Noise-induced hearing loss(NIHL)is primarily driven by inflammatory processes within the cochlea,where noise exposure triggers the activation of the NOD-like receptor protein 3(NLRP3)inflammasome,leading to an inflamm...Noise-induced hearing loss(NIHL)is primarily driven by inflammatory processes within the cochlea,where noise exposure triggers the activation of the NOD-like receptor protein 3(NLRP3)inflammasome,leading to an inflammatory cascade.The interaction between increased NLRP3 expression and NF-κB activity can further amplify cochlear inflammation.Our findings reveal that(R)-PFI-2 hydrochloride,a selective inhibitor of the SETD7 enzyme,effectively inhibits the activation of the cochlear NF-κB pathway,suppresses the release of proinflammatory factors,and prevents inflammasome assembly.This intervention disrupts the perpetuating cycle of inflammation,thereby alleviating damage to cochlear hair cells attributed to acoustic trauma.Consequently,(R)-PFI-2 hydrochloride emerges as a promising pharmacological candidate for NIHL,targeting and moderating the excessive immune and inflammatory responses implicated in the pathology of hearing loss.展开更多
The new method proposed is based on the formation of hydralazine-Bromophenol blue ion pair simply and without further extraction or heating. The ion pair was prepared in the presence of pH 3 citrate buffer forming a y...The new method proposed is based on the formation of hydralazine-Bromophenol blue ion pair simply and without further extraction or heating. The ion pair was prepared in the presence of pH 3 citrate buffer forming a yellow-colored chromogen. A new maximum UV-visible band formed at 416 nm. The color was stable for more than 10 hours and obeyed Beer’s Law over the concentration range of 10 - 50 µg/mL. The calculated molar absorptivity and Sandell’s sensitivity were 1.01 × 104 L∙mol−1∙cm−1 and 0.0514 µg/mL, respectively. The elements of method validation stipulated by The International Conference on Harmonization [Q2 (R1)] were applied for hydralazine hydrochloride assay in pure and pharmaceutical tablet formulation. The average recoveries of the pure solution and the pharmaceutical formulation were 98.94% and 99.50%, respectively. The results were statistically compared by F-test, which indicates that the method can be precise and repeatable for both pure and pharmaceutical solutions. The method was found to be accurate, reproducible, and cost-effective, and validated for the assay of hydralazine in terms of the routine quality control.展开更多
BACKGROUND Epidermal growth factor receptor(EGFR)tyrosine-kinase inhibitors are widely used for the treatment of non-small-cell lung cancer with EGFR mutations.However,patients with rare,even compound EGFR mutations h...BACKGROUND Epidermal growth factor receptor(EGFR)tyrosine-kinase inhibitors are widely used for the treatment of non-small-cell lung cancer with EGFR mutations.However,patients with rare,even compound EGFR mutations have different responses to EGFR-tyrosine-kinase inhibitors,which bring uncertainty to clinical treatment.CASE SUMMARY A 45-year-old female patient presented with a 3-mo history of cough and white sputum without chest pain.Chest computed tomography revealed lung spaceoccupying lesions and multiple lymphadenectasis.Bronchoscopy and pathology suggested lung adenocarcinoma.Compound variation of EGFR gene(exon 21 L858 R/V834 L)was detected in both tissue and circulating tumor deoxyribonucleic acid samples.As a result of next-generation sequencing and her family’s wishes,the patient was given oral treatment with icotinib hydrochloride(125 mg/d,tid)from March 21,2019 and has achieved stable disease for the last 1 year.CONCLUSION Non-small cell lung adenocarcinoma with EGFR L858 R/V834 L was treated successfully with icotinib,and it may be a new medication treatment option.展开更多
Chiral amino acids and their corresponding amino alcohols bearing camphoric backbone were prepared from D-（＋）-camphoric imide and characterized by infrared, elemental analysis, ESI-MS, and NMR measurements. Among t...Chiral amino acids and their corresponding amino alcohols bearing camphoric backbone were prepared from D-（＋）-camphoric imide and characterized by infrared, elemental analysis, ESI-MS, and NMR measurements. Among them, one intermediate （1S,3R）-3-amino-2,2,3- trimethyl cyclopentane-1-carboxylic acid hydrochloride 3 was structurally elucidated by X-ray diffraction techniques. Versatile intermolecular hydrogen bonding interactions observed in its packing structure result in a two-dimensional framework.展开更多
Four simple, sensitive and accurate spectrophotometric methods have been developed for the determination of some calcium channel blockers: Amlodipine besylate (ADB), Diltiazem hydrochloride (DTZ) and Verapamil hydroch...Four simple, sensitive and accurate spectrophotometric methods have been developed for the determination of some calcium channel blockers: Amlodipine besylate (ADB), Diltiazem hydrochloride (DTZ) and Verapamil hydrochloride (VPM) in pharmaceutical formulations. These methods based on formation ion pair complexes with Sulfochlorophenol-S (SCPS), Bromopyrogallol red (BPR), Eriochromecyanine- R (ECC) and Pyrocatechol violet (PCV) in acidic medium. The colored products are extracted with chloroform and measured spectrophoto- metrically at 462, 600, 440 and 442 for ECC, SCPS, BPR and PCV, respectively. Beer’s low was obeyed in the concentration range, for ECC: 25 - 175 μg·ml-1, 50 - 150 μg·ml-1 or 100 - 250 μg·ml-1, for SCPS: 300 - 800 μg·ml-1, 200 - 700 μg·ml-1 or 100 - 550 μg·ml-1, for BPR: 50 - 400 μg·ml-1, 200 - 700 μg·ml-1 or 200 - 700 μg·ml-1 for VPM, DTZ or ADB, respectively and for PCV: 50 - 250 μg·ml-1 for VPM or 200 - 500 μg·ml-1 for DTZ with molar absorptivity, for ECC: 2.2 × 104, 2.1 × 104, 1.6 × 104 L·mol-1·cm-1, for SCPS: 3.8 × 103, 5.6 × 103, 8.1 × 103 L·mol-1·cm-1, for BPR: 11 × 103, 4.8 × 103, 6.9 × 103 L·mol-1·cm-1 for VPM, DTZ or ADB, respectively and for PCV: 19.5 × 103 L·mol-1·cm-1 for VPM and 6.6 × 103 L·mol-1·cm-1 for DTZ and relative standard deviation, for ECC: 0.76%, 0.86%, 0.46%, for SCPS: 0.94%, 0.96%, 0.86%, for BPR: 0.96%, 0.95%, 0.55% for VPM, DTZ or ADB, respectively and for PCV: 0.81% for VPM and 0.65% for DTZ. These methods have been successfully applied for the assay of drug in pharmaceutical formulations. No interference was observed from common pharmaceutical adjuvants. Statistical comparison of the results with the reference method shows excellent agreement and indicates no significant difference in accuracy and precision.展开更多
A novel and simple procedure for the enantiospecific synthesis of penehyclidine hydrochloride （8018） isomers and the R configuration derivatives was described. The intramolecular asymmetric cyclization of the monosu...A novel and simple procedure for the enantiospecific synthesis of penehyclidine hydrochloride （8018） isomers and the R configuration derivatives was described. The intramolecular asymmetric cyclization of the monosulfonate of compound 1,2-diol was applied to the execution of the synthesis of the key chiral building block for the first time. The aimed products were obtained with moderate yield in〉99% ee.展开更多
基金supported by the Science and Technology Development Project of Xuzhou Science and Technology Bureau(KC21249)Science and Technology Development Project of Chongqing(CSTB2022NSCQ-M SX1598)+2 种基金Science and Technology Development Project of Xiaogan(XGKJ2023010010)Scientific Research Startup Foundation of Hainan UniversityScience and Technology Development Project of Hainan.
文摘Noise-induced hearing loss(NIHL)is primarily driven by inflammatory processes within the cochlea,where noise exposure triggers the activation of the NOD-like receptor protein 3(NLRP3)inflammasome,leading to an inflammatory cascade.The interaction between increased NLRP3 expression and NF-κB activity can further amplify cochlear inflammation.Our findings reveal that(R)-PFI-2 hydrochloride,a selective inhibitor of the SETD7 enzyme,effectively inhibits the activation of the cochlear NF-κB pathway,suppresses the release of proinflammatory factors,and prevents inflammasome assembly.This intervention disrupts the perpetuating cycle of inflammation,thereby alleviating damage to cochlear hair cells attributed to acoustic trauma.Consequently,(R)-PFI-2 hydrochloride emerges as a promising pharmacological candidate for NIHL,targeting and moderating the excessive immune and inflammatory responses implicated in the pathology of hearing loss.
文摘The new method proposed is based on the formation of hydralazine-Bromophenol blue ion pair simply and without further extraction or heating. The ion pair was prepared in the presence of pH 3 citrate buffer forming a yellow-colored chromogen. A new maximum UV-visible band formed at 416 nm. The color was stable for more than 10 hours and obeyed Beer’s Law over the concentration range of 10 - 50 µg/mL. The calculated molar absorptivity and Sandell’s sensitivity were 1.01 × 104 L∙mol−1∙cm−1 and 0.0514 µg/mL, respectively. The elements of method validation stipulated by The International Conference on Harmonization [Q2 (R1)] were applied for hydralazine hydrochloride assay in pure and pharmaceutical tablet formulation. The average recoveries of the pure solution and the pharmaceutical formulation were 98.94% and 99.50%, respectively. The results were statistically compared by F-test, which indicates that the method can be precise and repeatable for both pure and pharmaceutical solutions. The method was found to be accurate, reproducible, and cost-effective, and validated for the assay of hydralazine in terms of the routine quality control.
文摘BACKGROUND Epidermal growth factor receptor(EGFR)tyrosine-kinase inhibitors are widely used for the treatment of non-small-cell lung cancer with EGFR mutations.However,patients with rare,even compound EGFR mutations have different responses to EGFR-tyrosine-kinase inhibitors,which bring uncertainty to clinical treatment.CASE SUMMARY A 45-year-old female patient presented with a 3-mo history of cough and white sputum without chest pain.Chest computed tomography revealed lung spaceoccupying lesions and multiple lymphadenectasis.Bronchoscopy and pathology suggested lung adenocarcinoma.Compound variation of EGFR gene(exon 21 L858 R/V834 L)was detected in both tissue and circulating tumor deoxyribonucleic acid samples.As a result of next-generation sequencing and her family’s wishes,the patient was given oral treatment with icotinib hydrochloride(125 mg/d,tid)from March 21,2019 and has achieved stable disease for the last 1 year.CONCLUSION Non-small cell lung adenocarcinoma with EGFR L858 R/V834 L was treated successfully with icotinib,and it may be a new medication treatment option.
基金This work was funded by the National Natural Science Foundation of China (No. 20301009)
文摘Chiral amino acids and their corresponding amino alcohols bearing camphoric backbone were prepared from D-（＋）-camphoric imide and characterized by infrared, elemental analysis, ESI-MS, and NMR measurements. Among them, one intermediate （1S,3R）-3-amino-2,2,3- trimethyl cyclopentane-1-carboxylic acid hydrochloride 3 was structurally elucidated by X-ray diffraction techniques. Versatile intermolecular hydrogen bonding interactions observed in its packing structure result in a two-dimensional framework.
文摘Four simple, sensitive and accurate spectrophotometric methods have been developed for the determination of some calcium channel blockers: Amlodipine besylate (ADB), Diltiazem hydrochloride (DTZ) and Verapamil hydrochloride (VPM) in pharmaceutical formulations. These methods based on formation ion pair complexes with Sulfochlorophenol-S (SCPS), Bromopyrogallol red (BPR), Eriochromecyanine- R (ECC) and Pyrocatechol violet (PCV) in acidic medium. The colored products are extracted with chloroform and measured spectrophoto- metrically at 462, 600, 440 and 442 for ECC, SCPS, BPR and PCV, respectively. Beer’s low was obeyed in the concentration range, for ECC: 25 - 175 μg·ml-1, 50 - 150 μg·ml-1 or 100 - 250 μg·ml-1, for SCPS: 300 - 800 μg·ml-1, 200 - 700 μg·ml-1 or 100 - 550 μg·ml-1, for BPR: 50 - 400 μg·ml-1, 200 - 700 μg·ml-1 or 200 - 700 μg·ml-1 for VPM, DTZ or ADB, respectively and for PCV: 50 - 250 μg·ml-1 for VPM or 200 - 500 μg·ml-1 for DTZ with molar absorptivity, for ECC: 2.2 × 104, 2.1 × 104, 1.6 × 104 L·mol-1·cm-1, for SCPS: 3.8 × 103, 5.6 × 103, 8.1 × 103 L·mol-1·cm-1, for BPR: 11 × 103, 4.8 × 103, 6.9 × 103 L·mol-1·cm-1 for VPM, DTZ or ADB, respectively and for PCV: 19.5 × 103 L·mol-1·cm-1 for VPM and 6.6 × 103 L·mol-1·cm-1 for DTZ and relative standard deviation, for ECC: 0.76%, 0.86%, 0.46%, for SCPS: 0.94%, 0.96%, 0.86%, for BPR: 0.96%, 0.95%, 0.55% for VPM, DTZ or ADB, respectively and for PCV: 0.81% for VPM and 0.65% for DTZ. These methods have been successfully applied for the assay of drug in pharmaceutical formulations. No interference was observed from common pharmaceutical adjuvants. Statistical comparison of the results with the reference method shows excellent agreement and indicates no significant difference in accuracy and precision.
基金Project supported by the National Natural Science Foundation of China （No. 203900508）.
文摘A novel and simple procedure for the enantiospecific synthesis of penehyclidine hydrochloride （8018） isomers and the R configuration derivatives was described. The intramolecular asymmetric cyclization of the monosulfonate of compound 1,2-diol was applied to the execution of the synthesis of the key chiral building block for the first time. The aimed products were obtained with moderate yield in〉99% ee.
