ABSTRACT
Four new compounds (1-4), together with 23 known compounds (5-27), were isolated from the whole plant of Taraxacum mongolicum. Among them, one racemic mixture (4) was separated with a chiral HPLC column. Their structures were identified by spectroscopic evidence and mass spectrometry. The absolute configurations of compounds 1, 3, and 4 were determined via comparison of their calculated and experimental electronic circular dichroism (ECD) spectra. Compound 3 showed an inhibitory effect against aldose reductase with a 59.1% inhibition. Two known compounds (13 and 27) showed α-glucosidase inhibition of 51.5% and 56.0%, respectively.
Subject(s)
Alkaloids , Sesquiterpenes , Taraxacum , Taraxacum/chemistry , Furaldehyde , Molecular Structure , Phenols/pharmacology , Alkaloids/pharmacology , Circular Dichroism , Sesquiterpenes/pharmacologyABSTRACT
Eight previously undescribed compounds, two quinones (1-2), one sesquiterpene (3), and five phenol compounds (4-8), including three enantiomers (6a, 7a, and 8a), along with three corresponding known enantiomers (6b-8b) were isolated from the aerial parts of Morinda umbellata L. Their structures were elucidated by 1D and 2D NMR spectroscopy, X-ray diffraction, and experimental and calculated ECD spectra, respectively. Compound 5 was found to have weak cytotoxity, which inhibited the growth of seven human cancer cell lines (A2780, HeLa, MCF-7, BGC-823, H7420, Ketr3 and SW 1990) with IC50 values from 13.3 to 15.1 µM.
Subject(s)
Cytotoxins/toxicity , Morinda/chemistry , Phenols/toxicity , Quinones/toxicity , Sesquiterpenes/toxicity , Cell Line, Tumor , Chromatography, High Pressure Liquid , Crystallography, X-Ray , Cytotoxins/isolation & purification , Humans , Inhibitory Concentration 50 , Magnetic Resonance Spectroscopy , Phenols/isolation & purification , Plant Components, Aerial/chemistry , Plant Extracts/isolation & purification , Plant Extracts/toxicity , Quinones/isolation & purification , Sesquiterpenes/isolation & purificationABSTRACT
Fifteen new water-soluble alkaloids were obtained from the fresh herbs of Portulaca oleracea L. The structures of 15 alkaloids 1-15 were established according to spectroscopic data, and the stereoconfigurations were determined based on experimental and calculated electronic circular dichroism (ECD) data and single crystal X-ray diffraction. Alkaloids 1-15 were found to display good anti-inflammatory activity at 10 µM and could significantly reduce the interleukin-6 (IL-6) and nitric oxide (NO) levels induced by lipopolysaccharide (LPS) in RAW 264.7 macrophages.
Subject(s)
Alkaloids/chemistry , Anti-Inflammatory Agents/chemistry , Portulaca/chemistry , Alkaloids/isolation & purification , Alkaloids/pharmacology , Alkaloids/therapeutic use , Animals , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Crystallography, X-Ray , Edema/chemically induced , Edema/drug therapy , Edema/pathology , Interleukin-6/metabolism , Lipopolysaccharides/pharmacology , Macrophages/cytology , Macrophages/drug effects , Macrophages/metabolism , Male , Mice , Molecular Conformation , Nitric Oxide/metabolism , Plant Extracts/chemistry , Portulaca/metabolism , RAW 264.7 Cells , Solubility , Water/chemistryABSTRACT
BACKGROUND: General anesthesia combining with a caudal block (CB) has been commonly performed in pediatric patients undergoing circumcision surgeries. However, some severe complications have been suspected of a caudal block in the combined use. To avoid these issues of a caudal block, this study introduces a novel dorsal penile nerve block (DPNB) via perineum guided by ultrasound as an alternative to a caudal block in pediatric circumcision surgeries. METHODS: A total of 104 pediatric patients scheduled for circumcision surgeries were involved and randomly divided into 2 groups: the CB group (n=52) and the DPNB group (n=52). A laryngeal mask was inserted followed by induction and maintenance anesthesia of inhaled sevoflurane. In the DPNB group, a dorsal penile nerve block (DPNB) guided by a real-time ultrasonography was performed by a single injection via perineum of 0.25% ropivacaine plus 0.8% lidocaine with total injection volume of 3-5ml. In the CB group, a dose of 0.5 ml/kg was given via the caudal canal following the same general anesthesia with that of Group DPNB. The time to the first analgesic demand after surgery is the key data collected for comparing between the two study groups. Heart rates and respiratory rates changes before and during the surgical procedure, pain score when leaving the PACU, and the time taken for the first micturition after a surgery were also recorded to analyze the differences in analgesic effects between the CB and DPNB groups. RESULTS: No significant difference in heart rates and respiratory rates was found between the two groups before and during the surgery. Pain scores were similar before pediatric patients leave the PACU. However, the time taken for the first micturition after a surgery in Group DPNB is shorter than Group CB. The patients in Group DPNB asked for analgesics later than those in Group CB. Additionally, no significant differences in adverse effects were noted between two groups except the numbness of the lower limbs occurring less in Group DPNB. CONCLUSIONS: The ultrasound-guided dorsal penile nerve block via perineal approach can basically act as a safe and effective alternative to the caudal block in pediatric patients undergoing circumcision surgeries. Clinical Trials identifier is ChiCTR-IPR-15006670. Protocol is available at http://www.chictr.org.cn/showproj.aspx?proj=11319.