[Pre-formulation physicochemical properties of component-based Chinese medicine of Qinqi Fengshi Fang].

Pre-formulation physicochemical properties of the component-based Chinese medicine of Qinqi Fengshi Fang were investigated to provide a research basis for the design of the dosage form for component-based Chinese medicine of Qinqi Fengshi Fang. The macroporous resin adsorption and refining technology was used to prepare the total glycosides extract of Gentianae Macrophyllae Radix, Panacis Majoris Rhizome and Corni Fructus respectively in the prescription of Qinqi Fengshi Fang. Their physicochemical properties were investigated, including solubility, wettability, hygroscopicity, equilibrium solubility, oil-water partition coefficient, and stability. The results showed that the total glycosides of Gentianae Macrophyllae Radix, Panacis Majoris Rhizome and Corni Fructus all had good solubility and wettability. The solubility index of each total glycoside component was greater than 85%, and the water absorption index was greater than 50%. In the range of pH 2.0-7.4, the equilibrium solubility of three kinds of total glycosides all increased with the increase of pH, showing a consistent change trend of solubility. The hydrophilicity was also suitable and similar. Overall, three kinds of total glycosides showed good stability, but strong hygroscopicity. The degree of hygroscopicity was as follows: total glycosides of Gen-tianae Macrophyllae Radix > total glycosides of Corni Fructus > total glycosides of Panacis Majoris Rhizome. Therefore, the hygroscopi-city needed to be considered in the preparation of the component-based Chinese medicine of Qinqi Fengshi Fang. The excipients and packaging materials can be properly selected to reduce the hygroscopicity of the preparation. This study provides a reference for the dosage form design of the component-based Chinese medicine of Qinqi Fengshi Fang.

A pair of new neo-clerodane diterpenoid epimers from the roots of Croton crassifolius and their anti-inflammatory.

A pair of new neo-clerodane diterpenoid epimers, 3S-methoxyl-teucvin (1) and 3R-methoxyl-teucvin (2), were isolated from the Roots of Croton crassifolius. Their structures were completely established on the basis of spectroscopic methods, and the absolute configurations were determined by analysis of electronic circular dichroism (ECD) spectroscopy and X-ray diffraction analysis. Compounds 1 and 2 exhibited anti-inflammatory activities with IC50 values of 0.82 and 0.54 µM, respectively, while the IC50 value of dexamethasone as a positive control was found to be 0.14 µM.

The chemistry and pharmacology of Ligularia przewalskii: A review.

ETHNOPHARMACOLOGICAL RELEVANCE: Ligularia przewalskii (Maxim.) Diels (LP) (called zhangyetuowu in Chinese), is generally found in moist forest areas in the western regions of China. The root, leaves and flower of LP are utilized as a common traditional medicine in China. It has been utilized conventionally in herbal remedies for the remedy of haemoptysis, asthma, pulmonary phthisis, jaundice hepatitis, food poisoning, bronchitis, cough, fever, wound healing, measles, carbuncle, swelling and phlegm diseases. AIM OF THE STUDY: The review aims to provide a systematic summary of LP and to reveal the correlation between the traditional uses and pharmacological activities in order to provide updated, comprehensive and categorized information and identify the therapeutic potential for its use as a new medicine. MATERIALS AND METHODS: The relevant data were searched by using the keywords "Ligularia przewalskii" "phytochemistry", "pharmacology", "Traditional uses", and "Toxicity" in "Scopus", "Scifinder", "Springer", "Pubmed", "Wiley", "Web of Science", "China Knowledge Resource Integrated databases (CNKI)", "Ph.D." and "M.Sc. dissertations", and a hand-search was done to acquire peer-reviewed articles and reports about LP. The plant taxonomy was validated by the databases "The Plant List", "Flora Reipublicae Popularis Sinicae", "A Collection of Qinghai Economic Plants", "Inner Mongolia plant medicine Chi", Zhonghua-bencao and the Standard of Chinese herbal medicine in Gansu. RESULTS: Based on the traditional uses, the chemical nature and biological effects of LP have been the focus of research. In modern research, approximately seventy-six secondary metabolites, including thirty-eight terpenoids, nine benzofuran derivatives, seven flavonoids, ten sterols and others, were isolated from this plant. They exhibit anti-inflammatory, antioxidative, anti-bacterial and anti-tumour effects, and so on. Currently, there is no report on the toxicity of LP, but hepatotoxic pyrrolizidine alkaloids (HPA) were first detected with LC/MSn in LP, and they have potential hepatotoxicity. CONCLUSIONS: The lung-moistening, cough-relieving and phlegm-resolving actions of the root of LP are attributed to the anti-inflammatory properties of flavonoids and terpenoids. The heat-clearing, dampness-removing and gallbladder-normalizing (to cure jaundice) actions of the flowers of LP are based on the anti-inflammatory, antioxidant and hepatoprotective activity properties of terpenoids, flavonoids and sterols. The Traditional Chinese Medicine (TCM) characteristics of LP (bitter flavour) corroborate its potent anti-inflammatory effects. In addition, the remarkable anti-inflammatory and antioxidant capacities of LP contribute to its anti-tumour and antitussive activities. Many conventional uses of LP have now been validated by modernized pharmacological research. For future research, further phytochemical and biological studies need to be conducted on LP, In particular, the safety, mechanism of action and efficacy of LP could be of future research interest before beginning clinical trials. More in vivo experiments and clinical studies are encouraged to further clarify the relation between traditional uses and modern applications. Regarding the roots, leaves and flowers of LP, their chemical compositions and clinical effects should be compared. The information on LP will be helpful in providing and identifying its therapeutic potential and economic value for its use as a new medicine in the future.

[Study on Chemical Constituents of Delphinium caeruleum].

Objective: To study the chemical constituents from the whole plant of Delphinium caeruleum. Methods: The chemical constituents were isolated and purified by silica gel and Sephadex LH-20 column chromatography. The structures of the isolated compounds were elucidated by spectroscopic analysis and physicochemical properties. Results: Twelve compounds were isolated and purified from the ethanol extract of Delphinium caeruleum. They were identified as ß-sitosterol( 1),kaempferol( 2),quercetin( 3),isovanillic acid( 4),apigenin( 5),luteolin( 6),8-methoxy-5,7,3',4'-tetrahydroxy-flavone( 7),ß-daucosterol( 8),kaempferol-3-O-ß-D-glucoside( 9),3,5-dihydroxy-4'-methoxyflavone-7-yl-O-ß-D-glucopyranosyl-( 1→4)-α-L-rhamnopyranoside( 10),rutin( 11) and sucrose( 12). Conclusion: Compounds 1 ~ 12 are isolated from this plant for the first time.

[Chemical Constituents from Rubus stans].

Objective: To study the chemical constituents of Rubus stans. Methods: The chemical constituents were isolated and purified by silica gel and Sephadex LH-20 column chromatography. The structures were identified on the basis of spectroscopic analysis and physicochemical properties. Results: Eleven compounds were isolated and purified from the ethanol extract of Rubus stans. They were identified as ß-sitosterol( 1),betulinic acid( 2),euscaphic acid( 3),ursolic acid( 4),corosolic acid( 5),kaempferol( 6),quercetin( 7),2α,3ß,19α,23-tetrahydroxy-urs-12-en-28-oic acid( 8),ß-daucosterol( 9),quercetin-3-O-ß-D-glucoside( 10) and kaempferol-3-O-ß-D-6-O-( p-hydroxycinnamoyl)-glucopyranoside( 11). Conclusion: All the compounds are isolated from this plant for the first time.

[Mechanism of Musk and Borneol on Inflammatory of Cerebral Ischemia and Reperfusion Injury at Different Time Points of Acute Phase in Rats].

OBJECTIVE: To investigate the mechanism of Musk and Borneol on cerebral ischemia and reperfusion injury at different time points of acute phase in rats. METHODS: 180 rats were divided into seven groups including sham, ischemia-reperfusion after 24 h and 72 h model group, Musk 50 and 25 mg/kg groups, Borneol 50 and 25 mg/kg groups, and Xingnaojing 10 mL/kg group. Ischemia-reperfusion model was made after administration of each drug. The neurologic impairment scores at different time points after ischemia and reperfusion was evaluated, activities of cyclooxygenase (COX-2) and 5-lipoxygenase (5-LOX) in brain tissue were determined, and the expression of CysLT2 protein and mRNA in hippocampus were explored. RESULTS: Musk and Borneol significantly improved the neurologic impairment scores of ischemia-reperfusion injury rats, improved the pathological morphology of rats brain tissue, reduced the activities of COX-2 and 5-LOX in brain homogenates,and inhibited the expression of CysLT2 protein in hippocampus. CONCLUSION: Musk and Borneol have protective effect on inflammatory injury of acute injury in ischemia-reperfusion injury rats, the mechanism is related to inhibition the activity of COX-2 and 5-LOX in brain.

Relationship of serum homocysteine level with nutritional status and HbA1c level in elderly inpatients.

BACKGROUND: Hyperhomocysteinemia is a risk factor for vascular diseases. This study aimed to investigate the serum total homocysteine (tHcy) level and nutritional status in elderly inpatients and determine the relationship between tHcy level and nutritional status. METHODS: This cross sectional study was carried out in the Tongji hospital, and 142 subjects were consecutively recruited. Fasting blood was collected, and the liver and kidney function, blood glucose, glycosylated hemoglobin (HbA1c), plasma protein, lipid profile, folic acid, vitamin B12 and serum total tHcy were measured. Anthropometric measurements, grip strength and the shortened MNA form (MNA-SF) were used to assess the nutritional status. RESULTS: Undernutrition was common in this population. Based on MNA-SF scores, 34.2% of subjects were at risk of malnutrition, and malnourished subjects accounted for 4.9%. The mean tHcy was 14.10±5.46 µmol/l, and the prevalence of hyperhomocysteinemia was 32.4% (46/142). Hyperhomocysteinemia was a risk factor of cerebral infarction (RR=1.636, 95% CI: 1.169-2.288); Serum tHcy was negatively correlated with serum folic acid, vitamin B12 and MNA-SF score (r=-0.348,P=0.000; r=-0.236, P=0.005; r=-0.208, P=0.014), and positively with BMI within normal range (18.5-23.9; r=0.232, P=0.044). Serum tHcy was negatively correlated with HbA1c, (r=-0.196, P=0.021) and positively with serum creatinine (r=0.327, P=0.000), but unrelated to fasting blood glucose (r=-0.098, P=0.250). Multivariate stepwise regression analysis showed serum folic acid, serum creatinine, MNA-SF score and HbA1c were independent determinants of serum tHcy. CONCLUSION: Elderly subjects have higher serum tHcy level. Compromised renal function, poor nutritional status and lower blood glucose are likely to influence the serum tHcy level.

Relative performance of two equations for estimation of glomerular filtration rate in a Chinese population having chronic kidney disease.

BACKGROUND: The new Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) equation was developed to address the systematic underestimation of glomerular filtration rate (GFR) by the Modification of Diet in Renal Disease (MDRD) Study equation in patients with relatively well-preserved kidney function. Performance of the new equation in the Chinese population is unknown. The goal of the present study was to compare performance of these two equations in Chinese patients with chronic kidney disease (CKD). METHODS: We enrolled 450 Chinese patients (239 women and 211 men) with CKD in the present study. The renal dynamic imaging method was used to measure the referenced standard GFR (rGFR) for comparison with estimations using the two equations. Their overall performance was assessed with the Bland-Altman method and receiver-operating characteristics (ROC) analysis. Performance of the two equations in lower and higher estimated GFR (eGFR) subgroups was further investigated. RESULTS: Both eGFRs correlated well with rGFR (r = 0.88, 0.81, P < 0.05). In overall performance, the CKD-EPI equation showed less bias, higher precision and improved accuracy, and was better for detecting CKD. In the higher-eGFR subgroup, the CKD-EPI equation corrected the underestimation of GFR by the abbreviated MDRD equation. CONCLUSIONS: The CKD-EPI equation outperformed the abbreviated MDRD equation not only in overall performance but also in the subgroups studied. For the present, the CKD-EPI equation appears to be the first-choice prediction equation for estimating GFR.