Iridoid glycosides extracted from Zhizi (Fructus Gardeniae) decrease collagen-induced platelet aggregation and reduce carotid artery thrombosis in an in vivo rat model

Objective

To investigate the anti-platelet aggregation and antithrombotic effects in rats of iridoid glycosides extracted from Zhizi (Fructus Gardeniae).

Methods

The present study evaluated the antithrombotic activity of iridoid glycosides (IGs) in a rat model of carotid artery thrombosis. The effects on coagulation, such as thromboplastin time (APTT), thrombin time (TT) and prothrombin time (PT), and the effect on collagen-induced platelet aggregation in vivo were investigated. Rats were intragastrically administered IGs (50, 100 or 200 mg/kg) twice daily for 3 days.

Results

IGs were shown for the first time to have an antithrombotic action through the inhibition of platelet aggregation, with little effect on the coagulation time of peripheral blood. Our results also showed that IGs may significantly and dose-dependently reduce arterial thrombus load in a model of carotid artery thrombosis and inhibit collagen-induced platelet aggregation in rats. IGs (100 or 200 mg/kg) had no significant effect on APTT and PT, but did lengthen TT at a higher dose.

Conclusion

These data, together with the previously reported neuroprotective effects of IGs in rats with cerebral ischemia, suggest that the antithrombotic action of IGs may potentially contribute to the treatment of cerebral ischemic diseases, including cerebral apoplexy.     

Total steroidal alkaloids from Veratrum patulum L. Inhibit platelet aggregation, thrombi formation and decrease bleeding time in rats

Ethnopharmacological relevance

Veratrum patulum L. (Liliaceae) is used as one source of the Chinese traditional drug “Lilu” which has been used in the treatment of aphasia arising from apoplexy, wind type dysentery, headache, etc. for thousands of years.

Aim of the study

To evaluate the antithrombotic effect of Veratrum patulum L. (Liliaceae) total steroidal alkaloids (VpA) and explore the potential mechanisms.

Materials and methods

The antithrombotic effect of VpA was evaluated in two experimental thrombosis models in rat. The potential antithrombotic mechanisms of VpA were explored by determining the coagulation parameters and platelet aggregation induced by various agonists. Cutting-tail rat model was used to evaluate the influence of VpA on bleeding time.

Results

VpA significantly inhibit the formation of arterial and venous thrombosis and showed different inhibitory effect on the platelet aggregation induced by various agonists with the following potency order: collagen > ADP > thrombin. VpA showed no influence on the coagulation parameters in rat. But VpA decreased the cutting-tail bleeding time in rat.

Conclusion

VpA possess antithrombotic effect on venous and arterial thrombosis. The antithrombotic effect of VpA is due to its inhibition to platelet aggregation, especially induced by collagen.     

Hypercoagulability in cancer patients grouped by syndromes differentiated with the theory of abnormal hilit in traditional Uyghur medicine

Objective

To investigate the relationship in malignant-neoplasm patients of hypercoagulability between syndromes differentiated with the theory of abnormal hilit in traditional Uyghur medicine (TUM).

Methods

A total of 248 patients with malignant tumors were enrolled. Based on the theory of TUM they were divided into two groups: abnormal Savda and abnormal Non-Savda (including abnormal Khan, abnormal Sepra and abnormal Belghem types); fifty healthy volunteers were selected as controls. Platelet (PLT), prothrombin time (PT), plasma fibrinogen (FIB), thrombin time (TT), activated partial thromboplastin time (aPTT) and D-Dimer (D-D) were measured in both groups.

Results

Compared with the control and abnormal Non-Savda groups, in the abnormal Savda group the PLT count increased (P<0.05), the PT was lengthened (P<0.01), and the FIB significantly increased (P<0.01). D-Ds in the three groups were significantly different (P<0.05). No significant difference was found in TT and aPTT values (P>0.05).

Conclusion

Hypercoagulability existed in patients with malignant tumors in the different types of TUM syndromes, especially in the abnormal Savda group; this was characterized by increased blood viscosity, platelet aggregation and thrombosis. D-D appears to be a significant predictor for the therapeutic effect of TUM in relation to malignant tumor therapies.     

Pharmacokinetics of ferulic acid and potential interactions with Honghua and clopidogrel in rats

Aim of the study

Ferulic acid (FA), a compound isolated from herbs, has a big potential to be developed into a useful drug for the treatment of cardiovascular disease. Early estimation of potential drug interaction is critical for drug development. As a common Chinese herb and Western drug respectively, Honghua and clopidogrel are often combined with FA-containing herbs to treat cardiovascular disease in clinical practice. This study aimed to investigate the pharmacokinetics of FA and potential interaction with Honghua and clopidogrel in rats.

Materials and methods

The experiments were performed on following three groups: FA alone (10 mg/kg, P.O.), combination of FA and Honghua (700 mg/kg, P.O.), combination of FA and clopidogrel (7 mg/kg, P.O.). Blood samples were collected before dosing and at 0, 2, 4, 7, 10, 15, 20, 30, 45, 60, 90, 120, 150, 180 and 210 min after drug administration to determine the plasma drug concentration of FA.

Results

FA was rapidly absorbed following oral administration with a mean time to peak plasma concentration (T_max) of 0.03 h. The corresponding maximum plasma concentration (C_max) and the area under the concentration-time curve (AUC) were 8174.55 ng/L and 2594.45 h ng/mL respectively. Coadministration of Honghua and clopidogrel resulted in a 63.5% and 79.7% increase in the AUC respectively. The C_max of FA was significantly increased by coadministration with clopidogrel (74.3%, p < 0.01). Moreover, the T_max of FA when coadministered with Honghua or clopidogrel was 3 and 3.76 times slower than when administered alone. Other pharmacokinetic parameters estimated for FA were also altered by the coadministrations, but no statistically significant differences were observed.

Conclusion

FA was rapidly absorbed with a low bioavailability after a single oral administration. The pharmacokinetics profile of FA in rats was partly altered by the coadministration of FA with Honghua or clopidogrel.     

Purification and characterization of a novel antithrombotic peptide from Scolopendra subspinipes mutilans

Ethnopharmacological relevance

The centipede has been prescribed for the treatment of cardiovascular diseases in Korea, China and other Far Eastern Asian countries for several hundred years.

Materials and methods

A novel antithrombotic peptide was isolated from Scolopendra subspinipes mutilans using a combination of ultrafiltration, Sephadex G-50 column, Source 15Q anion exchange column and RP-HPLC C18 column.

Results

The molecular mass of the purified peptide is 346 Da measured by Electrospray Ionization Mass Spectrometry (ESI-MS). The primary structure of the peptide is Ser-Gln-Leu (SQL) determined by Edman degradation. SQL potently prolonged the activated partial thromboplastin time (aPTT), and inhibited platelet aggregation.

Conclusions

These results help to clarify the mechanism of the antithrombotic activity of the centipede for effective treatment of cardiovascular and cerebrovascular diseases.     

Huangqi−Honghua combination and its main components ameliorate cerebral infarction with Qi deficiency and blood stasis syndrome by antioxidant action in rats

Ethnopharmacological relevance

Combination of Radix Astragali (Huangqi) and Carthamus tinctorius L. (Honghua) has been extensively used as traditional herb medicine in China for the treatment of stroke and myocardial ischemia diseases with Qi deficiency and blood stasis (QDBS) syndrome.

Aim

To investigate the effect of Huangqi−Honghua combination (HH) and its main components astragaloside IV (AS-IV) and Hydroxysafflor yellow A (HSYA) on cerebral ischemia-reperfusion (IR) with QDBS in rat model.

Materials and methods

Male rats were randomly divided into the following six groups: sham group, QDBS+I/R model group and treatment group including AS-IV, HSYA, AS-IV+HSYA and HH. The whole blood viscosity (WBV), plasma viscosity (PV), neurological examination, infarct volume, histopathology changes and some oxidative stress markers were assessed after 24 h of reperfusion.

Results

HH and its main components AS-IV+HSYA could significantly decrease WBV, PV, and also significantly ameliorate neurological examination and infarct volume after 24 h of reperfusion. They also significantly increased expression of Nuclear factor erythroid 2-related factor 2 (Nrf2), activities of antioxidants, such as superoxide dismutase (SOD), catalase and glutathione peroxidase (GSH-Px), led to decrease levels of malondialdehyde (MDA) and reactive oxygen species (ROS).

Conclusion

AS-IV and HSYA are responsible for the main curative effects of HH. The study may provide scientific information to further understanding the mechanism(s) of HH and its main components in removing blood stasis and ameliorating cerebral infarction. Additionally, AS-IV and HSYA appear to have synergistic effects on neuroprotection.     

Effects of Cydonia oblonga Miller extracts on blood hemostasis,coagulation and fibrinolysis in mice,and experimental thrombosis in rats

Introduction

Cydonia oblonga Miller (COM) is traditionally used in Uyghur medicine for the prevention of cardiovascular disease. The present study is designed to explore the effects of COM extracts on models and markers of thrombosis and related biomarkers.

Materials and methods

20, 40, 80 mg/kg/day COM aqueous extracts and 5 mg/kg/day aspirin, orally for 14 days were compared to untreated controls in mice on bleeding and clotting times, using the tail cutting and glass slide methods and for death rates in collagen–epinephrine pulmonary thrombosis, thrombolysis in vitro and euglobulin lysis time (ELT). In rats, common carotid artery FeCl₃-induced thrombus and inferior vena cava thrombosis occlusion time, plasma concentrations of thromboxane B₂ (TXB₂) and 6-keto-prostaglandine F₁α (6-keto-PGF1α) were measured.

Results and conclusion

Compared to controls, COM extracts dose-dependently prolonged bleeding by 2.17, 2.78 and 3.63 times, vs. aspirin 2.58, and the clotting time by 1.44, 2.47 and 2.48 times, vs. aspirin 1.91. COM reduced pulmonary embolus mortality by 27, 40 and 53%, vs. 47% for aspirin. COM dose-dependently increased thrombolysis by 45, 55 and 63%, vs. 56% for aspirin, and shortened ELT to 71, 61 and 43%, vs. 43% for aspirin. In rats, venous occlusion time was prolonged. Arterial and venous thrombus weights were dose-dependently reduced in COM groups. TXB₂ decreased and 6-keto-PGF1α increased with COM and aspirin, with an association between 6-keto-PGF1α/TXB2 and arterial or venous thrombus weight for all products, and for occlusion time with COM but not for aspirin.

Conclusion

We confirm the experimental effects of COM on hemostasis and thrombosis. Further exploration of putative clinical effects appear justified.     

An herbal decoction of Radix astragali and Radix angelicae sinensis promotes hematopoiesis and thrombopoiesis

Ethnopharmacological relevance

A decoction containing Radix angelicae sinensis and Radix astragali (Danggui Buxue Tang, DBT) has been used to raise the “Qi” and nourish the “Blood”. However, its effects on haematopoiesis and particularly thrombopoiesis have not been studied.

Aims

This study aims to examine the effects of DBT on hematopoiesis and thrombopoiesis.

Materials and methods

A myelosuppression mouse model was treated with DBT (10 mg/kg/day). Peripheral blood cells from DBT and thrombopoietin-treated samples were counted on days 0, 7, 14 and 21. Then CFU assays were used to determine the effects of DBT on the megakaryocytic progenitor cells and other lineages. Last, analyses of annexin V, caspase-3, and mitochondrial membrane potential were conducted in megakaryocytic cell line M-07e.

Results

Morphological examination showed that DBT treatment significantly increased the recovery of the megakaryocytic series. DBT significantly enhanced the platelet recovery and CFU-MK formation in vivo. DBT significantly promoted CFU-MK and CFU-F formation. Last, we observed the antiapoptotic effects of DBT on M-07e cells.

Conclusion

DBT might promote haematopoiesis and thrombopoiesis in the mouse model through (i) directly promoting the growth of megakaryocytes; (ii) indirectly promoting the growth of bone marrow stromal cells; (iii) inhibiting apoptosis of megakaryocytes.     

Effects of Tribulus terrestris on endocrine sensitive organs in male and female Wistar rats

Aim of the study

Investigate the possible effects of Tribulus terrestris (TT) on endocrine sensitive organs in intact and castrated male rats as well as in a post-menopausal rat model using ovariectomized females.

Materials and methods

Three different dose levels of TT (11, 42 and 110 mg/kg/day) were administered to castrated males for 7 days and to intact males and castrated females for 28 days. In addition to TT treatment, all experiments also included a group of rats treated with dehydroepiandrosterone (DHEA). In experiments using castrated males and females we also used testosterone and 17α-ethynylestradiol, respectively, as positive controls for androgenicity and estrogenicity.

Results

Neither DHEA nor TT was able to stimulate androgen sensitive tissues like the prostate and seminal vesicle in both intact and castrated male rats. In addition, administration of TT to intact male rats for 28 days did not change serum testosterone levels as well as did not produce any quantitative change in the fecal excretion of androgenic metabolites. However, a slight increase in the number of homogenization-resistant spermatids was observed in rats treated with 11 mg/kg/day of TT extract. In ovariectomized females, TT did not produce any stimulatory effects in uterine and vaginal epithelia.

Conclusions

Tribulus terrestris was not able to stimulate endocrine sensitive tissues such as the prostate, seminal vesicle, uterus and vagina in Wistar rats, indicating lack of androgenic and estrogenic activity in vivo. We also showed a positive effect of TT administration on rat sperm production, associated with unchanged levels of circulating androgens.     

Taoren-Honghua herb pair and its main components promoting blood circulation through influencing on hemorheology, plasma coagulation and platelet aggregation

Ethnopharmacological relevance

Persicae Semen (Taoren) and Carthami Flos (Honghua) used in pair which is named as Taoren-Honghua (TH) herb pair has been used in traditional Chinese medicine (TCM) for promoting blood circulation to dissipate blood stasis for many years in China.

Aim of the study

This paper investigated the effects of TH and its main components amygdalin and hydroxysafflor yellow A (HSYA) on hemorheological disorders of blood stasis in rats.

Materials and methods

Rats were randomly divided into seven groups (control group, model group, TH group, amygdalin group, HSYA group, amygdalin + HSYA group, and aspirin group) with eight animals in each, whose gender was equally distributed throughout groups. All treatments were performed by gavage and administered seven times with an interval of 12 h. After the fifth administration, the model rats except those in control group with blood stasis were established by being placed in ice-cold water during the interval between two injections of adrenaline hydrochloride (Adr); and blood samples were collected 30 min after the last administration on the following day.

Results

TH could significantly decrease whole blood viscosity (WBV), plasma viscosity (PV) and packed cell volume (PCV). It also significantly prolonged thrombin time (TT) and thromboplastin time (APTT), increased prothrombin time (PT) and lowered fibrinogen content (FIB). HSYA which significantly decreased WBV and PV had no effect on plasma coagulation parameters. Amygdalin could significantly decrease PV, prolong APTT and decrease FIB, showing few effects on WBV. TH and its main components amygdalin and HSYA could significantly reduce platelet aggregation and protect vascular endothelial cells. Based on the above results, amygdalin and HSYA were responsible for the main curative effects of TH and usually had synergetic effects, such as decreasing PV and platelet aggregation percentage.

Conclusions

The study may provide scientific information to further understanding of the mechanism(s) of TH and its main components in activating blood circulation to dissipate blood. It may also create valuable insight into the possible effects and utilization of TH and its components as a feasible alternative therapeutic agent for patients with hemorheological disorders.     

Lipid-lowering effects of Danhong injection on hyperlipidemia rats

Ethnopharmacological relevance

Danhong injection (DHI), a Chinese medical product extracted from Radix et Rhizoma Salviae Miltiorrhizae (Salvia miltiorrhiza Bge., Labiatae, Danshen in Chinese) and Flos Carthami (Carthamus tinctorius L., Compositae, Honghua in Chinese), has been reported to have anti-inflammatory, anti-oxidative and anti-fibrinolytic properties and is used extensively for the clinical treatment of cardiovascular disease in clinic. This study aimed to investigate the preventive and therapeutic effects of DHI on hyperlipidemia.

Materials and methods

Forty-eight adult male Sprague-Dawley rats were randomly divided into four groups: normal control (NC), model control (MC) and DHI-treated at doses of 1.0 mL/kg and 2.0 mL/kg. The effects of DHI on serum triglyceride (TG), total cholesterol (TC), glucose, high density lipoprotein cholesterol (HDL-C) and low density lipoprotein cholesterol (LDL-C) were evaluated and insulin was determined by enzyme-linked immunosorbent assay (ELISA). Moreover, the expression of acetyl-CoA carboxylase 1 (ACC1), fatty acid synthase (FAS), carnitine palmitoyl transferase 1 (CPT1), hydroxymethylglutaryl-CoA reductase (HMGR) and peroxisome proliferator-activated receptor alpha (PPAR-α) in liver were determined by real-time PCR.

Results

Compared with the MC group, rats treated with DHI had significantly reduced TG, TC, LDL-C and arteriosclerosis index (AI). Expression of FAS and HMGR mRNA was significantly reduced, whereas the CPT1 and PPAR-α were significantly increased.

Conclusion

DHI treatment was accompanied by significantly increased lipolysis in the liver and decreased fatty acid synthesis. The insights gained from this study will improve both understanding of the mechanisms involved in the effect of DHI on hyperlipidemia and the pharmacological rationale for the use of DHI in diseases caused by lipid metabolic disorders.     

Entzugssyndrom beim Neugeborenen – Nachweis von aktiven organischen und psychischen Ohrakupunkturpunkten

Background

Neonatal Abstinence Syndrome (NAS) may occur in neonates whose mothers abused drugs during pregnancy, as well as in neonates whose mothers received substitution therapy during pregnancy.

Objective

To determine the presence of active ear points in neonates with NAS.

Patients and Method

Since September, 2008 all neonates with NAS admitted to the Division of Neonatology at the University Hospital Graz were examined (provided acceptance through their legal guardians). The examination was conducted on the third day (mean value 70,3 hours) after delivery, using a neuronal pen (PS 3 © Silberbauer, Vienna, Austria).

Results

From September, 2008 until December, 2009 we examined 6 neonates (4 male, 2 female) with NAS. The psychovegetative rim was the most sensitive area, followed by Shen men (55) and a few organotropic points: esophagus (85), lung (101), kidney (95). In all neonates we found the presence of psychotropic ear points. The detectable psychotropic ear points were the frustration-point, R-point, respectively known as Haldol- or Bourdiol-points, and the Psychotropic Area (PT1–PT2).

Discussion and Conclusion

In neonates with NAS, ear points are detectable by a neuronal pen equally on both ears. The most important area is the psycho-vegetative rim as well as some organotropic points. This result coincides with earlier studies on healthy on-date children. However, the investigated neonates revealed active signals in some psychotropic ear points, in contrast to healthy neonates.     

Sedative and hypnotic effect of freeze-dried paeoniflorin and Sini San freeze-dried powder in pentobarbital sodium-induced mice

Objective

To investigate the sedative and hypnotic activity of paeoniflorin and freeze-dried Sini San powder on mice and provide a reliable method for determining the pharmacodynamic material basis of Sini San.

Methods

Male adult mice weighing 20–22 g were used in this study. Three experiments were carried out. Synergism with pentobarbital was used as an index for hypnotic effect. Loss of the righting reflex was used to determine the start of sleep. Sleep latency and sleeping time were recorded in each experiment.

Results

The coefficient of variation of the supra-threshold dose (55 mg/kg) was significantly lower than that of the threshold dose. The sleep latency of mice was significantly decreased, and the sleeping time of mice was significantly prolonged. The effects of paeoniflorin and Sini San on prolonging the sleeping time of mice induced by pentobarbital sodium were significantly stronger than those in the control group.

Conclusion

Paeoniflorin produces significant sedative and hypnotic effects, and there is an obvious dose-effect relationship.     

Preventive and therapeutic effects of Danhong injection on lipopolysaccharide induced acute lung injury in mice

Ethnopharmacological relevance

Danhong injection (DHI), a Chinese Materia Medica standardized product extracted from Radix et Rhizoma Salviae Miltiorrhizae (Salvia miltiorrhiza Bge., Labiatae, Danshen in Chinese) and Flos Carthami (Carthamus tinctorius L., Compositae, Honghua in Chinese), has been reported to have anti-inflammatory, anti-oxidative and anti-fibrinolytic properties, which is used extensively for the treatment of cardiovascular diseases in clinic.

Aim of this study

The present study aimed to investigate the preventive and therapeutic effects of DHI on lipopolysaccharide (LPS) induced acute lung injury (ALI) in mice.

Materials and methods

Lung injury was induced by intranasal instillation with 10 μg LPS. Mice were randomly divided into four groups:Control group; LPS group; LPS+5 ml/kg DHI group and LPS+10 ml/kg DHI group. The effects of DHI on LPS-induced neutrophils influx, inflammatory cytokines release, protein leakage, myeloperoxidase (MPO) and superoxide dismutase (SOD) activities, malondialdehyde (MDA) level were examined. In addition, the NF-κB activation in lung tissues was detected by Western blot.

Results

In LPS challenged mice, DHI significantly reduced the infiltration of activated neutrophils and decreased the levels of TNF-α and IL-6 in bronchoalveolar lavage fluid (BALF). DHI also inhibited protein extravasation in BALF, attenuated edema and the pathological changes in the lung. In addition, DHI markedly prevented LPS-induced elevation of MDA and MPO levels, as well as reduction of SOD activity. Further study demonstrated that DHI effectively inhibited the NF-κB activation in lung tissues.

Conclusion

DHI has been demonstrated to protect mice from LPS induced acute lung injury by its anti-inflammatory and anti-oxidant activities.     

Dragon's Blood extract has antithrombotic properties, affecting platelet aggregation functions and anticoagulation activities

Ethnopharmacological relevance

Dragon's Blood from Dracaena cochinchinensis (Lour.) S.C. Chen (Yunnan, China), as a traditional Chinese medicinal herb, was shown to have certain antithrombotic effects. A new preparation process was used to extract effective components from Dragon's Blood. A 95% ethanol extract A (EA) and a precipitate B (PB) fraction were obtained and compared. Reliability of the preparation process was validated by pharmacodynamic experiments.

Materials and methods

A rat/mouse thrombosis and blood stasis model was developed for this study, and EA and PB effects on thrombosis, platelet functions and blood coagulation activities were analyzed.

Results

It was observed that the EA fraction had significantly better inhibitory effects than the PB fraction on thrombosis (p < 0.05), platelet aggregation function (p < 0.01) and anticoagulation activity (p < 0.05-0.01).

Conclusions

The results obtained here showed that EA fraction from Dragon's Blood contained pharmacologically effective compounds with antithrombotic effects, partially improving platelet function and anticoagulation activity.     

Biological indicators of sub-optimal health status

Objective

To investigate biological indicators of sub-optimal health status and provide means of objective assessment of sub-optimal health status.

Methods

We set the unified standards for diagnosing a SHS. We tested various laboratory indicators in 407 cases that we selected randomly from 2807 subjects and collected 15 mL of fasting venous blood from each case. We measured serum immunoglobulin A (IgA) and immunoglobulin G (IgG) concentrations, serum beta endorphins (β-EP), cortisol (C), testosterone (T), plasma adrenocorticotropic hormone (ACTH) and serum T lymphocyte subsets CD3+ and CD4+.

Results

Mean serum testosterone concentrations and their ratio to cortisol (C) concentrations were significantly higher in the healthy group than in those with sub-optimal health status (P<0.01). Mean serum CD3+ concentrations were significantly higher in those with sub-optimal health status than in the healthy group (P<0.05).

Conclusion

Decreased serum testosterone/cortisol ratio may be an objective indication of sub-optimal health status. Changes in neuroendocrine and immunological indicators may explain some of the symptoms, including malaise and poor work performance, attributable to persistent or relapsing fatigue in subjects with sub-optimal health status.     

Effect of Honghua (Flos Carthami) on nitric oxide production in RAW 264.7 cells and α-glucosidase activity

Objective

To study the effects of extracts from Honghua (Flos Carthami) on lipopolysaccharide induced nitric oxide (NO) production in RAW 264.7 cells and the influence of the extracts on yeast α-glucosidase activity. The total flavonoid content of the extracts was also determined.

Methods

Cytotoxicity of the extracts to RAW 264.7 cells was evaluated by the ATPlite™ method. Inhibitory effects of the extracts on NO production were evaluated by Griess assay. Curcumin was used as a positive control. Screening of extracts for potential α-glucosidase inhibitors was done by a fluorometric assay. The assay was based on the hydrolysis of 4-methylumbelliferyl-a-D-glucopyranoside to form the fluorescent product, 4-methylumbellifer-one. Acarbose was used as a positive control. The total flavonoid content was tested using kaempferol as the standard.

Results

There were significant inhibitory effects on NO production when the extracts were 25-100 μg/mL (P<0.05) and curcumin was 2-4 μg/mL (P< 0.001). The extracts showed an inhibitory effect on α-glucosidase activity at the concentrations of 15.6-125 μg/mL with a half maximal (50%) inhibitory concentration (IC50) of (32.8 ± 5.7) μg/mL, compared with the IC₅₀ of acarbose at (1.8±0.4) μg/mL. There was a significant difference between the two IC₅₀ values (P<0.001). The total content of flavonoids per gram of dried herb was 1.14 mg.

Conclusion

Honghua (Flos Carthami) showed inhibitory effects on NO production in activated RAW 264.7 macrophage cells and an inhibitory effect on yeast α-glucosidase. There might be a relationship between these pharmacological effects and its flavonoid content.     

Effective constituents in Xiexin Decoction for anti-inflammation

Aim of the study

To ascertain the effective constituents in Xiexin Decoction for anti-inflammation and the interactions of these constituents at the pharmacodynamic level.

Materials and Methods

Rats were administered oral Xiexin Decoction 1 h before intraperitoneal lipopolysaccharide. Nitric oxide production and Xiexin Decoction constituents in venous serum samples were quantified and the correlation between nitric oxide production and each constituent in serum was calculated. Raw264.7 cells were stimulated with lipopolysaccharide and one or more Xiexin Decoction constituents; cell viability and nitric oxide production was quantified.

Results

Xiexin Decoction significantly decreased nitric oxide production in vivo, which correlated well with rhein, baicalin, emodin and aloe-emodin. All the typical constituents of Xiexin Decoction, with the exception of physcione and chrysophanol, dose-dependently inhibited nitric oxide production in vitro. In an orthogonal designed in vitro study, rhein was the most powerful constituent, followed by baicalin then berberine and no synergy was found among these constituents.

Conclusions

Rhein was the most effective anti-inflammatory constituent in Xiexin Decoction followed by baicalin; no synergy was observed between rhein, baicalin and berberine at the pharmacodynamic level in vitro.