OBJECTIVE:To study the HPLC fingerprint profiles of crude and processed Semen Cassiae so as to provide basis for the establishment of chromatographic fingerprint of Semen Cassiae.METHODS: The samples of Semen Cassiae were hydrolyzed in the 1.5 mol?L-1 hydrochloride acid and then reflux extracted with chloroform.The HPLC analysis was run in gradient elution.The whole information of single-wavelength chromatographic fingerprint,two-dimension information data at full wavelength 220 nm～550 nm and the data of 18 fingerprint peaks compared with chrysophanol were treated by cluster analysis.RESULTS:It was observed that the contents of several chemical components were higher in the crude or processed Semen Cassiae than in chrysophanol.There were differences between the crude and the processed Semen Cassiae in HPLC fingerprint profiles though they were of good similarity.CONCLUSION: The HPLC fingerprints of liposoluble constituents were obtained with good resolution under the experimental chromatographic system.Three pure chromatographic peaks of chrysophanol,emodin and physcion have been identified.More reliable cluster result can be obtained from two-dimension information data at full wavelength 220 nm～550 nm than from the whole information of single-wavelength chromatographic fingerprint or from the information of chromatographic fingerprint of characteristic peaks.

Objective To study the growth inhibitory effect of chemotherapeutic drugs on the pancreatic cancer cell line Aspc-1 and Bxpc-3, and the relations to the varied concentration and exposere time of chemotherapeutic drugs administrated in single or in combination. Methods Four chemotherapeutic drugs included 5-fluorouracil (5-FU), epirubicin (E-ADM), mitomycin(MMC) or cisplatin (DDP) administrating in single or in combination and using varied concentrations(d1、d2、d3 and d4) and exposure times(24、28 and 72 hours); and then the growth inhibitory effect on the two cell lines. resulted from these drugs were assayed by MTT colorimetry and analysed by “ t ” test. Results The growth inhibitory rate of two cell lines was increased, with the increment of drug concentration and/or the prolongation of exposure time ( P

OBJECTIVETo investigate the principle and basis about the chromatographic fingerprint peak matching of Semen Cassiae by the asymptotic window orthogonal projection analytical method.

METHODThe samples of Semen Cassiae were hydrolyzed in the 1.5 mol x L(-1) hydrochloride acid and then reflux extracted with chloroform. The chromatographic condition was that the HPLC was run on Agilent 1100 column, Zorbax Eclipse XDB-C18 (4.6 mm x 250 mm, 5 microm). The protected column was Scienhome C18 column (3.0 mm x 20 mm, 5 microm) with acetonitrile-water (0.1% phosphoric acid) as mobile phase in gradient elution at a flow rate of 1.0 mL x min(-1). The detection wavelength and reference wavelength were 278 nm and 550 nm, respectively.

RESULTThe characteristic fingerprint collection of illustrative plates of Semen Cassiae were obtained with different HPLC instruments and chromatographic columns. And the asymptotic window orthogonal projection analytical method was used to decide the chromatographic fingerprint peak matching of Semen Cassiae, promptly and prapidly.

CONCLUSIONThe asymptotic window orthogonal projection analytical method can progress the matching of different fingerprint collection of illustrative plates peak matching well and truly.

COVID-19 ; Drugs, Chinese Herbal/therapeutic use* ; Humans ; Molecular Docking Simulation ; SARS-CoV-2 ; Technology

Objective To explore the therapeutic effect of transdermal patches containing Cassia seed extract applied at the navel on slow transit constipation (STC) in rats and explore the spectrum-effect relationship of the patches. Method In a STC rat model established by gavage of compound diphenoxylate suspension for 14 days, the transdermal patches containing low, medium and high doses of Cassia seed extract (41.75, 125.25, and 375.75 mg/kg, respectively) were applied at the Shenque acupoint on the abdomen for 14 days after modeling, with constipation patches (13.33 mg/kg) as the positive control. After the treatment, fecal water content and intestinal propulsion rate of the rats were calculated, the pathological changes in the colon were observed with HE staining. Serum NO and NOS levels and the total protein content and NO, NOS and AChE expressions in the colon tissue were determined. HPLC fingerprints of the transdermal patches were established, and the spectrum-effect relationship between the common peaks of the patches and its therapeutic effect were analyzed. Results Treatment with the transdermal patches containing Cassia seed extract significantly increased fecal water content and intestinal propulsion rate of the rat models, where no pathological changes in the colon tissue were detected. The treatment also suppressed the elevations of serum and colonic NO and NOS levels and reduction of AChE in STC rats. Twenty-eight common peaks were confirmed in the HPLC fingerprints of 6 batches of Cassia seed extract-containing patches. Analysis of the spectrum-effect relationship showed that autrantio-obtusin had the greatest contribution to the therapeutic effect of the patches in STC rats. Conclusion The Cassia seed extract-containing patches alleviates STC in rats via synergistic actions of multiple active ingredients in the extract, where autrantio-obtusin, rhein, chrysoobtusin, obtusin, obtusifolin, emodin, chrysophanol, and physcion are identified as the main active ingredients.

Objective To explore the therapeutic effect of transdermal patches containing Cassia seed extract applied at the navel on slow transit constipation (STC) in rats and explore the spectrum-effect relationship of the patches. Method In a STC rat model established by gavage of compound diphenoxylate suspension for 14 days, the transdermal patches containing low, medium and high doses of Cassia seed extract (41.75, 125.25, and 375.75 mg/kg, respectively) were applied at the Shenque acupoint on the abdomen for 14 days after modeling, with constipation patches (13.33 mg/kg) as the positive control. After the treatment, fecal water content and intestinal propulsion rate of the rats were calculated, the pathological changes in the colon were observed with HE staining. Serum NO and NOS levels and the total protein content and NO, NOS and AChE expressions in the colon tissue were determined. HPLC fingerprints of the transdermal patches were established, and the spectrum-effect relationship between the common peaks of the patches and its therapeutic effect were analyzed. Results Treatment with the transdermal patches containing Cassia seed extract significantly increased fecal water content and intestinal propulsion rate of the rat models, where no pathological changes in the colon tissue were detected. The treatment also suppressed the elevations of serum and colonic NO and NOS levels and reduction of AChE in STC rats. Twenty-eight common peaks were confirmed in the HPLC fingerprints of 6 batches of Cassia seed extract-containing patches. Analysis of the spectrum-effect relationship showed that autrantio-obtusin had the greatest contribution to the therapeutic effect of the patches in STC rats. Conclusion The Cassia seed extract-containing patches alleviates STC in rats via synergistic actions of multiple active ingredients in the extract, where autrantio-obtusin, rhein, chrysoobtusin, obtusin, obtusifolin, emodin, chrysophanol, and physcion are identified as the main active ingredients.

OBJECTIVE: To explore the target, signaling pathways and their biological functions of Decoction in the treatment of COVID-19 based on network pharmacology and molecular docking technology. METHODS: The active components and target proteins in 21 drugs such as and in decoction were analyzed, and the signaling pathways and biological functions of the target proteins common with COVID-19 were screened by using TCMSP, Swiss Target Prediction, CooLGeN, GeneCards, DAVID and other databases. The network diagram of decoction was constructed using Gephi software. RESULTS: We identified 163 active ingredients, including MOL004798, MOL000519, MOL004824, MOL000554, MOL010428, and MOL013443, from 18 drugs in decoction (such as , , , , and ). These ingredients activate renin-angiotensin system signaling pathway and apoptosis signaling pathway by regulating 10 protein targets (ACE, ACE2, AGTR1, FURIN, TNF, CASP3, CASP6, DPP4, MCL1 and POLD1) to execute 42 biological functions such as renin-angiotensin regulation of blood volume and systemic arterial blood pressure to treat COVID-19. The results of preliminary molecular docking showed that MOL000519 (from ), MOL000554 (from ), MOL004798 (from ), MOL004824 (from ), MOL010428 (from ), and MOL013443 (from ) had good affinity with SARS-CoV-2 3CL hydrolase to form complexes with stable conformations and high binding activity (binding energy ≤- 5 kJ/mol). CONCLUSIONS decoction can treat COVID-19 through its multiple medicinal ingredients that have multiple targets and involve multiple signaling pathways for different biological functions. Our finding provides reference for further investigation into the pharmacological mechanism of decoction in treating COVID-19.
Betacoronavirus ; Coronavirus Infections ; drug therapy ; Drugs, Chinese Herbal ; Humans ; Molecular Docking Simulation ; Pandemics ; Pneumonia, Viral ; drug therapy

OBJECTIVE: To study the plasma concentration and pharmacokinetics of 3, 29-Dibenzoyl Karounitriol (3, 29-DK) from sustained- release pellets and extracts of Trichosanthes at different time points in rats using high-performance liquid chromatography- tandem mass spectrometry (LC-MS/MS). METHODS: Healthy male SD rats were given a single gavage of Trichosanthes sustained-release pellets or Trichosanthes extract, and orbital blood samples were taken at different time points within 48 h after drug administration in the pellet group and within 5 h in Trichosanthes extract group for determination of the plasma concentrations of 3, 29-DK using LC-MS/MS. The standard curve of 3, 29-DK content was established, and the specificity, minimum detection limit, precision and accuracy, extraction recovery, stability and matrix effect of LC-MS/MS analysis were assessed. The mean plasms levels of 3, 29-DK at different time points after the drug administration were determined and its pharmacokinetic parameters were calculated using Das 2.0 software. RESULTS: LC-MS/MS analysis showed a good linearity of 3, 29-DK concentration within the range of 0.5-32 ng/mL, and the results of methodological validation confirmed the validity of this method for biological sample determination. Trichosanthes sustained-release pellets and Trichosanthes extract showed significant differences in their AUC, AUC, MRT, MRT, t and T of 3, 29-DK after administration in rats ( < 0.05). CONCLUSIONS Trichosanthes sustained-release pellets are capable of sustained-release of 3, 29-DK in rats, and thus provides a basis for the study of new dosage forms of Trichosanthes.
Animals ; Area Under Curve ; Benzoates ; pharmacokinetics ; Chromatography, Liquid ; Delayed-Action Preparations ; Male ; Rats ; Rats, Sprague-Dawley ; Reproducibility of Results ; Tandem Mass Spectrometry ; Trichosanthes ; chemistry

Infective endocarditis is a microbial infection of the endocardium and can easily affect heart valve.Its characteristic lesion is vegetation formation,and the shedding of vegetation results in arterial embolism and ischemic necrosis of corresponding tissues and organs.A case of infective endocarditis with multiple extracardiac complications was described in this article.The characteristic ultrasound finding was the vegetation formation in anterior mitral valve.CT and MRI scans revealed involvements in multiple organs and blood vessels,which were manifested as splenic infarction,renal infarction,cerebral infarction,splenic aneurysm,superior mesenteric artery aneurysms,renal artery aneurysms,and distal segment stenosis and occlusion of right middle cerebral artery.
Embolism ; Endocarditis ; Endocarditis, Bacterial ; Humans ; Infarction ; Mitral Valve

OBJECTIVE: To study the plasma concentration and pharmacokinetics of 3, 29-Dibenzoyl Karounitriol (3, 29-DK) from sustained- release pellets and extracts of Trichosanthes at different time points in rats using high-performance liquid chromatography- tandem mass spectrometry (LC-MS/MS). METHODS: Healthy male SD rats were given a single gavage of Trichosanthes sustained-release pellets or Trichosanthes extract, and orbital blood samples were taken at different time points within 48 h after drug administration in the pellet group and within 5 h in Trichosanthes extract group for determination of the plasma concentrations of 3, 29-DK using LC-MS/MS. The standard curve of 3, 29-DK content was established, and the specificity, minimum detection limit, precision and accuracy, extraction recovery, stability and matrix effect of LC-MS/MS analysis were assessed. The mean plasms levels of 3, 29-DK at different time points after the drug administration were determined and its pharmacokinetic parameters were calculated using Das 2.0 software. RESULTS: LC-MS/MS analysis showed a good linearity of 3, 29-DK concentration within the range of 0.5-32 ng/mL, and the results of methodological validation confirmed the validity of this method for biological sample determination. Trichosanthes sustained-release pellets and Trichosanthes extract showed significant differences in their AUC, AUC, MRT, MRT, t and T of 3, 29-DK after administration in rats ( < 0.05). CONCLUSIONS Trichosanthes sustained-release pellets are capable of sustained-release of 3, 29-DK in rats, and thus provides a basis for the study of new dosage forms of Trichosanthes.
Animals ; Chromatography, High Pressure Liquid ; Delayed-Action Preparations ; Male ; Rats ; Rats, Sprague-Dawley ; Reproducibility of Results ; Tandem Mass Spectrometry ; Trichosanthes