The evaluation of the safety and therapeuctic efficacy of CV.artecan (dihydroartemisinin 40mg - piperaquine 320mg) combination in experimental mice. LD50 dose of CV.artecan were identified in experimental mice. In vitro test was carried out on mice injected P.berghei (chloroquine resistant isolate) treated with various doses of CV.artecan: 115.2mg/kg; 230.4mg/kg; 460.8mg/kg and 921.6mg/kg. In vivo tests of CV.artecan with the total doses of 6.2/51.2mg/kg in 137 patients with uncomplicated malaria.Therapeutic dose of adults in the first day: 4 tablets divided into 2 times, the first day and second day: 2 tablets per day, the children doses acorrding to age. The patients were followed up for 28 days. The results: The dose LD50 of CV.artecan was identified as 2167mg/kg (2129-2205mg/kg). The total dose of CV.artecan 57mg/kg in malaria patients was far duration from LD50 doses
malaria ; therapeutics ; therapy ; Artemisinins ; Quinolines

Three compounds, including scolosprine C(1), uracil(2) and hypoxanthine(3), were isolated and purified from the ethyl acetate fraction of centipede by silica gel normal-phase column chromatography, reversed-phase medium pressure preparation chromatography, and high-pressure semi-preparative HPLC. The structure was elucidated through a combination of spectroscopic analyses [such as nuclear magnetic resonance(NMR) and mass spectrometry(MS)] and literature review. Among them, compound 1 was a new quinoline alkaloid. In previous reports, we have described the isolation and structure elucidation of one new and two known quinoline alkaloids. In this paper, we would report the isolation and structure elucidation of scolosprine C in detail.
Alkaloids ; Animals ; Arthropods ; Chilopoda ; Quinolines

Background: Infection with Mycobacterium tuberculosis, the causative agent of TB, is responsible for one of the global epidemics. Thus, new drugs are needed that do not confer cross-resistance with currently administered front-line therapeutics. Quinoline-based natural products and synthetic derivatives have been extensively explored for antitubercular activity.
Objective: The main goal of this study was to prepare a collection of benzylated 8-hydroxyquinoline derivatives through synthesis and assess their antitubercular activity along with a molecular docking study to clarify their biological mechanism of action.
Methodology: The benzylated 8-hydroxyquinoline derivatives were synthesized using Williamson synthesis methods. Antitubercular activity was assessed against fast replicating M. tuberculosis H??Rv using Microplate Alamar Blue Assay (MABA) and non-replicating cultures using Low-Oxygen Recovery Assay (LORA). Molecular docking studies were carried out against enoyl-acyl carrier protein reductase (InhA).
Results: Five benzylated 8-hydroxyquinoline derivatives were synthesized in moderate yields and characterized using NMR spectroscopy. MABA and LORA assays indicate compounds 3-5 as the most inhibitory derivatives with MIC90's ranging from 6.38 to 54.28 ?M. Molecular docking against InhA showed modest 90 binding energies for compounds 4 (-8.5 kcal/mol) and 5 (-8.6 kcal/mol).
Conclusion: Findings suggest a rationale for the further evolution of this promising series of antitubercular quinoline small molecules. Structure-activity analysis shows that an 8-benzyl moiety with chlorine atom/s is important for improved activity against replicating and non-replicating M. tb. H??Rv. This is also supported by our in silico studies.

OBJECTIVE: To study the association of cytoplasmic phospholipase A2 (PLA2G4) rs932476 polymorphism with the development of bronchial asthma and the response to montelukast, a leukotriene receptor antagonist, in children. METHODS: A total of 128 children with bronchial asthma were enrolled as case group, and 100 healthy children were enrolled as control group. The genotype and allele frequencies of PLA2G4 rs932476 were compared between the two groups. The children in the case group were administered with montelukast except routine treatment for 2 months, and the changes in serum levels of leukotriene B4 (LTB4), interleukin-4 (IL-4), immunoglobulin E (IgE), and interferon gamma (IFN-γ), pulmonary function and fractional exhaled nitric oxide (FeNO) after treatment were observed. RESULTS: There were no significant differences in the genotype and allele frequencies of PLA2G4 rs932476 between the case and control groups, as well as between the groups with different severities of asthma (P>0.05). After treatment, the children with AA genotype had a significantly higher overall response rate than those with GG genotype. After treatment, the case group had significant reductions in the serum levels of IgE and IL-4 and a significant increase in the level of IFN-γ (P<0.05). After treatment, the children with GG genotype had a higher serum level of IL-4 and a lower level of IFN-γ than those with AA genotype. After treatment, the case group had significant increases in pulmonary function parameters, and the children with AA genotype had significantly higher parameters than those with GG genotype. The case group had a significant reduction in the level of FeNO, and the children with AA genotype had a significantly lower level than those with GG genotype after treatment. The case group had a significantly higher serum level of LTB4 than the control group before treatment (P<0.05). After treatment the case group had a significant reduction in the serum level of LTB4 (P<0.05). The children with GG genotype had a significantly higher level of LTB4 than those with AA genotype after treatment (P<0.05). CONCLUSIONS PLA2G4 rs932476 polymorphism is not associated with the susceptibility and severity of bronchial asthma in children, but it may has certain influence on children's response to the leukotriene receptor antagonist montelukast, possibly by affecting the level of LTB4.
Acetates ; Asthma ; Child ; Humans ; Leukotriene Antagonists ; Quinolines

Delayed pressure urticria is a type of physical urticaria, characterized by the appearance of painful swelling for a few hours after physical stimulus. A 27-year-old woman suffered from pressure urticaria for eight months. The patient was unresponsive to conventional antihistamine, glucocorticoid, cyclosporine and azathioprine. Since the patient was treated with 10 mg/day montelukast and 1 mg/day ketotifen for 10 months, erythema and wheals have not developed. We report a case of pressure urticaria treated with a leukotriene inhibitor.
Acetates ; Adult ; Azathioprine ; Cyclosporine ; Erythema ; Female ; Humans ; Ketotifen ; Quinolines ; Urticaria

A strategy combining collision cross section(CCS) prediction and quantitative structure-retention relationship(QSRR) model for quinoline and isoquinoline alkaloids was established based on UHPLC-IM-Q-TOF-MS and applied to Phellodendri Chinensis Cortex and Phellodendri Amurensis Cortex. The strategy included the following three steps.(1) The molecular features were extracted by the "find features" algorithm.(2) The potential quinoline and isoquinoline alkaloids were screened by filtering the original characteristic ions extracted from Phellodendri Chinensis Cortex and Phellodendri Amurensis Cortex by the established CCS vs m/z prediction interval.(3) According to the retention time of candidate compounds predicted by QSRR model, the chemical constituents were identified in combination with the characteristic fragment ions and pyrolysis law of secondary mass spectrometry. With the strategy, a total of 80 compounds were predicted, and 15 were identified accurately. The strategy is effective for the identification of small analogs of traditional Chinese medicine.
Chromatography, High Pressure Liquid ; Algorithms ; Alkaloids ; Isoquinolines ; Quinolines

PURPOSE: This study assessed the association between the ratio of leukotriene E4 (LTE4) to fractional exhaled nitric oxide (FENO) in the response of children with exercise-induced bronchoconstriction (EIB) enrolled in a therapeutic trial with montelukast or inhaled corticosteroid (fluticasone propionate [FP]). METHODS: Children aged 6 to 18 years with EIB were randomized in a 4-week, placebo-controlled, double-blinded trial with montelukast or FP. Before and after treatment, treadmill exercise challenges were performed. The LTE4 levels in the induced sputum and urine and the FENO levels were measured in subjects before and 30 minutes after the exercise challenges. The same tests were conducted after treatment. RESULTS: A total of 24 patients completed the study: 12 in the montelukast group and 12 in FP group. Both study groups displayed a similar postexercise maximum decrease in forced expiratory volume in one second (FEV1) before treatment as well as after treatment. However, there were significant differences in the magnitude of change between the two (Delta; -18.38+/-14.53% vs. -4.67+/-8.12% for the montelukast and FP groups, respectively; P=0.021). The Delta logarithmic sputum baseline and postexercise LTE4/FENO ratio were significantly lower in the montelukast group than in the FP group (baseline; -0.09+/-0.21 vs. -0.024+/-0.03, P=0.045; postexercise, -0.61+/-0.33 vs. -0.11+/-0.28, P=0.023). CONCLUSIONS: These data indicate that the efficacy of montelukast for preventing a maximum decrease in FEV1 after exercise is significantly higher than that of FP, and the high LTE4/FENO ratio is associated with a greater response to montelukast than to FP for EIB therapy. These results suggest that LTE4 may play an important role in EIB.
Acetates ; Aged ; Bronchoconstriction ; Child ; Diethylpropion ; Forced Expiratory Volume ; Humans ; Leukotriene E4 ; Nitric Oxide ; Quinolines ; Sputum

PURPOSE: Relapsing polychondritis is an uncommon systemic autoimmune disorder which is characterized by recurrent and often progressive inflammatory episodes involving multiple organ systems, including the ophthalmic, otorhinolaryngeal, respiratory, musculoskeletal, renal, cardiovascular, and dermatologic systems. The most common ocular manifestations are episcleritis and scleritis. Uveitis, especially the nongranulomatous type, has been reported in 3% to 22% of relapsing polychondritis cases. We report uncommon hypopyon uveitis as an ophthalmic finding associated with relapsing polychondritis. CASE SUMMARY: A 56-year-old woman with known relapsing polychondritis presented with ocular pain and redness in the right eye which had developed two months before and was managed for scleritis. However, she developed blurred vision, and hypopyon and vitreous opacity was found. The patient presented to our clinic and we diagnosed her with hypopyon uveitis associated with relapsing polychondritis. The patient was started on systemic steroid therapy consisting of 1% prednisolone acetate, 0.5% moxifloxacin, and 0.5% tobramycin in the right eye. Hypopyon disappeared 8 days following the initiation of treatment, and all symptoms had resolved after 14 days.
Aza Compounds ; Eye ; Female ; Humans ; Middle Aged ; Polychondritis, Relapsing ; Prednisolone ; Quinolines ; Scleritis ; Tobramycin ; Uveitis ; Vision, Ocular

PURPOSE: To report the clinical results of moxifloxacin mixed augmented amniotic membrane transplantation (AMT) in 2 patients with perforating infectious keratitis. CASE SUMMARY: Moxifloxacin mixed augmented amniotic membrane transplantations were performed in 2 patients with rapidly deteriorating deep perforated bacterial keratitis. All patients preserved their eyesight. Complete re-epithelization over the amniotic membrane were observed within a month. The corneal surfaces were healed with opacity, and there were no active infectious infiltrations or recurrences for 3 months after application. CONCLUSIONS: Moxifloxacin mixed augmented AMT has proven to be successful both tectonically and physiologically for cases with perforating active bacterial keratitis.
Amnion ; Aza Compounds ; Corneal Perforation ; Corneal Ulcer ; Fibrin Tissue Adhesive ; Humans ; Keratitis ; Quinolines ; Recurrence ; Transplants

PURPOSE: To report a case of fusarium keratitis treated with only moxifloxacin 0.5% ophthalmic solution (Vigamox(R), Alcon Laboratories, Inc., Ft Worth, TX, USA). CASE SUMMARY: A 37-year-old healthy male patient experienced a right eye injury due to grain 7 days prior to presentation at our hospital with visual disturbance and ocular pain. A 2.7 x 4.3 mm sized corneal epithelial defect with irregular featherlike midstromal infiltration was observed, and slit lamp examination revealed a dry, rough texture. Thus a smear and culture were performed. Moxifloxacin 0.5% ophthalmic solution (Vigamox(R)) and lubricant were applied for treatment. Three days after using the eye solution, all clinical features improved. Seven days later, Fusarium species was identified in culture. CONCLUSIONS: As standard treatment for Fusarium, the authors of the present study used an antifungal agent. Although hyphae were detected in culture, the use of only moxifloxacin 0.5% ophthalmic solution (Vigamox(R)) result in a satisfactory result and improvement in clinical features.
Adult ; Aza Compounds ; Edible Grain ; Eye ; Eye Injuries ; Fusarium ; Humans ; Hyphae ; Keratitis ; Male ; Quinolines