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Effects of beetroot (Beta vulgaris) supplements on selective enzymatic and non-enzymatic antioxidants in iron deficiency anemia. 甜菜根(Beta vulgaris)补充剂对缺铁性贫血患者选择性酶和非酶抗氧化剂的影响。
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-07-01
Shamaila Khalid, Syed Mohammad Mahboob Alam, Syed Saud Hassan, Shaikh Nadeem Ahmad, Dabeeran Zehra, Hafiz Syed Imran-Ul-Haq

Iron deficiency anemia (IDA) is not only associated with iron deficiency but has shown strong association with the over production of free radicles and deficiency of antioxidant enzymes. The result of this imbalance is oxidative stress (OS) which is now considered as an important associated factor with various diseases. Treating IDA in most of cases with oral iron supplements results in more OS as iron is a transition metal. A more suitable alternate for iron supplementation is Beta vulgaris supplement, which being herbal in origin is far less associated with side effects. We studied effects of beta vulgaris supplements on enzymatic and non-enzymatic antioxidants in IDA patients. A significant increase in all study parameters were observed after treatment (p <0.05). When pre-supplemental values of super oxide dismutase (SOD) and reduced glutathione (GSH-PX) of IDA were compared with post-supplemental values, they were significantly low (p <0.05). A positive correlation was noted between the two antioxidants and hemoglobin (Hb) values suggesting a direct relationship between antioxidant status and Hb levels. Non enzymatic antioxidants included vitamin A,C and E. We also found a significant improvement (p <0.05) of these vitamins when compared with their initial values and the control group. Our study shows improvement of antioxidant status of anemic patients with 12 week supplementation of Beta vulgaris.

缺铁性贫血(IDA)不仅与缺铁有关,还与自由基产生过多和抗氧化酶缺乏密切相关。这种失衡的结果就是氧化应激(OS),而氧化应激目前被认为是各种疾病的重要相关因素。在大多数情况下,通过口服铁补充剂治疗 IDA 会导致更多的 OS,因为铁是一种过渡金属。β-芸苔素补充剂是一种更合适的铁补充剂替代品,它源自草本,副作用小得多。我们研究了 beta vulgaris 补充剂对 IDA 患者酶和非酶抗氧化剂的影响。治疗后,所有研究参数均有明显增加(p
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引用次数: 0
Attenuation of age-related cognitive decline and memory deficits through apomorphine administration. 服用阿朴吗啡可减轻与年龄有关的认知衰退和记忆障碍
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-07-01
Huma Ikram, Rumaisa Zakir, Darakhshan Jabeen Haleem

Oxidative stress, stemming from heightened production of reactive oxygen species and free radicals, significantly contributes to the aging process. Apomorphine emerges as a pivotal medication for managing Alzheimer's, Parkinson's and other age-related conditions. This study aims to explore the memory-enhancing and neuroprotective properties of apomorphine, utilizing male Albino Wistar rats aged 4 and 24 months as subjects. Rats were intraperitoneally injected with apomorphine for 6 days. Decreased glutathione peroxidase, superoxide dismutase and catalase activities with increased lipid peroxidation were observed in the brain and plasma samples of aged rats, which were reversed upon apomorphine administration. Superoxide dismutase (SOD) and AChE activities were significantly decreased along with a decline in short-term- and long-term memory of aged rats, which was reverted by apomorphine. Furthermore, a notable reduction in biogenic amines and metabolite levels in the brains of aged rats was reversed in aged rats treated with apomorphine. The findings indicate a significant restoration of memory impairment and oxidative stress in aged rats by apomorphine. Overall, our data suggests that apomorphine, at a dosage of 1mg/kg, holds promise as a potential therapeutic intervention for dementia and associated disorders in elderly patients.

氧化应激源于活性氧和自由基的大量产生,是导致衰老的重要原因。阿扑吗啡是治疗阿尔茨海默氏症、帕金森氏症和其他老年相关疾病的关键药物。本研究以年龄分别为 4 个月和 24 个月的雄性白化 Wistar 大鼠为研究对象,旨在探索阿扑吗啡增强记忆和保护神经的特性。大鼠腹腔注射阿朴吗啡 6 天。在老龄大鼠的大脑和血浆样本中观察到谷胱甘肽过氧化物酶、超氧化物歧化酶和过氧化氢酶活性降低,脂质过氧化反应增加,而服用阿朴吗啡后这些现象得到逆转。老龄大鼠的超氧化物歧化酶(SOD)和乙酰胆碱酯酶(AChE)活性明显降低,同时短期和长期记忆力也有所下降,而服用阿朴吗啡后这种情况得到了逆转。此外,老年大鼠大脑中生物胺和代谢物水平的明显降低在使用阿朴吗啡治疗后也得到了逆转。这些研究结果表明,阿扑吗啡能显著恢复老年大鼠的记忆损伤和氧化应激。总之,我们的数据表明,阿扑吗啡的剂量为1毫克/千克,有望成为老年痴呆症和相关疾病的潜在治疗干预措施。
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引用次数: 0
Effect of Bixie combined with perioperative multimodal analgesia management on postoperative pain and wound healing of mixed hemorrhoids. Bixie 联合围手术期多模式镇痛对混合痔术后疼痛和伤口愈合的影响。
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-07-01
Yuanyuan Wu, Lanlan Wu, Yifang Ma, Jianguo Li, Xiangyang Song, Jun Li, Xiaofeng Song

We were to explore the effect of Bixie combined with perioperative multimodal analgesia management on postoperative pain and wound healing of mixed hemorrhoids. A total of 240 patients with mixed hemorrhoids in this hospital from June 2022 to September 2023 were chosen, with 120 in the control group receiving perioperative multimodal analgesia management and 120 in the observation group receiving Bixie combined with perioperative multimodal analgesia management. The results showed that compared with the control group, the observation group had lower visual analogue scale (VAS) scores at 1, 3, 5 and 7 days after the surgery; the 5-hydroxytryptamine (5-HT), prostaglandin E2 (PGE2), nitric oxide (NO), interleukin-2 (IL-2), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) of the observation group at 24 hours and 72 hours after the surgery were lower; the vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), platelet-derived growth factor (PDGF) and wound healing rate of the observation group at 7 days after the surgery were higher; the total effective rate of the observation group was higher. Therefore, combining Bixie with perioperative multimodal analgesia management could improve postoperative pain, decrease inflammatory factor levels, promote angiogenesis and accelerate wound healing in patients with mixed hemorrhoids.

我们旨在探讨Bixie联合围手术期多模式镇痛管理对混合痔术后疼痛和伤口愈合的影响。选取2022年6月-2023年9月该院收治的混合痔患者共240例,其中对照组120例接受围手术期多模式镇痛管理,观察组120例接受Bixie联合围手术期多模式镇痛管理。结果显示,与对照组相比,观察组术后1、3、5和7天的视觉模拟量表(VAS)评分较低;观察组术后24小时和72小时的5-羟色胺(5-HT)、前列腺素E2(PGE2)、一氧化氮(NO)、白细胞介素-2(IL-2)、白细胞介素-6(IL-6)和肿瘤坏死因子-α(TNF-α)均较低;观察组术后 7 天的血管内皮生长因子(VEGF)、碱性成纤维细胞生长因子(bFGF)、血小板衍生生长因子(PDGF)和伤口愈合率较高;观察组的总有效率较高。因此,将Bixie与围手术期多模式镇痛治疗相结合,可改善混合痔患者的术后疼痛,降低炎性因子水平,促进血管生成,加速伤口愈合。
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引用次数: 0
Identification of lovastatin production in Aspergillus terreus strain (KF971363.1) and its antifungal role. 鉴定土曲霉菌株(KF971363.1)中洛伐他汀的产生及其抗真菌作用。
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-07-01
Aasma Khalid, Fatima Ismail

Lovastatin has received interest for its potential therapeutic use in treating numerous diseases, for example, the blood cholesterol level by restraining hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. The research utilized the fungal growth bioassay technique to disengage and evaluate filamentous organism for the lovastatin creation. The clever type of Aspergillus terreus (KF971363.1) was embraced for lovastatin creation by solid-state fermentation (SSF). Lovastatin production was optimized using physiological parameters such as pH and temperature at SSF. The addition of nitrogen source enhanced the production of lovastatin by the breakdown of lignocellulose that improved the production of lovastatin. The research verified a yeast growth inhibition bioassay approach, in addition to thin-layer chromatography and liquid chromatography-mass spectrometry (LC-MS). All of these techniques were used to confirm lovastatin production. The purified extract subjected to the TLC analysis showed retention factor (Rf) value of 0.73. Moreover, the inhibition bioassay method reassures the lovastatin production by comparing the zone of inhibition against C. albicans.

洛伐他汀因其在治疗多种疾病方面的潜在疗效而受到关注,例如通过抑制羟基-3-甲基戊二酰辅酶 A(HMG-CoA)还原酶来降低血液中的胆固醇水平。该研究利用真菌生长生物测定技术来分离和评估丝状生物对洛伐他汀的产生作用。通过固态发酵(SSF)技术,采用聪明的赤曲霉菌(KF971363.1)制造洛伐他汀。利用 SSF 的 pH 值和温度等生理参数对洛伐他汀的生产进行了优化。添加氮源可通过分解木质纤维素提高洛伐他汀的产量。研究验证了酵母生长抑制生物测定方法,以及薄层色谱法和液相色谱-质谱法(LC-MS)。所有这些技术都用于确认洛伐他汀的生产。纯化的提取物经 TLC 分析后,保留因子(Rf)值为 0.73。此外,抑菌生物测定法通过比较对白僵菌的抑菌区来确定洛伐他汀的产量。
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引用次数: 0
Ascorbic acid mitigates doxorubicin-induced spleen injury in rats: Histopathological and immunohistochemical insights. 抗坏血酸可减轻多柔比星诱导的大鼠脾脏损伤:组织病理学和免疫组织化学的启示。
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-05-01
Arzu Gezer, Mustafa Ozkaraca, Ebru Karadag Sari, Gursel Bedir, Pelin Aydın, Hasan Asker, Am Abd El-Aty

This study assessed the protective potential of ascorbic acid against doxorubicin-induced spleen tissue damage in rats. Twenty-eight male Sprague-Dawley rats were divided into four groups. The control group received saline every other day at a dose of 1mL throughout the experiment. The ascorbic acid group was administered 50mg/kg of ascorbic acid daily for 10 days. The doxorubicin group received a single dose of 15mg/kg of doxorubicin on day 7. The ascorbic acid + doxorubicin group received both 50mg/kg of ascorbic acid daily for 10 days and a single dose of 15mg/kg of doxorubicin on day 7. After the experiment, splenic tissue samples were examined histopathologically and immunohistochemically. Histopathological analysis revealed edema, destruction and degeneration in the doxorubicin group, but these changes were alleviated in the ascorbic acid-treated group, approaching control group levels. Immunohistochemical analysis showed increased CD4+ and CD8+ cell immunopositivity in the ascorbic acid + doxorubicin group compared to the doxorubicin group. Biochemical tests indicated that doxorubicin reduced superoxide dismutase activity and increased malondialdehyde levels, whereas ascorbic acid mitigated these effects. The findings suggest that ascorbic acid may have a protective role against doxorubicin-induced spleen injury in rats.

本研究评估了抗坏血酸对多柔比星诱导的大鼠脾组织损伤的保护潜力。28 只雄性 Sprague-Dawley 大鼠被分为四组。对照组在整个实验期间每隔一天接受一次生理盐水,剂量为 1 毫升。抗坏血酸组每天服用 50 毫克/千克抗坏血酸,持续 10 天。多柔比星组在第 7 天单次服用 15 毫克/千克多柔比星。抗坏血酸+多柔比星组在10天内每天服用50毫克/千克抗坏血酸,并在第7天单次服用15毫克/千克多柔比星。实验结束后,对脾脏组织样本进行了组织病理学和免疫组织化学检查。组织病理学分析表明,多柔比星组出现水肿、破坏和变性,而抗坏血酸处理组的这些变化有所缓解,接近对照组的水平。免疫组化分析显示,与多柔比星组相比,抗坏血酸+多柔比星组的 CD4+ 和 CD8+ 细胞免疫阳性率增加。生化测试表明,多柔比星降低了超氧化物歧化酶的活性,增加了丙二醛的含量,而抗坏血酸减轻了这些影响。研究结果表明,抗坏血酸可能对多柔比星诱发的大鼠脾脏损伤具有保护作用。
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引用次数: 0
Aloe vera leaf mucilage and lemon oil as potential penetration-enhancing agents to increase lornoxicam transdermal administration using nano vesicular gel. 将芦荟叶粘液和柠檬油作为潜在的渗透增强剂,利用纳米囊状凝胶增加洛诺昔康的透皮给药。
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-05-01
Gopinath Subramaniyan, Shaik Rubina, Bachu Venkata Ramana, A Meriton Stanley, Devasena Srinivasan

The goal of the existing work was to create matrix transdermal patches with lornoxicam (LXM) gel using lemon oil (LO) and Aloe vera leaves mucilage (AVLM) as penetration enhancers to boost LXM transport crossways the skin and test its in vivo analgesic effects. Nine formulas were produced for this purpose using Design Expert® 11 in line with CCD design. The response factors, on the other hand, were Q1d (Y1), Q2d (Y2) and Q3d, or LXM permeation at days 1, 2 and 3. The AVLM concentration (X1) and lemon oil (X2) were selected as independent variables. The optimized patch's skin sensitivity response and analgesic activity were tested on rats. The results exhibited that a matrix system with prolonged (zero-order) LXM release of 24.15% (@24h), 49.00% (@48h) and 69.45% (optimized for the needed analgesic asset by using AVLM and LO as penetration enhancers. It was resolute that the formulation known as LTDP-8, which contains 3mL of AVLM and LO as permeability enhancers, is the best one. In light of its ability to administer LXM across the skin sustainably while producing a tolerable analgesic effect. The study concludes that the artificial transdermal LXM delivery system is a suitable substitution for the oral route.

现有工作的目标是利用柠檬油(LO)和芦荟叶粘液(AVLM)作为渗透增强剂,制作含有洛诺昔康(LXM)凝胶的基质透皮贴片,以促进 LXM 在皮肤上的跨膜运输,并测试其体内镇痛效果。为此,使用 Design Expert® 11 按照 CCD 设计制作了九种配方。反应因子则为 Q1d(Y1)、Q2d(Y2)和 Q3d,即 LXM 在第 1、2 和 3 天的渗透率。选择 AVLM 浓度(X1)和柠檬油(X2)作为自变量。在大鼠身上测试了优化贴片的皮肤敏感反应和镇痛活性。结果表明,通过使用 AVLM 和 LO 作为渗透增强剂,基质系统的 LXM 长效(零阶)释放率分别为 24.15%(24 小时)、49.00%(48 小时)和 69.45%(针对所需的镇痛资产进行了优化)。经确定,含有 3 毫升 AVLM 和 LO 作为渗透增强剂的 LTDP-8 配方是最佳配方。鉴于它能够持续地通过皮肤给药 LXM,同时产生可耐受的镇痛效果。研究得出结论,人工透皮 LXM 给药系统是口服途径的合适替代品。
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引用次数: 0
Effect analysis of tanshinone IIA sulfonate sodium combined with a-lipoic acid in patients with diabetes peripheral neuropathy. 丹参酮 IIA 磺酸钠联合硫辛酸对糖尿病周围神经病变患者的疗效分析。
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-05-01
Mingyu Cheng, Xiaoling Jia, Jiangbo Zhao

To investigate the effect of tanshinone IIA sulfonate sodium combined with α-Lipoic acid on fasting blood sugar (FPG), 2h postprandial blood glucose (2hPG), total cholesterol (TG), triacylglycerol (TC) and therapeutic effect in patients with diabetes peripheral neuropathy (DPN). The control group (n=52) was treated with tanshinone IIA sodium sulfonate alone. The study group was treated with α-Lipoic acid and tanshinone IIA sodium sulfonate. The changes in blood glucose, blood lipid levels, oxidative stress indicators and the improvement of nerve function conduction of both two groups were compared. After treatment, study group's FPG, 2hPG, TG and TC were found to be lower than the control group (P<0.05). The levels of Super oxide dismutase (SOD) and nitric oxide (NO) in the study group were higher than those in the control group. The study group had lower Malondialdehyde (MDA) (P<0.05). The study group had higher nerve motor conduction velocity (MNCV) and sensory nerve conduction velocity (SNCV) (P<0.05). Tanshinone IIA sulfonate sodium combined with α-Lipoic acid can improve DPN patients' blood glucose and lipid levels, alleviate the oxidative stress reaction of the body, promote the recovery of nerve conduction function and enhance the therapeutic effect.

目的 研究丹参酮 IIA 磺酸钠联合α-硫辛酸对糖尿病周围神经病变(DPN)患者空腹血糖(FPG)、餐后 2 小时血糖(2hPG)、总胆固醇(TG)、三酰甘油(TC)的影响及治疗效果。对照组(52 人)单独使用丹参酮 IIA 磺酸钠治疗。研究组使用α-硫辛酸和丹参酮 IIA 钠磺酸盐治疗。比较两组患者血糖、血脂、氧化应激指标的变化以及神经功能传导的改善情况。治疗后,研究组的 FPG、2hPG、TG 和 TC 均低于对照组(P<0.05)。
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引用次数: 0
Formulation and development of frovatriptan succinate in situ gel for nasal drug delivery: In vitro and ex vivo evaluation. 用于鼻腔给药的琥珀酸伐他普坦原位凝胶的配制与开发:体外和体内评估。
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-05-01
Mohammed Layth Hamzah, Hanan Jalal Kassab

Magrain is a depleting disease that sometimes requires extensive treatment, ideally with medication that targets the brain, with minimized systemic adverse effects, preferably with a single daily medication; these properties are offered partially by the current dosage form of Frovatriptan. formulation of Frovatriptan binary ethosome into mucoadhesive nasal in situ gel to extend the drug's residence time. The particle size was ‎154.1±4.38‎ nm of the Frovatriptan binary ethosome. In situ, gel formulas were prepared to utilize the cold technique, using 18%w/v poloxamer 407 with different concentrations of Carbopol 934 and the clarity, pH, Frovatriptan content spreadability, mucoadhesive force, in vitro diffusion via nasal mucosa and the optimal formula underwent further investigations. In-situ gel F2 (0.2% Carbopol) demonstrated the best spreadability of 12.88±0.186 cm2/min, 99% drug content mucoadhesive strength of 645.32±0.054 dynes/cm2, percent release of 98.56±0.041 after 24 hours and permeability increased by around 3.68-fold compared to the pure drug and histopathologically showed favorable outcomes. Mucoadhesive Frovatriptan-binary ethosome-loaded nasal in situ gel is an effective method of treating migraines.

马格列是一种消耗性疾病,有时需要广泛的治疗,理想的治疗方法是使用针对大脑的药物,将全身不良反应降至最低,最好每天只需服用一种药物;弗罗阿曲普坦的现有剂型部分具备这些特性。弗罗阿曲普坦二元乙素体的粒径为 154.1±4.38 nm。利用冷冻技术,使用18%w/v的poloxamer 407和不同浓度的Carbopol 934制备了原位凝胶配方,并对其透明度、pH值、弗罗阿曲普坦含量的铺展性、粘附力、体外经鼻粘膜扩散性和最佳配方进行了进一步研究。与纯药物相比,原位凝胶 F2(0.2% Carbopol)具有最佳的铺展性(12.88±0.186 cm2/min)、99%药物含量的粘附力(645.32±0.054 dynes/cm2)、24 小时后的释放率(98.56±0.041)和渗透性增加了约 3.68 倍,组织病理学也显示了良好的结果。粘液黏附型弗罗阿曲普坦-二元乙素鼻腔原位凝胶是治疗偏头痛的一种有效方法。
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引用次数: 0
Role of metformin in male oxidative stress infertility (MOSI): An in vitro experimental study. 二甲双胍在男性氧化应激性不育症(MOSI)中的作用:体外实验研究。
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-05-01
Nida Farooqui, Sher Khan, Nida Zahid, Syed Muhammad Nazim, Mohammad Tahir, Rehana Rehman

The study aimed to determine the in-vitro effect of metformin on total antioxidant capacity (TAC) of seminal samples of infertile male subjects. It was conducted from January to June 2022 on forty-four seminal plasma samples collected from male infertile patients, age ranging from 18 to 55 years. All 44 semen samples were treated as three distinct groups: (i) a control group (ii) a study group subjected to oxidative stress (OS) induction and (iii) a test group exposed to OS induction and subsequent treatment with metformin. OS was introduced by using commercially available 100μM hydrogen peroxide (H2O2) and incubated for twenty-four hours at 37ºC. After that 1 ml of 100 mmol/l concentration of commercially available Metformin (PHR 1331, CAS: 461-58-5) was administered to test group samples for additional 24h at 37ºC. Low levels of TAC were observed after OS induction in comparison to the control group (p=0.01). In test samples (after treatment with Metformin), a positive correlation of TAC with sperm count, normal sperm morphology and sperm motility were observed however, results were not significant. The antioxidant effect of Metformin was shown to improve the antioxidant capacity of OS induced samples and their sperm parameters in seminal plasma of infertile male subjects.

该研究旨在确定二甲双胍对不育男性精液样本总抗氧化能力(TAC)的体外影响。研究于 2022 年 1 月至 6 月进行,采集了 44 份男性不育患者的精浆样本,他们的年龄在 18 岁至 55 岁之间。所有 44 份精液样本被分为三组:(i) 对照组;(ii) 氧化应激(OS)诱导研究组;(iii) OS 诱导试验组,试验组随后接受二甲双胍治疗。使用市售的 100μM 过氧化氢(H2O2)诱导氧化应激,并在 37ºC 温度下培养 24 小时。之后,在 37ºC 下给测试组样本再注射 1 毫升 100 毫摩尔/升浓度的市售二甲双胍(PHR 1331,CAS:461-58-5)24 小时。与对照组相比,OS 诱导后观察到的 TAC 水平较低(p=0.01)。在测试样本中(二甲双胍治疗后),观察到 TAC 与精子数量、正常精子形态和精子活力呈正相关,但结果并不显著。研究表明,二甲双胍的抗氧化作用提高了不育男性精浆中OS诱导样本的抗氧化能力及其精子参数。
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引用次数: 0
Effective inhibition of Sesbania grandiflora bioactive compounds against C-di-GMP phosphodiesterase of Pseudomonas aeruginosa. 大叶芝麻生物活性化合物对铜绿假单胞菌 C-di-GMP 磷酸二酯酶的有效抑制。
IF 0.7 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2024-05-01
Srilakshmi Ravi, Subashkumar Rathinasamy, Sivaranjini Annamalai, Shoba Gunasekaran, Balamuralikrishnan Balasubramanian, Souparnika Biju Reji, Arumugam Vijaya Anand, Santhosh Baboo Sethuraman, Shivakumar Bandhumy Lingam

Sesbania grandiflora also known as Agasthya has potent antibiofilm activity and its bioactive compounds obtained from the leaves are medicarpin, isoniazid and 4-methyl oxazole. Extra cellular polymeric substances (EPS) created by the bacterium involve the formation of biofilm and this causes the infections such as nosocomial infections, and urinary tract infections. Pseudomonas aeruginosa has been linked with high levels of intracellular Cyclic-di-Guanosine Monophosphate (c-di-GMP; PA4781) in biofilm formation. In this study, Human BLAST analysis of c-di-GMP Phosphodiesterase has been carried out and it shows an insignificant result and it is believed to be a possible drug target for UTI infection caused by P. aeruginosa. Its protein structure was retrieved from PDB database which was subjected to molecular docking against S. grandiflora bioactive compounds and control drug ciprofloxacin. Compounds taken for the study were screened for ADMET properties and drug-likeliness properties. Molecular interaction analysis of c-di-GMP with medicarpin compound shows -6.75 Kcal/mol binding energy with two hydrogen bonds when compared to the control drug with -6.86 kcal/mol binding energy and two hydrogen bonds respectively. Hence, our findings in the current study suggest that medicarpin could be an inhibitor of c-di-GMP and possess anti-biofilm activity, which could be validated experimentally.

大叶芝麻(Sesbania grandiflora)又名 Agasthya,具有强大的抗生物膜活性,从叶片中提取的生物活性化合物包括 medicarpin、异烟肼和 4-甲基噁唑。细菌产生的细胞外高分子物质(EPS)会形成生物膜,从而导致感染,如医院内感染和尿路感染。铜绿假单胞菌与生物膜形成过程中细胞内高水平的单磷酸环二鸟苷(c-di-GMP;PA4781)有关。在本研究中,对 c-di-GMP 磷酸二酯酶进行了人类 BLAST 分析,结果显示该酶并不显著,因此认为它可能是铜绿假单胞菌引起的UTI 感染的一个药物靶点。研究人员从 PDB 数据库中检索了它的蛋白质结构,并将其与 S. grandiflora 生物活性化合物和对照药物环丙沙星进行了分子对接。研究中使用的化合物都经过了 ADMET 特性和可药性特性筛选。c-di-GMP 与药黄素化合物的分子相互作用分析表明,药黄素化合物的结合能为 -6.75 Kcal/mol,有两个氢键,而对照药物的结合能为 -6.86 kcal/mol,有两个氢键。因此,本研究的结果表明,茜草素可能是一种 c-di-GMP 抑制剂,具有抗生物膜活性,这一点可以通过实验来验证。
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引用次数: 0
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Pakistan journal of pharmaceutical sciences
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