker. RESULTS: HHI-I could increase the blood flow of the cerebral microcirculation in rats and possess some protective effects on the brain microcirculatory disturbance. Besides, HHI-I could decrease the brain edema occurring in the process of lethal hypoxia in mice. While increasing the blood flow of brain, HHI-I could lower the BBB permeability in rats. CONCLUSION: HHI-I has several beneficial effects on the cerebral microcirculation, blood-brain barrier in rats and anti-hypoxic activity in mice.

Da-Cheng-Qi-Tang promotes the recovery of gastrointestinal motility after abdominal surgery in humans.

In order to examine the effects of Da-Cheng-Qi-Tang (DCQT) on gastrointestinal motility functions after abdominal surgery in humans, 33 patients with abdominal surgeries and 36 patients with cholecystectomies were divided into the DCQT and the control groups at random. Electrogastrography (EGG) and gastroduodenojejunal manometry was performed and the levels of plasma motilin were measured by radioimmunoassay. The results were as follows: (1) on the day of surgery, the ratio of EGG normal frequency in the DCQT group was higher than in the control group (P=0.0016); (2) the power of EGG in the DCQT group was higher than in the control group on the second and third days after surgeries (P=0.0011 and P=0.0215, respectively); (3) the percentage of normal bowel peristalsis was significantly higher in the DCQT group than in the control group (P<0.01); and (4) in the DCQT group, the plasma motilin level reached its peak earlier than in the control group. Our results suggest that DCQT can increase plasma motilin, enhance gastrointestinal motility, improve gastric dysrythmia, and reduce gastroparesis after abdominal surgery.

[Intensive effect of traditional Chinese medicines activating blood to resolve stasis on medicines dredging intestines--influence on peristalsis of small intestine in guinea pigs].

OBJECTIVE: To observe the changes of peristalsis of small intestine in guinea pigs after administration of traditional Chinese medicines activating blood to resolve stasis (Compound Danshen Decoction, CDSD) or/and medicines dredging intestines (Dachengqi Decoction, DCQD), and to explore the synergetic or intensive effect of CDSD on DCQD. METHODS: By means of BL-420 Biological Experimental System, peristalsis of small intestine was recorded and analyzed following administration of DCQD, CDSD or Huoxue Chengqi Decoction (HXCQD, compound of CDSD and DCQD) respectively in different experimental periods. RESULTS: The amplitude and frequency of intestinal peristaltic wave obviously increased following administration of the three decoctions, but HXCQD appeared to be most dominantly. CONCLUSION: The effect of DCQD can be further enhanced by combining use of CDSD, suggesting that the traditional Chinese medicines activating blood to resolve stasis have an intensive effect on medicines dredging intestines.