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ASSESSMENT OF MEDICATION ADHERENCE TO ORAL ANTINEOPLASTIC DRUGS AMONG CANCER PATIENTS IN A TERTIARY HOSPITAL IN SOUTH-SOUTH, NIGERIA 评估尼日利亚南部一家三级医院癌症患者口服抗肿瘤药物的依从性
Pub Date : 2024-07-26 DOI: 10.59493/ajopred/2024.2.10
Monday Ikponmwosa Osarenmwinda, Chukwudi Uzowuihe
The prevalence of cancer in developing countries is on the increase, and is associated with a high mortality rate. The study aimed to evaluate medication adherence to oral antineoplastic therapy in a tertiary health facility, in Benin City. A cross-sectional study was carried out among cancer patients at the oncology unit of the University of Benin Teaching Hospital, Benin City, using semi-structured and standardized Morisky Green Test instruments. The analysis was descriptive and inferential, and the results were considered significant at p < 0.05. Medication adherence to oral antineoplastic drugs was 74.4%. The patients had a significant (p < 0.05) Morisky Green Test score of 25.6%. Respondents using Bevacizumab, Docetaxel and Oxaliplastin, were totally (100%) compliant with their medications. Major reasons for medication non-adherence with oral cancer chemotherapy were forgetfulness (18.9%) and carelessness about time to take medications (14.1%). Significant (p < 0.05) factors and attitudes associated with medication adherence were gender, number of medications per day, forgetting to take medications, not knowing how and when to take medications, checking name and dosage before taking medication, and storing medications in an appropriate place. Overall, the patients had above-average adherence to their oral antineoplastic therapy, but experienced difficulty in treatment with a positive Morisky green Test score.
发展中国家的癌症发病率呈上升趋势,而且死亡率很高。本研究旨在评估贝宁市一家三级医疗机构口服抗肿瘤药物治疗的依从性。研究采用半结构化和标准化的莫里斯基-格林测试工具,对贝宁市贝宁大学教学医院肿瘤科的癌症患者进行了横断面研究。分析方法为描述性和推论性,结果以 p < 0.05 为显著。口服抗肿瘤药物的依从性为 74.4%。患者的莫里斯基绿色测试得分率为 25.6%,具有显著性(P < 0.05)。使用贝伐单抗、多西他赛和奥沙利铂的受访者完全(100%)遵医嘱用药。口服癌症化疗药物不达标的主要原因是健忘(18.9%)和不注意服药时间(14.1%)。与服药依从性相关的重要因素和态度(p < 0.05)是性别、每天服药次数、忘记服药、不知道服药方法和时间、服药前核对药名和剂量以及将药物存放在适当的地方。总体而言,患者对口服抗肿瘤药物治疗的依从性高于平均水平,但在治疗过程中遇到了困难,莫里斯基绿色测试得分呈阳性。
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引用次数: 0
PRELIMINARY PHARMACOGNOSTIC EVALUATION OF ETHANOL EXTRACT OF LEAF OF OLAX SUBSCORPOIDEA OLIV (OLACACEAE) 橄榄科植物橄榄叶乙醇提取物的初步药效学评价
Pub Date : 2024-07-26 DOI: 10.59493/ajopred/2024.2.11
L. U. Nwankwo, Benedict Bolakponumigha Iwetan, Jacinta Enoh APITIKORI-OWUMI, Emily Uyovwiesiri Emudainohwo, Japheth Ojehomon Ojeifo
One of the most common objections leveled against natural products is a lack of standardization, necessitating the exploration of various quality control approaches aimed at proving the safety and quality of crude medications. The purpose of this study was to assess the quality of Olax subscorpoidea leaves. The ethanol extract of Olax subscorpoidea leaves was obtained by the maceration process. Chemo-microscopy and physicochemical examination (moisture content, total ash value, acid insoluble ash, water soluble ash, extractive values) of the crude drug were performed using established procedures. The presence or absence of starch, mucilage, calcium oxalate, cellulose, and lignin was determined to deduce various microscopic traits with chemical reagents. The crude drugs qualitative phytochemical investigation disclosed the presence of tannins, saponins, flavonoids, alkaloids, phenols, terpenoids, steroids, and cardiac glycosides. Quantitative phytochemical analysis revealed that the plant extract had more alkaloids and saponins than the other phytoconstituents present. Chemomicroscopy of Olax subscorpoidea leaves indicated the presence of starch, mucilage, cellulose, calcium oxalate, and lignin. The physicochemical study of Olax subscorpoidea ethanol leaf extract indicated moisture content (8±0.03%) and total ash content (0.15±0.01%), respectively. The extractive value also revealed that polar solvents are most suited for extracting the crude drug. This study was able to provide useful information that aids pharmacognostic standardization, thereby building a scientific platform to buttress the quality of Olax subscorpoidea powdered leaf and its ethanol extract for ease of formulation and commercialization.
对天然产品最常见的反对意见之一是缺乏标准化,因此有必要探索各种质量控制方法,以证明粗制药物的安全性和质量。本研究的目的是评估Olax subscorpoidea叶片的质量。Olax subscorpoidea 叶子的乙醇提取物是通过浸渍过程获得的。采用既定程序对粗药进行了化学显微镜检查和理化检查(水分含量、总灰分值、酸不溶性灰分、水溶性灰分、萃取值)。通过化学试剂测定淀粉、粘液质、草酸钙、纤维素和木质素的存在与否,从而推断出各种微观特征。原药的定性植物化学调查显示了鞣质、皂苷、黄酮类、生物碱、酚类、萜类、甾体和强心苷的存在。定量植物化学分析显示,植物提取物中的生物碱和皂苷含量高于其他植物成分。Olax subscorpoidea 叶子的化学显微镜检查表明,其中含有淀粉、粘液、纤维素、草酸钙和木质素。Olax subscorpoidea 乙醇叶提取物的理化研究表明,水分含量(8±0.03%)和总灰分含量(0.15±0.01%)分别为 0.01%和 0.01%。萃取值还表明,极性溶剂最适合提取粗药物。这项研究提供了有助于药典标准化的有用信息,从而建立了一个科学平台,以提高亚鼠李叶粉及其乙醇提取物的质量,便于配方和商业化。
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引用次数: 0
ANTI-INFLAMMATORY AND ANTIMICROBIAL ACTIVITIES OF THE LEAVES OF ACALYPHA WILKESIANA MUELL. ARG. (EUPHORBIACEAE) FORMULATED AS HERBAL CREAM 芹菜叶的消炎和抗菌活性。ARG.(配制成草本乳膏
Pub Date : 2024-07-17 DOI: 10.59493/ajopred/2024.2.9
T. Abere, Amarachi Chukwuma Offor, Onohwekaroma Abere, Favour Ireoluwa Eniayekan, Wilson Obadu Ishima
The use of some traditional creams in Nigeria is associated with negative outcomes. In order to tackle this problem, we conducted a study on the antibacterial and anti-inflammatory characteristics of Acalypha wilkesiana leaves, which were utilized in the creation of a herbal cream. Standard methods were employed to conduct analytical procedures for the analysis of the phytochemical and chromatographic content of A. wilkesiana leaves. The anti-inflammatory efficacy of the unrefined ethanol extract was assessed using the egg albumin technique, throughout a dosage range of 15.6 to 500 mg/ml. The effectiveness of the herbal cream and the raw ethanol extract of A. wilkesiana in killing specific bacteria were evaluated. A comprehensive evaluation was carried out to determine the physicochemical characteristics of the herbal cream formulation using appropriate methodologies. The phytochemical examination of A. wilkesiana which gave a yield of 12.6 % indicated the existence of alkaloids, tannins, and saponins. The anti-inflammatory properties of the crude extract derived from A. wilkesiana had a comparable effect to that of aspirin, a commonly prescribed medicine at doses of 125, 250 and 500 mg/kg. The herbal cream (25.5 ± 0.22) and crude extract (19.5 ± 0.01) had the greatest antibacterial effectiveness against Candida albicans at 200 mg/ml. The physicochemical examination of the cream that was created: pH (5.6 ± 0.64); consistency (5 mm); viscosity (22 x 106 cps); spreadability (36 g.cm/sec); Extrudability (510 gm) showed similarities to the commercially available Gentamycin cream. The herbal cream containing A. wilkesiana has demonstrated substantial promise and could function as a practical alternative to traditional creams for treating skin infections.
在尼日利亚,使用某些传统药膏会产生不良后果。为了解决这个问题,我们对 Acalypha wilkesiana 叶子的抗菌和消炎特性进行了研究,并将其用于制作草药面霜。我们采用了标准方法,对 Acalypha wilkesiana 叶子的植物化学成分和色谱含量进行了分析。在 15.6 至 500 毫克/毫升的剂量范围内,使用鸡蛋白蛋白技术评估了未精制乙醇提取物的抗炎功效。还评估了草药乳膏和 A. wilkesiana 未提炼乙醇提取物在杀死特定细菌方面的功效。采用适当的方法对草药乳膏配方的理化特性进行了综合评估。对 A. wilkesiana 进行的植物化学检查表明,其中含有生物碱、鞣质和皂苷,产量为 12.6%。从 A. wilkesiana 提取的粗提取物的抗炎特性与阿司匹林(一种常用处方药,剂量分别为 125、250 和 500 毫克/千克)的效果相当。草药膏(25.5 ± 0.22)和粗提取物(19.5 ± 0.01)在 200 毫克/毫升的剂量下对白色念珠菌的抗菌效果最好。乳膏的理化检查结果显示:pH 值(5.6 ± 0.64);稠度(5 毫米);粘度(22 x 106 cps);涂抹性(36 克厘米/秒);可挤压性(510 克)与市售的庆大霉素乳膏相似。含有 A. wilkesiana 的草药乳膏已显示出巨大的前景,可作为治疗皮肤感染的传统乳膏的实用替代品。
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引用次数: 0
PREPARATION OF LIPID-BASED FORMULATIONS USING LOCAL BEESWAX SOURCED FROM HONEYCOMBS 利用蜂巢中的本地蜂蜡制备脂基配方
Pub Date : 2024-07-16 DOI: 10.59493/ajopred/2024.2.8
C. Agbo, M. I. Ngwu, U. Anyaji, Chinenye Ubahakwe, Godswill Nnanna Asogwa, P. Akpa, P. Nnamani, K. Ofokansi, A. Attama
Solid lipids used in formulation of novel drug delivery systems in most developing countries are sourced from abroad and are quite expensive. Wax from honeycombs is readily available, and is even disposed as waste, but can be utilized as a solid lipid for the formulation of different lipid-based drug delivery systems. This study aims to formulate and compare the features of the solid lipid nanoparticle (SLNs) and nanostructured lipid carrier (NLCs) delivery systems of quinine hydrochloride made with local beeswax (that is beeswax from locally sources honeycomb waste) and other solid lipids sourced from abroad. Local beeswax was first purified by hot bath method. Solidified reverse micellar solutions (SRMS) were prepared by fusion method using Phospholipon®90H and either local beeswax, Softisan®154, foreign beeswax, or stearic acid, separately. SLNs and NLCs of quinine made with SRMS of each of these solid lipids were formulated using hot homogenization method. These SLNs and NLCs were characterized. The average particle size of SLNs and NLCs made with local beeswax was 93.60 ± 4.44 nm and 112.80 ± 3.89 nm, respectively, and was not significantly (p > 0.05) different from the sizes of formulations made from other solid lipids (SLNs: 96.64 to 118.9 ± 4.13 nm and NLCs: 99.68 ± 6.75 to 117.30 ± 4.60 nm). The particles were monodispersed having PDI ranging from 0.281±0.054 to 0.308±0.055. Encapsulation efficiency and loading capacity were generally poor, especially among the SLN formulations. However, SLNs made with local beeswax and stearic acid were able to encapsulate quinine, whereas foreign beeswax and Softisan®154 had zero encapsulation. This study reveals that the features of the SLNs and NLCs made with local beeswax where highly comparable with those formulated with the imported solid lipids. Therefore, local beeswax can serve as a suitable affordable and available alternative to other imported solid lipids for formulating different lipid drug delivery systems.
在大多数发展中国家,用于配制新型给药系统的固体脂质都来自国外,而且价格昂贵。蜂窝中的蜡很容易获得,甚至被当作废物处理,但可以用作固体脂质,用于配制不同的脂质给药系统。本研究旨在利用本地蜂蜡(即来自本地蜂巢废弃物的蜂蜡)和国外其他固体脂质配制盐酸奎宁固体脂质纳米颗粒(SLNs)和纳米结构脂质载体(NLCs)给药系统,并比较其特点。本地蜂蜡首先通过热浴法纯化。分别使用 Phospholipon®90H 和本地蜂蜡、Softisan®154、国外蜂蜡或硬脂酸,通过融合法制备固化反向胶束溶液(SRMS)。采用热均质法配制了使用上述每种固体脂质的 SRMS 制成的奎宁 SLN 和 NLC。对这些 SLNs 和 NLCs 进行了表征。用本地蜂蜡制成的 SLNs 和 NLCs 的平均粒径分别为 93.60 ± 4.44 nm 和 112.80 ± 3.89 nm,与用其他固体脂质制成的制剂的粒径(SLNs:96.64 至 118.9 ± 4.13 nm,NLCs:99.68 ± 6.75 至 117.30 ± 4.60 nm)相比,差异不大(p > 0.05)。颗粒呈单分散状态,PDI 为 0.281±0.054 至 0.308±0.055。封装效率和负载能力普遍较差,尤其是在 SLN 配方中。不过,用本地蜂蜡和硬脂酸制成的 SLN 能够包封奎宁,而用外国蜂蜡和 Softisan®154 制成的 SLN 的包封率为零。这项研究表明,使用本地蜂蜡制成的 SLN 和 NLC 的特性与使用进口固体脂质配制的 SLN 和 NLC 非常相似。因此,在配制不同的脂质给药系统时,本地蜂蜡可作为其他进口固体脂质的一种经济实惠且可用的替代品。
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引用次数: 0
EXTRACTION, PURIFICATION AND CHARACTERIZATION OF PECTIN OBTAINED FROM THE PULP OF PARKIA BIGLOBOSA AND THE EVALUATION OF ITS CYTOTOXIC ACTIVITY ON HEPG2 CANCER CELL LINE 从大叶朴树果肉中提取、纯化和鉴定果胶并评估其对 HPG2 癌细胞系的细胞毒活性
Pub Date : 2024-07-13 DOI: 10.59493/ajopred/2024.2.6
Ahmad Rufai Junaid, Kabiru Ado, S. Garba
Pectin, a naturally occurring polysaccharide that has a wide range of industrial applications especially in the pharmaceutical industries, has in recent times gained a lot of attention by researchers with potential breakthrough as a therapeutic agent. The aim of this research was to extract, purify and characterize pectin obtained from the pulp of Parkia biglobosa and to evaluate its cytotoxic assay on HepG2 cancer cell line. Acidified water (using HNO3 and HCl) was used for the extraction at pH levels 1.5, 3 and 5. Chemical and spectroscopic characterizations were adopted for this rresearch,and it was observed that pectin was best extracted from the source at a pH level of 1.5. The oil holding capacity was 1.41 g/g, while the percentage solubility, ash content and moisture content were 70%, 2.87% and 15.72% respectively. The pectin extract was found to have an equivalent weight of 953.19 kgmol-1, whereas the AUA (anhydrouronic acid) content, methoxyl content, and DE (degree of esterification) were found to be 60.48%, 7.40%, and 69.50% respectively. The following functional groups: carboxyl, hydroxyl (3500 - 3300 cm-1 indicating -OH stretching vibration of carboxylic group), C-O-C stretching vibration, and an aromatic C-H vibration of methyl group, were found present. The percentage cytotoxicity values obtained at various concentrations (125 µg/cm3, 250 µg/cm3, 500 µg/cm3 and 1000 µg/cm3) of the pectin extract, were 4.60 %, 13.70 %, 16.8 % and 46.8 % respectively. This shows the cytotoxic activity of pectin extracted from the pulp of Parkia biglobosa on HepG2 cancer cells, and its potential of being an anticancer agent. The findings in this research have further placed Parkia biglobosa as a good source of commercial pectin for pharmaceutical application.
果胶是一种天然多糖,具有广泛的工业用途,尤其是在制药业。本研究的目的是从大叶朴树果肉中提取、纯化和鉴定果胶,并评估其对 HepG2 癌细胞系的细胞毒性。提取采用酸化水(使用 HNO3 和 HCl),pH 值分别为 1.5、3 和 5。本研究采用了化学和光谱特性分析,结果表明,果胶在 pH 值为 1.5 时提取效果最佳。持油量为 1.41 g/g,溶解度、灰分含量和水分含量分别为 70%、2.87% 和 15.72%。果胶提取物的当量重量为 953.19 kgmol-1,AUA(无水酸)含量、甲氧基含量和 DE(酯化度)分别为 60.48%、7.40% 和 69.50%。发现存在以下官能团:羧基、羟基(3500 - 3300 cm-1 表示羧基的 -OH 伸展振动)、C-O-C 伸展振动和甲基的芳香族 C-H 振动。果胶提取物在不同浓度(125 微克/立方厘米、250 微克/立方厘米、500 微克/立方厘米和 1000 微克/立方厘米)下的细胞毒性百分比分别为 4.60%、13.70%、16.8% 和 46.8%。这表明从大叶朴树果肉中提取的果胶对 HepG2 癌细胞具有细胞毒性活性,具有抗癌潜力。这项研究结果进一步将大叶朴树作为商业果胶的良好来源,用于医药应用。
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引用次数: 0
PREVALENCE AND FACTORS ASSOCIATED WITH DEPRESSION AMONG HIV/AIDS CLIENTS IN A SECONDARY HEALTH FACILITY IN NIGERIA 尼日利亚一家二级医疗机构中艾滋病毒/艾滋病患者中抑郁症的患病率及相关因素
Pub Date : 2024-07-13 DOI: 10.59493/ajopred/2024.2.7
M. Akunne, G. Etim, C. Anosike
About 13% of all diseases worldwide are mental health disorders. A mental health condition known as depression is characterized by a low mood, diminished interest in or enjoyment from activities, low energy, feelings of guilt or low self-worth, trouble sleeping or eating, and difficulty concentrating. The objectives of this study were to determine the prevalence level of depression and the factors associated with depressive symptoms among the studied participants. It was a cross-sectional descriptive evaluation, carried out between October and December 2022, at Bishop Shanahan Hospital Nsukka, a renowned secondary health facility located at Nsukka Local Government in Enugu State. Data were collected using the Nine Symptom Checklist questionnaire for the assessment of depression. The cut-off points for mild, moderate, moderately severe, and severe depression were indicated by total scores of 5, 10, 15 and 20 respectively. A section of the questionnaire was designed to collect the participants’ socio-demographics and their clinical characteristics. Ethical clearance was obtained from the hospital. Statistical Package for Social Sciences (SPSS) version 23.0 was used for both descriptive and inferential statistics during the data analysis process. A significance threshold of p<0.05 was applied. The response rate was 99.6%. More males responded (50.4%). Most (64.7%) of the participants were minimally-mildly depressed. However, 0.4% were severely depressed. Marital status (P=0.02) and time on ART (P=0.016) were found to be closely associated with the level of depression. This study showed that most participants had no depressive symptoms. The respondents who were single and had been on ART medications for more than one year were more depressed than others. Though few participants were severely depressed, there’s a strong need to enforce the psychotherapy aspects of HIV management.
全球约有 13% 的疾病属于精神疾病。抑郁症是一种精神疾病,主要表现为情绪低落、对活动的兴趣或乐趣减退、精力不足、内疚感或自我价值感低、睡眠或进食困难以及注意力难以集中。本研究的目的是确定研究对象中抑郁症的流行程度以及与抑郁症状相关的因素。这是一项横断面描述性评估,于 2022 年 10 月至 12 月期间在恩苏卡主教沙纳汉医院进行,该医院是位于埃努古州恩苏卡地方政府的一家著名二级医疗机构。收集数据时使用了九种症状清单问卷来评估抑郁症。轻度、中度、中重度和重度抑郁症的临界点分别为总分 5、10、15 和 20 分。问卷中还设计了一个部分,用于收集参与者的社会人口统计数据和临床特征。调查获得了医院的伦理许可。在数据分析过程中,使用了社会科学统计软件包(SPSS)23.0 版进行描述性和推断性统计。显著性阈值为 p<0.05。答复率为 99.6%。男性答复者较多(50.4%)。大多数参与者(64.7%)为轻度抑郁。然而,0.4% 的人患有严重抑郁症。研究发现,婚姻状况(P=0.02)和接受抗逆转录病毒疗法的时间(P=0.016)与抑郁程度密切相关。本研究显示,大多数参与者没有抑郁症状。单身且接受抗逆转录病毒疗法超过一年的受访者比其他人更抑郁。虽然严重抑郁的受访者很少,但在艾滋病管理中仍有必要加强心理治疗方面的工作。
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引用次数: 0
EVALUATION OF ANTIBACTERIAL ACTIVITIES OF SELECTED DISINFECTANTS SOLD IN OGIGE MARKET IN NSUKKA, NIGERIA, ON SOME CLINICAL BACTERIAL ISOLATES 评估尼日利亚恩苏卡 Ogige 市场上出售的某些消毒剂对一些临床细菌分离株的抗菌活性
Pub Date : 2024-07-11 DOI: 10.59493/ajopred/2024.2.5
S. Enemuor, Blessing Ada Eze, C. Ezeh
Disinfectants are chemicals that can kill or inhibit the growth of microorganisms and are widely used in hospitals and in households. This study was aimed at evaluating the antibacterial activity of six household disinfectants (D1, D2, D3, D4, D5 and D6) used in Nsukka, Enugu Nigeria on four clinical bacterial isolates including Escherichia coli, Staphylococcus aureus, Bacillus subtilis and Pseudomonas aeruginosa. The test organisms used were obtained from Medical Diagnostic Laboratory of University of Nigeria, Medical Centre, Nsukka. Dilutions of each disinfectant were prepared. The antibacterial activities of various dilutions of the disinfectants against the test organisms were determined using well diffusion technique. Phenol coefficient of each disinfectant was determined using Rideal-Walker method. Dilutions of phenol (1:80, 1:90 and 1:100) and disinfectants (1:400, 1:450 and 1:500) were prepared. Test organisms (0.1 ml suspension) were inoculated into different dilutions of the disinfectants and phenol. At intervals of 5, 10 and 15 minutes, 0.1 ml was taken from each dilution and inoculated into nutrient broth (2 ml) and incubated for 48 h at 37 oC. All experiments were carried out in duplicates. D3 with active ingredients (chlorhexidine gluconate (0.3%) and cetrimide (3%)) showed the highest inhibition against all the test organisms. D4 with active ingredient (Dichloro-meta-xylenol) showed the least inhibition against all the test organisms followed by D6 with Lysol as active ingredient. The phenol coefficient of the disinfectants ranged from 0-5.5 for the test organisms. All the disinfectants exhibited antibacterial activity and the most active disinfectant contains chlorhexidine gluconate and cetrimide.
消毒剂是一种可以杀死或抑制微生物生长的化学物质,广泛用于医院和家庭。本研究旨在评估尼日利亚埃努古州恩苏卡市使用的六种家用消毒剂(D1、D2、D3、D4、D5 和 D6)对四种临床细菌分离物(包括大肠杆菌、金黄色葡萄球菌、枯草杆菌和铜绿假单胞菌)的抗菌活性。所使用的检测菌体来自恩苏卡尼日利亚大学医学中心的医学诊断实验室。配制了每种消毒剂的稀释液。使用井扩散技术测定了各种消毒剂稀释液对测试微生物的抗菌活性。采用 Rideal-Walker 法测定每种消毒剂的酚系数。制备苯酚(1:80、1:90 和 1:100)和消毒剂(1:400、1:450 和 1:500)的稀释液。将试验生物(0.1 毫升悬浮液)接种到不同稀释度的消毒剂和苯酚中。每隔 5、10 和 15 分钟,从每个稀释液中取 0.1 毫升接种到营养肉汤(2 毫升)中,在 37 oC 下培养 48 小时。所有实验均重复进行。含有活性成分(葡萄糖酸氯己定(0.3%)和西曲肽(3%))的 D3 对所有测试微生物的抑制率最高。含有活性成分(二氯甲基二甲酚)的 D4 对所有测试微生物的抑制作用最小,其次是含有来苏活性成分的 D6。消毒剂的酚系数在 0-5.5 之间。所有消毒剂都具有抗菌活性,其中最有效的消毒剂是葡萄糖酸氯己定和西曲肽。
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引用次数: 0
DEMETHOXYLATED CURCUMINOIDS AS ANTIDIABETIC COMPLICATION DRUG LEADS – IN SILICO STUDIES 作为抗糖尿病并发症药物线索的去甲氧基化姜黄素--硅学研究
Pub Date : 2024-01-20 DOI: 10.59493/ajopred/2024.1.2
O. S. Ajala, Dolapo Omolade INNOCENT-UGWU, Peace Udodiri Okechukwu, Olayinka Hannah Dada
Curcuma longa is used traditionally in the treatment of diabetes and diabetic complications. Aldose Reductase (ALR2) inhibition is a plausible therapeutic strategy against diabetic complications. This work was aimed at evaluating Curcuma longa phytochemicals, in silico, for their ALR2 inhibitory potentials. Thirty-nine (39) phytoconstituents of Curcuma longa were subjected to a succession of in silico screenings comprising molecular docking, drug-likeness and safety profiling to identify ALR2 inhibitor leads, validating their binding interactions with molecular dynamics simulations at 50 ns simulation time. The in silico evaluations afforded two demethoxylated curcuminoids, bisdemethoxycurcumin and demethoxycurcumin, as potential ALR2 inhibitor leads forming stable ALR2 complexes, their relative potencies correlating to their degrees of demethoxylation. The two curcuminoids are herein recommended as leads for the discovery of ALR2 inhibitory antidiabetic complication drug leads.
姜黄在传统上被用于治疗糖尿病和糖尿病并发症。抑制醛糖还原酶(ALR2)是治疗糖尿病并发症的一种可行策略。这项工作旨在对莪术植物化学物质的 ALR2 抑制潜力进行硅学评估。研究人员对 39 种莪术植物成分进行了一系列硅学筛选,包括分子对接、药物相似性和安全性分析,以确定 ALR2 抑制剂的先导物,并在 50 ns 模拟时间内通过分子动力学模拟验证其结合相互作用。硅学评估发现了两种去甲氧基姜黄素,即双去甲氧基姜黄素和去甲氧基姜黄素,它们是潜在的 ALR2 抑制剂,能形成稳定的 ALR2 复合物,其相对效力与去甲氧基程度相关。在此推荐将这两种姜黄素作为发现 ALR2 抑制性抗糖尿病并发症药物的线索。
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引用次数: 0
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AFRICAN JOURNAL OF PHARMACEUTICAL RESEARCH AND DEVELOPMENT
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