Pharmaceutical Chemistry Journal最新文献

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Preparation, Physicochemical Properties, and Antibacterial Activity of Hydrogel Films Based on Starch and Poly(Vinyl Alcohol) with Added Ethonium 基于淀粉和添加了乙醇的聚乙烯醇的水凝胶薄膜的制备、理化性质和抗菌活性
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-18 DOI: 10.1007/s11094-024-03213-y
T. V. Kryuk, T. I. Zavyazkina, T. G. Tyurina, G. P. Goncharuk, M. V. Buyanovskaya, V. A. Senenko
{"title":"Preparation, Physicochemical Properties, and Antibacterial Activity of Hydrogel Films Based on Starch and Poly(Vinyl Alcohol) with Added Ethonium","authors":"T. V. Kryuk, T. I. Zavyazkina, T. G. Tyurina, G. P. Goncharuk, M. V. Buyanovskaya, V. A. Senenko","doi":"10.1007/s11094-024-03213-y","DOIUrl":"https://doi.org/10.1007/s11094-024-03213-y","url":null,"abstract":"<p>Hydrogel films with a polymer base of corn starch and poly(vinyl alcohol) (50:50 wt%), citric acid as a crosslinking agent, and glycerin as a plasticizer were synthesized. Their physical and mechanical characteristics corresponded to the performance level of commercial wound dressings of the same type. The degree of swelling increased by ~30%, whereas the elastic modulus and water-vapor permeability decreased by ~60% when ethonium was introduced into the polymer matrix (from 1 to 5 wt% of the polymer weight). Drug release from the polymer matrix occurred within 90-105 min at drug contents of 2.5-5 wt%. The developed films inhibited the growth of the microorganisms <i>E. coli</i> and <i>P. aeruginosa</i>.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"10 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142269351","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Study of Changes in Enterosgel Structure in Case of Violation of Drug Storage Conditions 违反药物储存条件时肠溶凝胶结构变化的研究
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-18 DOI: 10.1007/s11094-024-03214-x
N. E. Kuz’mina, S. V. Moiseev, E. Yu. Severinova, V. M. Shchukin, N. D. Bunyatyan
{"title":"Study of Changes in Enterosgel Structure in Case of Violation of Drug Storage Conditions","authors":"N. E. Kuz’mina, S. V. Moiseev, E. Yu. Severinova, V. M. Shchukin, N. D. Bunyatyan","doi":"10.1007/s11094-024-03214-x","DOIUrl":"https://doi.org/10.1007/s11094-024-03214-x","url":null,"abstract":"<p>The structure of enterosgel before and after freezing (samples I and II, respectively) was comparatively analyzed by gravimetric analysis and NMR methods [PMR, <sup>13</sup>C NMR, diffusion-ordered NMR spectroscopy (DOSY)] to understand the reason for the negative effect of freezing on the adsorption capacity of enterosgel. The methylsiloxane moieties in samples I and II were shown to be magnetically equivalent by PMR and <sup>13</sup>C NMR methods. The molecular masses of samples I and II were estimated by the DOSY method and corresponded to the cyclic dimer of methylsilicic acid (MM 152 Da) for sample I and the linear dimer of methylsilicic acid (MM 170 Da) for sample II. It was hypothesized that the conformationally rigid cyclic dimer structure was destroyed upon freezing of enterosgel due to rupture of a siloxane bond. The adsorption capacity of enterosgel deteriorated because of the structure disruption and hydrophobicity change. Thermogravimetric analysis revealed that water did not participate in hydrogen bonding with enterosgel.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"19 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142258958","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, In Vitro Antimycobacterial Activity of Some 2-((5-Amino-1,3,4-Thiadiazol-2-YL)Methyl)-6-Aryl-Tetrahydropyridazin-3-One Derivatives 一些 2-((5-氨基-1,3,4-噻二唑-2-YL)甲基)-6-芳基四氢哒嗪-3-酮衍生物的合成和体外抗霉菌活性
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-18 DOI: 10.1007/s11094-024-03203-0
Mamdouh Allahyani, Abdulaziz Alsharif, Mazen Almehmadi, Shivani Verma, Mohammad Asif
{"title":"Synthesis, In Vitro Antimycobacterial Activity of Some 2-((5-Amino-1,3,4-Thiadiazol-2-YL)Methyl)-6-Aryl-Tetrahydropyridazin-3-One Derivatives","authors":"Mamdouh Allahyani, Abdulaziz Alsharif, Mazen Almehmadi, Shivani Verma, Mohammad Asif","doi":"10.1007/s11094-024-03203-0","DOIUrl":"https://doi.org/10.1007/s11094-024-03203-0","url":null,"abstract":"<p>A series of 2-((5-amino-1,3,4-thiadiazol-2-yl)methyl)-6-aryl-2,3,4,5-tetrahydro-pyridazin-3-one (<b>4a-e</b>) was synthesized and evaluated for its <i>in vitro</i> antimycobacterial activity. All the synthesized compounds were structurally confirmed by using physicochemical and spectral analysis such as melting point, <i>R</i><sub><i>f</i></sub> value, elemental analysis, IR, NMR and mass spectra. <i>In vitro</i> antimycobacterial activity was screened by the microplate Alamar Blue Assay (MABA) method against <i>Mycobacterium tuberculosis</i> H37Rv strain. Derivatives with 4-ethyl phenyl substitution (<b>4b</b>) and chloro phenyl substitution (<b>4e</b>) at the <i>p</i>-position of pyridazinone nuclei showed good antimycobacterial activity with a MIC value of 6.25 μg/ml compared to other aryl substitutions such as 4-methoxy phenyl (<b>4a</b>), 4-methyl phenyl (<b>4c</b>) with a MIC value of 25 and 12.5 μg/ml. The results of <i>in vitro</i> antimycobacterial activity revealed that the synthesized compounds have potential antimycobacterial action and can be further optimized and developed as lead compounds.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"203 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142258918","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
HPLC Determination of Myricitrin in Leaves of Common Myrtle (Myrtus communis L.) 高效液相色谱法测定普通桃金娘叶(Myrtus communis L.)
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-18 DOI: 10.1007/s11094-024-03211-0
V. A. Kurkin, V. D. Maslova, A. R. Mubinov
{"title":"HPLC Determination of Myricitrin in Leaves of Common Myrtle (Myrtus communis L.)","authors":"V. A. Kurkin, V. D. Maslova, A. R. Mubinov","doi":"10.1007/s11094-024-03211-0","DOIUrl":"https://doi.org/10.1007/s11094-024-03211-0","url":null,"abstract":"<p>A method for quantitative determination of myricitrin in common myrtle (<i>Myrtus communis</i> L.) leaves using high-performance liquid chromatograph (HPLC) was developed. The content of the dominant flavonoid myricitrin (myricetin 3-<i>O</i>-α-L-rhamnopyranoside) in common myrtle leaves varied from 0.98 ± 0.02% to 1.51 ± 0.07%. The error of a single determination and the average error of the myricitrin content determination in common myrtle leaves were ±15.81% and ±4.77%, respectively, with confidence probability 95%.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"36 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142258960","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Long-Acting Hydrogel Eye Drops Composite Sequentially Releases Basic Fibroblast Growth Factor and Carbomer for Synergistic Promotion of the Repair of Corneal Epithelium 长效水凝胶滴眼液复合剂依次释放碱性成纤维细胞生长因子和卡波姆,协同促进角膜上皮的修复
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-18 DOI: 10.1007/s11094-024-03202-1
Wanling Chen, Kaiping Zhang, Chengyuan Zhang
{"title":"Long-Acting Hydrogel Eye Drops Composite Sequentially Releases Basic Fibroblast Growth Factor and Carbomer for Synergistic Promotion of the Repair of Corneal Epithelium","authors":"Wanling Chen, Kaiping Zhang, Chengyuan Zhang","doi":"10.1007/s11094-024-03202-1","DOIUrl":"https://doi.org/10.1007/s11094-024-03202-1","url":null,"abstract":"<p>Corneal epithelial injury is a high-incidence corneal disease. The purpose of this research is to determine how basic fibroblast growth factors affect bFGF and Carbomer (CAR) long-acting hydrogel eye drops regarding the repair of corneal epithelial injury. Liposome hydrogel eye drops containing both bFGF and CAR were prepared by a thin film hydration method (bFGF-CAR-HED). Particle size, potential and transmission electron microscopy were used to characterize the performance. UV was used to calculate the encapsulation rate, drug loading, and in vitro release. The antioxidant capacity was detected by ABTS and FRAP. Safety was evaluated by cell assay. After parallel mechanical corneal epithelium injury in normal mice, the repair of corneal epithelium injury, sensitivity repair and the expression of inflammatory factors in the cornea were detected. bFGF-CAR-HED is a multilayer liposome with good stability with a particle size of 308.4 ± 7.25 nm, and a potential of 36.3 ± 6.27 mV. The encapsulation rate of bFGF in bFGF-CAR-HED was 92.01 ± 1.05%, the encapsulation rate of CAR was 91.94 ± 0.34%, the drug load of bFGF was 18.82 ± 0.35%, and the drug load of CAR was 19.97 ± 0.39%, which showed sustained release function, low cytotoxicity and good antioxidant capacity. Long-acting hydrogel eye drops can strengthen drug application performance and extend the time of drug action, effectively improving bFGF, eye absorbency and the function of CAR, effectively promoting corneal epithelium damage repair and restoring corneal sensitivity, thereby providing better strategies for promoting corneal epithelium damage repair.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"17 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142258919","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and Evaluation of the Neurotropic Activity of New β-Cycloketol Derivatives 合成和评估新的β-环酮醇衍生物的神经刺激活性
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-17 DOI: 10.1007/s11094-024-03200-3
S. L. Kocharov, H. A. Panosyan, L. S. Mirzoyan, I. M. Nazaryan, R. G. Paronikyan
{"title":"Synthesis and Evaluation of the Neurotropic Activity of New β-Cycloketol Derivatives","authors":"S. L. Kocharov, H. A. Panosyan, L. S. Mirzoyan, I. M. Nazaryan, R. G. Paronikyan","doi":"10.1007/s11094-024-03200-3","DOIUrl":"https://doi.org/10.1007/s11094-024-03200-3","url":null,"abstract":"<p>Two types of known and new derivatives of substituted β-cycloketols were synthesized; characterized using IR, PMR, and <sup>13</sup>C NMR spectroscopy; and tested for neurotropic activity. Bioscreening of the compounds was performed. A study of the neurotropic properties of the synthesized new β-cycloketol derivatives revealed that some of them exhibited a pronounced anticonvulsant effect as antagonism of corazol. The compounds were superior in anticonvulsant activity to the well-known drug ethosuximide but inferior to diazepam. Like ethosuximide, the studied compounds did not exhibit central muscle relaxant activity at anticonvulsant doses, unlike diazepam. However, they exhibited psychotropic effects, e.g., pronounced anxiolytic, antidepressant, and activating behavior. The results showed that further searching for neurotropic properties in new polyfunctional cycloketol derivatives was advisable.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"18 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142258961","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
An Update on the Green Synthesis of Benzimidazole Scaffolds as Antifungal Agents 苯并咪唑支架作为抗真菌剂的绿色合成最新进展
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-17 DOI: 10.1007/s11094-024-03210-1
Anchal Tyagi, Monika Chauhan, Sumitra Nain
{"title":"An Update on the Green Synthesis of Benzimidazole Scaffolds as Antifungal Agents","authors":"Anchal Tyagi, Monika Chauhan, Sumitra Nain","doi":"10.1007/s11094-024-03210-1","DOIUrl":"https://doi.org/10.1007/s11094-024-03210-1","url":null,"abstract":"<p>The heterocyclic nucleus has a wide range of biological activities with the benzimidazole nucleus having diverse biological activities such as antifungal, antihistaminic, anti-convulsant, anti-inflammatory, analgesic, antiviral agents, etc. From an in-depth literature review, we have complied here a green synthesis of benzimidazole derivatives that are antifungal agents. This review is intended to be of assistance to the scientific community working in the area of heterocyclic nuclei.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"45 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142258959","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design, Synthesis, and Cardiotropic Properties of N1-Benzyl-N2-{2-[(2,3,4-Trimethoxybenzyl)Amino]-Ethyl}Ethane-1,2-Diamines N1-苄基-N2-{2-[(2,3,4-三甲氧基苄基)氨基]-乙基}乙烷-1,2-二胺的设计、合成和强心特性
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-16 DOI: 10.1007/s11094-024-03198-8
G. V. Mokrov, T. Yu. Vorobieva, V. E. Birukova, A. S. Pantileev, E. I. Barchukova, I. B. Tsorin, M. B. Vititnova, A. G. Rebeko, S. A. Kryzhanovskiy, T. A. Gudasheva, V. L. Dorofeev
{"title":"Design, Synthesis, and Cardiotropic Properties of N1-Benzyl-N2-{2-[(2,3,4-Trimethoxybenzyl)Amino]-Ethyl}Ethane-1,2-Diamines","authors":"G. V. Mokrov, T. Yu. Vorobieva, V. E. Birukova, A. S. Pantileev, E. I. Barchukova, I. B. Tsorin, M. B. Vititnova, A. G. Rebeko, S. A. Kryzhanovskiy, T. A. Gudasheva, V. L. Dorofeev","doi":"10.1007/s11094-024-03198-8","DOIUrl":"https://doi.org/10.1007/s11094-024-03198-8","url":null,"abstract":"<p>A new group of unsymmetrical ALM-802 analogs, <i>N</i><sup>1</sup>-benzyl-<i>N</i><sup>2</sup>-{2-[(2,3,4-trimethoxybenzyl)amino]-ethyl}ethane-1,2-diamines of general formula <b>1</b>, in which one of the aromatic groups was changed, was studied. The anti-ischemic and antiarrhythmic activities of the new compounds were studied. Their ADME characteristics were analyzed. The 2,3,4-trimethoxyphenyl group used as one of the aromatic pharmacophores was shown to play a key role in the activity of compounds of this type. The presence of a second aromatic group was also important since its removal led to the disappearance of cardiotropic activity. However, its structure had significantly less impact on the activity of the corresponding compounds because a rather wide variation of substituents in this group did not change the activity in most arrhythmia and ischemia models.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"82 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142258962","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Fullerene C60 Decreases Inflammation, Oxidative Stress and Apoptosis Induced by 7,12-Dimethylbenz[a]Anthracene (DMBA) in Muscle Tissue Via Caspase-3 and NRF-2 Protein Signaling Pathway 富勒烯 C60 通过 Caspase-3 和 NRF-2 蛋白信号通路降低 7,12-二甲基苯并[a]蒽 (DMBA) 在肌肉组织中诱导的炎症、氧化应激和细胞凋亡
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-16 DOI: 10.1007/s11094-024-03207-w
Abdullah Aslan, Seda Beyaz, Ozlem Gok, Ibrahim Hanifi Ozercan, Can Ali Agca
{"title":"Fullerene C60 Decreases Inflammation, Oxidative Stress and Apoptosis Induced by 7,12-Dimethylbenz[a]Anthracene (DMBA) in Muscle Tissue Via Caspase-3 and NRF-2 Protein Signaling Pathway","authors":"Abdullah Aslan, Seda Beyaz, Ozlem Gok, Ibrahim Hanifi Ozercan, Can Ali Agca","doi":"10.1007/s11094-024-03207-w","DOIUrl":"https://doi.org/10.1007/s11094-024-03207-w","url":null,"abstract":"<p>Fullerene C<sub>60</sub> exhibits potent antioxidant anti-inflammatory activities as well as anticancer activities. In this study using 60 Wistar albino female rats (<i>n</i> = 60, 8 weeks old), they rats were divided into 4 groups, including 15 rats each. The groups were arranged as follows: (i) Control Group: Group fed with standard diet; (ii) C<sub>60</sub> Group: C<sub>60</sub> (1.7 mg/kg bw, oral gavage); (iii) DMBA (7,12-dimethylbenz[<i>a</i>]anthracene) Group: DMBA (45 mg/kg bw, oral gavage); (iv) C<sub>60</sub> and DMBA Group: C<sub>60</sub> (1.7 mg/kg bw, oral gavage) and DMBA (45 mg/kg bw, oral gavage) group. DMBA increased the malondialdehyde levels in muscle tissue, while decreasing GSH and CAT levels; however, treatment with fullerene C<sub>60</sub> reversed these effects. In addition, the oral administration of fullerene C<sub>60</sub> increased caspase-3 and Nrf-2 protein expression and significantly decreased Bcl-2, NF-κB, TNF-α, COX-2 and p38α (MAPK) protein expression in C<sub>60 +</sub> DMBA compared to the DMBA group. Moreover, histopathological imaging revealed that the oral administration of fullerene C<sub>60</sub> decreases inflammatory cells, edema formation, and hydropic degeneration in the muscles. Taken together, the results of the present study indicated that fullerene C<sub>60</sub> nanoparticle provides effective protection by preventing muscle tissue damage.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"117 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142258966","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Withanolides of the Aerial Part of Datura stramonium Growing in Uzbekistan and Cytotoxicity of Daturametelin H 生长在乌兹别克斯坦的曼陀罗药用部分的 Withanolides 和 Daturametelin H 的细胞毒性
IF 0.9 4区 医学
Pharmaceutical Chemistry Journal Pub Date : 2024-09-16 DOI: 10.1007/s11094-024-03212-z
M. M. Makhmudova, B. A. Abdurakhmanov, R. M. Khalilov, I. D. Bobaev, Kh. M. Bobakulov, G. B. Sotimov, N. D. Abdullaev, E. O. Terent’eva
{"title":"Withanolides of the Aerial Part of Datura stramonium Growing in Uzbekistan and Cytotoxicity of Daturametelin H","authors":"M. M. Makhmudova, B. A. Abdurakhmanov, R. M. Khalilov, I. D. Bobaev, Kh. M. Bobakulov, G. B. Sotimov, N. D. Abdullaev, E. O. Terent’eva","doi":"10.1007/s11094-024-03212-z","DOIUrl":"https://doi.org/10.1007/s11094-024-03212-z","url":null,"abstract":"<p>The extract obtained from the aerial part of <i>Datura stramonium</i> by treatment with EtOH (90%) was fractionated with various organic solvents. Use of extraction naphtha produced 0.28% (in percentage of the raw material mass) of the extracted substances; CHCl<sub>3</sub>, 2.24%; EtOAc, 1.19%; and <i>n</i>-BuOH, 12.43%. Six withanolides such as daturalactone (<b>I</b>), (22<i>R</i>)-7b,27-hydroxy-1-oxowitha-2,5,24-trienolide (<b>II</b>), daturataturin A (<b>III</b>), withastramonolide (<b>IV</b>), (22<i>R</i>)-27-hydroxy-7b-methoxy-1-oxovita-3,5,24-trienolide (<b>V</b>), and daturametelin H (<b>VI</b>) were isolated from the aerial parts of <i>D. stramonium</i> collected in the Fergana Region of Uzbekistan. Their structures were elucidated on the basis of vast data of IR, UV, and NMR spectroscopic studies. The presence of compounds <b>II</b>, <b>III</b>, and <b>V</b> in the aerial parts of <i>D. stramonium</i> growing in Uzbekistan was proven, while compound <b>VI</b> was isolated for the first time from aerial parts of <i>D. stramonium</i>. The cytotoxicity of chemically pure daturametelin H was studied on cancer cell lines such as cervical epithelial carcinoma HeLa, mammary adenocarcinoma HBL-100 (ATCC NTV 124), adenocarcinoma of the larynx HEp-2 (ATCC:CCL-23), and T-lymphoblastic leukemia CCRF-CEM (ATCC:CCL-19). Daturametelin H was found to exhibit pronounced cytotoxicity at a concentration of 100 mM only against T-lymphoblastic leukemia cells <i>in vitro</i>.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":"32 1","pages":""},"PeriodicalIF":0.9,"publicationDate":"2024-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142269489","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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