Enhancing effect and mechanism of muscone on transdermal penetration of traditional Chinese medicine ingredients with different log P value / 中国中药杂志

This study aimed to investigate the enhancing effect of muscone on the transdermal penetration of traditional Chinese medicine ingredients and explore its possible mechanism of action. The Franz diffusion cells were employed to investigate the effect of muscone on the transdermal permeation of a series of model drugs with a wide range of log P values. The solubilities at saturation and the stratum corneum(SC)/vehicle partition coefficients of model drugs were measured to evaluate the effect of muscone on drug thermodynamic activities and partition of drugs into SC. Attenuated total reflectance-Fourier transform infrared spectroscopy(ATR-FTIR) was employed to explore the effect of muscone on the molecular structure of SC. The results showed that muscone significantly promoted the transdermal penetration of hydrophilic and lipophilic drugs, and the enhancement ratio(ER) increased with the decrease in the log P. Muscone could interact with the SC lipids to increase the disorder and fluidity of lipid bilayer packing, which improved skin permeability and promoted transdermal absorption of drugs. This study provides a scientific basis for the application of muscone in traditional Chinese medicine topical preparations.

Brain Protection of Muscone in Rats with Brain Injury / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To observe cerebral protective effect of muscone (nasal administration) on traumatic brain injury model rats.</p><p><b>METHODS</b>SD rats were divided into the sham-operation group, the model group, and the treatment groups according to random digit table, 50 in each group. Traumatic brain injury model was established by controlled cortical strike. Rats in the sham-operation group received surgery and anesthesia procedures only, with no strike. Muscone (1.8 mg/kg) was delivered to rats in the treatment group using in situ nasal perfusion, 30 min each time, twice daily for 7 successive days. Water content of brain tissue was detected in each group before intervention (T1), at day 3 of intervention (T2), day 5 of intervention (T3), and after intervention (T4), respectively. Expression levels of brain derived neurotrophic factor (BDNF) and nerve growth factor (NGF) were detected using immunohistochemical analysis.</p><p><b>RESULTS</b>Compared with the sham-operated group, water content of brain tissue increased (P < 0.05), and expression levels of NGF and BDNF decreased in the model group at T1, T2, T3, and T4 (P <0. 01). Compared with the model group, water content of brain tissue decreased (P < 0.05), and expression levels of NGF and BDNF increased (P < 0.01) in the treatment group at T1, T2, and T3.</p><p><b>CONCLUSION</b>Nasal administration of muscone could reduce water content of brain tissue, alleviate cerebral edema, promote secretion of BDNF and NGF by olfactory ensheathing cells in traumatic brain injury rats.</p>

Preparation and evaluation of Shedan in situ forming gel based on ocular characteristics / 中国中药杂志

To develop an ophthalmic preparation of Shedan, an in situ forming gel was prepared with the formulation containing 18% of poloxamer 407 and 5% of poloxamer 188 by response surface designs plus central composite designs. The rheology results showed that LVE range gamma should limited within 0.5%, Shedan high-frequency region, and the thixotropy recovery time is less than 5 seconds. The phase transition temperature was 33.25 °C according to curve of storage modulus and loss modulus determined by temperature scanning. Surface tension and osmometer of it determined by surface tension meter and dew point osmometer were 36.43 mN · m(-1), and 320.6 mOsm · kg(-1), respectively. Fluorescein sodium was selected as the marker to monitor the corneal residence time, and the results showed that Shedan gel could prolong drug residence for 180 min. In line with zero-order kinetics, releases of muscone and salvianolic acid B in vitro depends on gels erosion. The results of rabbit ocular irritation experiments suggested that Shedan in situ forming gel was biocompatible and nonirritant. In conclusion, a novel Shedan in situ forming gel was developed and characterized for potential drug treatment of retinal vein occlusion.

Determination of the content of residual solvents in muscone by head-space gas chromatography / 中国医学科学院学报

<p><b>OBJECTIVE</b>To explore the usefulness of a head-space gas chromatography in the determination of residual solvents including methanol,ethanol,ethyl ether,and petroleum ether in muscone in artificial musk.</p><p><b>METHODS</b>The head-space gas chromatography was performed on HP-5(30 m×0.53 mm,5 Μm)capillary column with a hydrogen flame ionization detector. The carrier gas was nitrogen and the solvent was dimethyl sulfoxide. The injector temperature and the detector temperature were controlled at 180 ℃ and 250 ℃,respectively. The containers of head-space injector were preheated at 80 ℃ for 15 minutes. The column temperature was programmed raised,which achieved baseline separation of the components.</p><p><b>RESULTS</b>The results showed a good linear relationship for methanol,ethanol,ethyl ether,and petroleum ether(60-90 ℃)in the range of each consistency; and the limit of detection was 0.8,1.0,0.1,and 0.3 Μg/ml,respectively. The precision and average recoveries were satisfactory.</p><p><b>CONCLUSION</b>The head-space gas chromatography is simple,rapid,and precise technique for measuring residual solvents in muscone.</p>

Effect of borneol on intestinal absorption of muscone in rats / 中国中药杂志

<p><b>OBJECTIVE</b>To explore the influence of borneol on intestinal absorption of muscone in rats.</p><p><b>METHOD</b>An in situ intestinal circulation perfusion experiment was used to study the changes in intestinal absorption kinetics of muscone before and after being compatible with borneol.</p><p><b>RESULT</b>Compared with the muscone group (MG), the absorption rate constants (Ka), the half-life period (T1/2) and the absorption rate (A) of muscone in the borneol + muscone group (BMG) were on the rise, but with no significant difference; after being compatible with borneol for a long period, Ka, T1/2 and A in the last borneol on muscone group (LBMG) increased, with significant difference (P < 0.05). in duodenum, LBMG showed better effects than MG (T1/2, P < 0.05); and so did in jejunum (Ka, P < 0.05; T1/2, P < 0.05); in ileum, there was no significant statistical difference between LBMG and MG.</p><p><b>CONCLUSION</b>Borneol can promote the intestinal absorption of muscone in rats to some extent.</p>

Determination method of muscone in rat intestinal perfusate by GC-MS/MS and its intestinal absorption kinetic characteristics in rats / 中国中药杂志

<p><b>OBJECTIVE</b>To establish the method for determining muscone in rat intestinal perfusate by GC-MS/MS and study its intestinal absorption kinetic characteristics in rats.</p><p><b>METHOD</b>The GC-MS/MS method was used to determine the content of muscone in rat intestinal circulation fluid. In situ intestinal circulation perfusion was adopted to study absorption kinetics of muscone in rats.</p><p><b>RESULT</b>Muscone was proved to be well absorbed in each section of small intestine. Its absorption rate constants (Ka) and the absorption rate (A) in the rat intestine showed duodenum > jejunum (P < 0.05) , duodenum > ileum (P < 0.01). Its Ka, A and t1/2 in rat small intestine was 0.990 h(-1) , 43.58% and 0.705h, respectively.</p><p><b>CONCLUSION</b>Muscone was well absorbed in each intestinal section, with duodenum better than jejunum (Ka, T1/2, P < 0.05) significantly better than ileum (Ka, T1/2, P < 0.01; A, P < 0.05). There is no obvious statistical difference between jejunum and ileum.</p>

Protective effects and machanism of muskone on pheochromocytoma cell injure induced by glutamate / 中国中药杂志

<p><b>OBJECTIVE</b>To explore the mechanism of glutamate (Glu)-induced PC12 cell apoptosis and the protective effect of muscone.</p><p><b>METHOD</b>PC12 cells were randomly divided into six groups: normal group (Normal), model group injured by glutamate (Glu), nimodipine group (Nim) and muskone groups (Mus) of high, middle and low doses. The PC12 cells were pretreated with or without different concentrations of muskone for 30 min and then exposed to glutamate. MTT assay for cell survival, flow cytometric detection of apoptotic cells, DCF assay for reactive oxygen species (ROS) and flow cytometric assay was performed to determine the mitochondrial membrane potential in PC12 cell.</p><p><b>RESULT</b>PC12 cell damage, the concentrations of [Ca2+], and apoptosis induced by Glu were decreased after being administrated with paeoniflorin.</p><p><b>CONCLUSION</b>Muskone inhibited Glu-induced apoptosis in PC12 cells. The mechanism is related to inhibiting intracellular Ca2+ overload and maintaining mitochondral membrance potential.</p>

Effects of series of Muskone on heart hemodynamics and myocardial consumption of oxygen in experimental dogs / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the effects of series of Muskone (the muskone includes Slender Dutchmanspipe Root, Inula Root and neither kind of Common Aucklandia Root) on the heart hemodynamics and myocardial consumption of oxygen in experimental dogs, and to explain its pharmacological action on cardiovascular system.</p><p><b>METHOD</b>Arterial blood pressure, coronary blood flow, resistance in coronary artery, total peripheral resistance, work of left artrium and oxygen consumption index of the cardiac muscles were observed in anaesthetic dogs.</p><p><b>RESULT</b>The series of Muskone decreased arterial blood pressure significantly, dilated coronary artery and peripheral arteries significantly, increased coronary blood flow, decreased resistance in coronary artery, improved the work of left artrium, the oxygen availability of cardiac muscles and the complaisance of arteries in cardiac muscles.</p>

Review on investigations related to chemical constituents and biological activities of Periplaneta americana / 中国中药杂志

With the fast development of medicinal animals as new drugs, research on Periplaneta americana become hot recently. Several drugs which mainly consisted of P. americana were approved for clinical applications. The chemical constituents and pharmacological bioactivities of this insect were summarized herein, which provides informativon for further researches on this medicinal animal.

Study on comparative pharmacology of series of Muskone / 中国中药杂志

<p><b>OBJECTIVE</b>To study the therapeutic effects of the series of Muskone (the Muskone includes Slender Dutchmanspipe Root, Tumuxiang, and not Slender Dutchmanspipe Root) on experimental myocardial infarct and pain in rats.</p><p><b>METHOD</b>Coronary artery ligation was applied for the model of myocardial infarct. Therapeutic effects were evaluated by measuring parameters of histomorphometry, blood plasm of ET, 6- keto-PGF1alpha and TXB2. Intraperitoneal injection acetic was applied for the model of ache, the frequency and eclipse period of writhing were evaluated its effect of resisting pain.</p><p><b>RESULT</b>The Muskone including Radix Aristolociae, the Muskone including Radix Inulae and the Muskone without Radix Aucklandiae all can decrease the area of myocardial infarction in rats, the level of TXB2, ET, and the frequency of writhing significantly. Also it can increase the level 6-keto-PGF1alpha, the ratio of 6-keto-PGF1alpha and TXB2. Single Radix Aristolociae or Radix Inulae only relieved pain.</p><p><b>CONCLUSION</b>The Muskone including Radix Aristolociae, the Muskone including Radix Inulae and the Muskone without Radix Aucklandiae all have significant therapeutic effect on both myocardial infarction and pain, while single Radix Aristolociae or Radix Inulae only can relieve pain.</p>

Study on therapeutic effects of series of muskone on myocardial infarction canines / 中国中药杂志

<p><b>OBJECTIVE</b>To observe the effects of the series of Muskone (the Muskone includes Slender Dutchmanspipe Root, Tumuxiang, and not Slender Dutchmanspipe Root) on myocardial ischemia, myocardial infarction and hematological index in experimental canines, and to explain the pharmacological action and characteristic of its therapeutic effect on ischemic heart disease.</p><p><b>METHOD</b>The range and degree of myocardial ischemia was evaluated by epicardial electrogram mapping, and the range extent of myocardial infarction was determined by quantitate histology (N-BT staining method). Meanwhile, the changes of ET, TXB2, 6-Keto-PGF1alpha were determined to study the effects of the series of Muskone on myocardial ischemia, myocardial infarction and hematological index in experimental canines.</p><p><b>RESULT</b>The series of Muskone can improve myocardial ischemia and infarction in experimental canines, and relieve significantly the degree of myocardial ischemia (Sigma-ST) determined by epicardial electrogram mapping, decrease the range of myocardial ischemia (N-ST) determined by epicardial electrogram mapping and decrease infarction zone determined by N-BT staining method. And it has a significant inhibition on activity of ET induced by myocardial ischemia and infarction, and increases 6-Keto-PGF1alpha and 6-Keto-PGF1alpha/TXB2 induced by myocardial ischemia.</p><p><b>CONCLUSION</b>The series of Muskone has significant therapeutic effect on myocardial infarction.</p>

Synthesis of some F-heterocyclic compounds of potential anticancer activity using 8-fluoro-1- benzosuberone as a synthon

8-fluoro-1-benzosuberone I condensed with aromatic aldehydes in the presence of potassium hydroxide to yield the arylmethylene derrivatives II, which condensed with phenylhydrazinc and thiourea to give the corresponding pyrazol and pyrimidine derivatives III and IV, respectively Compound IV reacted with chloroctic acid, alpha - bromopropionic acid or beta-bromopropionic acid to afford the thiazolopy-rimidine, methylthiazolopyrimia and thiazinopyrimidine derivatives V, VI and VII, respectively. Compound V condensed with aromatic aldehydes to afford the arylmethycine derivativcs VIII. Also, the pyrano and pyridino-fluorobenzosubcronc derivatives IX and X were synthesized. The obtained products were preliminarily tested as anticancer agents and it was found that the products IIa, IIb, IXa, IXb and X showed promising activity against non-small cell lung cancer

Study of diffusion of muscone in different inclusion complexes and liposome through mouse (correction of rat) skin in vitro / 中国中药杂志

<p><b>OBJECTIVE</b>To compare the penetrating rate of muscone in different inclusion complexes and liposome.</p><p><b>METHOD</b>The transdermal effect of muscone in different inclusion complexes and liposome was studied comparatively on mouse [corrected] skin with 40% EtOH as the absorption solution and with an improved Franz diffuse cell.</p><p><b>RESULT</b>Among the different inclusion complexes and liposome, the penetrating rate of muscone in the HP-beta-cyclodextrin inclusion and the liposome were higher than muscone, and that of muscone in the beta-cyclodextrin inclusion is the lowest.</p><p><b>CONCLUSION</b>The HP-beta-cyclodextrin inclusion and the liposome can hence the muscone transdermal speed.</p>

Calcium modulatory properties of O,O-diphenyl O-N-cyclooctyl phosphoramidate [corrected] isolated from Ptychodiscus brevis in rat atria and smooth muscle.

Calcium modulatory activity of a marine toxin has been studied employing in vitro preparations. The toxin induced contracture in rat diaphragm was not modified by denervation, d-tubocurarine and tetrodotoxin (TTX). In contrast, varying concentrations of calcium, EGTA and ryanodine inhibited the contracture significantly. The toxin produced a series of repeating contractions in vas deferens. Experiments with TTX, adrenoceptor blockers and other agents exclude a release of neuromediators or direct stimulation of post synaptic receptors to account for the rhythmic effect in vas deferens. The dependence of rhythmicity on external Ca2+ concentration and inhibiting effect of Mn2+, ryanodine and nifedipine indicate a direct activation of voltage-sensitive calcium channel. The toxin also evoked a similar pattern of response in paced atria mediated through Ca2+ influx.