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Evaluation of bromelain and temozolomide synergistic combination in human glioblastoma cells 评估菠萝蛋白酶和替莫唑胺在人胶质母细胞瘤细胞中的协同作用
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-10-23 DOI: 10.1007/s13596-023-00717-y
Megha Gautam, Reema Gabrani

The development of effective therapy is required for glioblastoma multiforme (GBM) patients because of the resistance action to temozolomide (TMZ). Bromelain (BRO) is a plant-derived therapeutic used against inflammation. The objective of this study is to appraise the effect of the BRO + TMZ combination on U87MG and LN229 cells and investigate its mechanism. The BRO + TMZ treatment resulted in synergistic effects that restricted cell growth and inhibited the colony formation of GBM cells. The combined treatment led to the initiation of early apoptosis resulting in the overexpression of BAX/caspase-3 (CASP3) and decreased transcript level of BCL-2. The BRO + TMZ induced the arrest in G0/G1 phase and decreased the migration mediated by the dysregulation of MMP-2 and MMP-9. The BRO and TMZ combination treatment was observed to be more effective than the individual compound to inhibit cell growth in human GBM cell lines.

由于多形性胶质母细胞瘤(GBM)患者对替莫唑胺(TMZ)产生抗药性,因此需要开发有效的疗法。菠萝蛋白酶(BRO)是一种植物提取的治疗炎症的药物。本研究的目的是评估 BRO + TMZ 联合疗法对 U87MG 和 LN229 细胞的影响,并研究其作用机制。BRO + TMZ治疗产生了协同效应,限制了细胞生长并抑制了GBM细胞的集落形成。联合治疗导致细胞早期凋亡,BAX/caspase-3(CASP3)过度表达,BCL-2转录水平下降。BRO + TMZ可诱导细胞停滞在G0/G1期,并在MMP-2和MMP-9失调的介导下减少细胞迁移。与单个化合物相比,BRO 和 TMZ 联合治疗对人类 GBM 细胞株细胞生长的抑制效果更好。
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引用次数: 0
Antimycobacterial, antibiofilm and efflux pump inhibitory activity of extracts from selected Combretum species used in traditional medicine in Zimbabwe 津巴布韦传统医学中使用的部分康柏属植物提取物的抗霉菌、抗生物膜和外排泵抑制活性
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-10-18 DOI: 10.1007/s13596-023-00711-4
Sharon Netsai Chikafa, Chi Godloves Fru, Stanley Mukanganyama

Non-tuberculous mycobacteria infect mostly immunocompromised people. NTM infections incidence and prevalence increase has led to a public health problem. Combretum species are used as food by humans and animals, and medicinal purposes. The aim of the study was to evaluate the antimycobacterial effects of plant extracts from selected Combretum species on Mycobacterium smegmatis and Mycobacterium aurum as well as their mode of action on the most susceptible organisms. Antimycobacterial activity of the plant extracts was screened. Mycobacterium smegmatis was more susceptible to the extracts. The potent Combretum extracts were investigated for their effects on Rhodamine 6G transport and biofilms in M. smegmatis. The amount of Rhodamine 6G accumulated in M. smegmatis in the presence of extracts were also investigated. The C. zeyheri acetone extracts were the most potent efflux pump inhibitors. Surface extracts from C. zeyheri were the most potent disrupters and inhibitors of biofilms. The ethylacetate extract of another species, C. apiculatum lacked the effect on biofilms and this may be due to the lack of penetration of the extract into the already established biofilm. The ultra-high performance liquid chromatography UPHLC-MS/MS analysis of acetone extracts from C. zeyheri indicated the presence of cirsimaritin, quinic acid, and ampelopsin glucoside and these could have contributed to the antimycobacterial activities of the extract. In conclusion, phytochemicals from C. zeyheri, C. platypetalum, C. apicultum species used in traditional medicine in Zimbabwe showed antimycobacterial and antibiofilm activity and may be used as sources of lead compounds targeting non-tuberculosis infections caused by M. smegmatis.

非结核分枝杆菌主要感染免疫力低下的人群。非结核分枝杆菌感染发病率和流行率的上升已成为一个公共卫生问题。Combretum 物种被人类和动物用作食物和药用。这项研究的目的是评估从选定的康普瑞特木物种中提取的植物提取物对烟分枝杆菌和金黄色葡萄球菌的抗霉菌作用,以及它们对最易感生物的作用模式。对植物提取物的抗霉菌活性进行了筛选。分枝杆菌对这些提取物更易感。研究了强效康柏提取物对罗丹明 6G 运输和烟曲霉生物膜的影响。此外,还研究了萃取物在烟曲霉体内积累的罗丹明 6G 量。C. zeyheri丙酮提取物是最有效的外排泵抑制剂。C. zeyheri 的表面提取物是最有效的生物膜破坏剂和抑制剂。另一个物种 C. apiculatum 的乙酸乙酯提取物对生物膜没有影响,这可能是由于提取物无法渗透到已经形成的生物膜中。对 C. zeyheri 的丙酮提取物进行的超高效液相色谱 UPHLC-MS/MS 分析表明,该提取物中含有卷曲霉素、奎宁酸和安瓿葡糖苷,这些物质可能有助于提高其抗炎活性。总之,津巴布韦传统医学中使用的 C. zeyheri、C. platypetalum 和 C. apicultum 物种的植物化学物质显示出抗结核菌和抗生物膜活性,可用作针对由烟曲霉菌引起的非结核感染的先导化合物来源。
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引用次数: 0
A review on therapeutic potential of wild mushrooms with their relative status in Chhattisgarh, Central India 印度中部恰蒂斯加尔邦野生蘑菇的治疗潜力及其相对状况综述
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-10-10 DOI: 10.1007/s13596-023-00713-2
Srishti Verma, Samay Tirkey, Kamlesh Shukla

Wild mushrooms are a rich source of bioactive compounds. They have diverse pharmacological and nutraceutical importance that help to boost immunity against many life-threatening diseases. They have biological functions such as; antibacterial, antifungal, antioxidant, antiviral, anticancer, immunomodulatory, and hepatoprotective activities, etc. Besides, they are globally used as a functional food due to low calorie (low lipid) and rich in proteins and carbohydrates. Overall, they are abundant in vitamins, minerals, fibres, nutrients, and a mighty source of potential bioactive secondary metabolites. This review aims to focus on the therapeutic values of wild mushrooms, which are found worldwide, and the availability of such wild mushrooms in Chhattisgarh based on previous literatures, to account the status of study on mushrooms in this state. It is found that a little to no work has been done on the diversity and therapeutic potentials of wild mushrooms in Chhattisgarh. This review gives a solid basis to investigate their properties from this region to support the livelihood of humanity.

野生蘑菇是生物活性化合物的丰富来源。它们具有多种药理和营养保健作用,有助于提高免疫力,预防多种威胁生命的疾病。它们具有抗菌、抗真菌、抗氧化、抗病毒、抗癌、免疫调节和保肝等生物功能。此外,由于低热量(低脂)、富含蛋白质和碳水化合物,它们在全球被用作功能性食品。总之,它们含有丰富的维生素、矿物质、纤维和营养物质,是潜在生物活性次生代谢物的重要来源。本综述旨在重点介绍野生蘑菇的治疗价值,野生蘑菇在世界各地都有发现,本综述根据以往的文献资料,介绍恰蒂斯加尔邦的野生蘑菇供应情况,并说明该邦对蘑菇的研究现状。研究发现,关于恰蒂斯加尔邦野生蘑菇的多样性和治疗潜力的研究很少,甚至没有。这篇综述为研究该地区野生蘑菇的特性、改善人类生活提供了坚实的基础。
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引用次数: 0
Detailed review on phytosomal formulation attenuating new pharmacological therapies 关于植物体制剂减弱新药物疗法的详细综述
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-10-06 DOI: 10.1007/s13596-023-00712-3
Jyotsana Dwivedi, Pranjal Sachan, Pranay Wal, Sumeet Dwivedi, Mukesh Chandra Sharma, Surada Prakash Rao

Nowadays, numerous diseases are benefitted from phytosomal therapy. However, poor selectivity and bioavailability may be limiting factors of their therapeutic applicability. The distribution of hydrophobic phytochemicals has been proposed as a potential use for nanovesicles. Phytosomes are more stable, according to a recent assessment of the literature, since a chemical link is created between the phospholipid molecules and the phytoconstituent. Fewer phytoconstituents are needed, extending the action, and they are more bioavailable in their complex form. Due to the easy preparation of the bilayer vesicles and their adaptability, they have been widely used and approved by the scientific literature. In this review paper we describe the promising clinical and experimental findings of more than 100 phytosomal studies. The effects of phytosomes on the immunological, circulatory, gastrointestinal, genitourinary, respiratory, integumentary, central and peripheral nervous systems, and musculoskeletal systems have all been studied according to the research compiled. These results confirm the greater effectiveness of phytosomes, both in terms of biological activity or reduced dosage, highlighting curcumin and silymarin as the most formulated compounds. Using such formulations to increase the bioactivity of phytochemicals and their bioavailability generally has advantages, allowing for lower dosages or higher biological activity as compared to using unformulated compounds. The conclusion of this study encourages the researchers to transfer their findings from research laboratories to market, for a further development of these products. The potential role of phytophospholipid complexes has a promising future for pharmaceutical applications with the help of physicians and other researchers.

如今,许多疾病都能从植物体疗法中获益。然而,选择性差和生物利用率低可能是限制其治疗适用性的因素。疏水性植物化学物质的分布被认为是纳米微粒的潜在用途。根据最近的文献评估,由于磷脂分子与植物成分之间建立了化学联系,因此植物体更加稳定。所需的植物成分更少,作用时间更长,而且复合形式的植物成分生物利用率更高。由于双层囊泡易于制备且适应性强,它们已被广泛使用并得到科学文献的认可。在这篇综述论文中,我们介绍了 100 多项植物体研究的临床和实验结果。根据所汇编的研究成果,我们研究了植物体对免疫系统、循环系统、胃肠道系统、泌尿生殖系统、呼吸系统、皮肤、中枢神经系统和周围神经系统以及肌肉骨骼系统的影响。这些研究结果证实,无论是在生物活性方面还是在减少用量方面,植物载体都具有更大的功效,其中姜黄素和水飞蓟素是配制最多的化合物。与使用未配制的化合物相比,使用此类配制物来提高植物化学物质的生物活性及其生物利用度通常具有优势,可以降低用量或提高生物活性。这项研究的结论鼓励研究人员将他们的研究成果从研究实验室推向市场,以进一步开发这些产品。在医生和其他研究人员的帮助下,植物磷脂复合物在医药应用中的潜在作用前景广阔。
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引用次数: 0
Ethnomedicinal uses, biological activities, and toxicity of Voacanga africana Stapf Ex Scott-Elliot Voacanga africana Stapf Ex Scott-Elliot 的民族药用价值、生物活性和毒性
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-10-03 DOI: 10.1007/s13596-023-00709-y
Emelia Oppong Bekoe, Jochebed A. Amene Opare, Michael Lartey, Patrick Amoateng

Voacanga africana, is a medicinal plant widely used in many African countries. Various parts of this plant are used, but more especially the seeds are held in high esteem for it’s their additional economic value due to the presence of the alkaloids ibogaine, tabersonine, and voacangine. These alkaloids have peculiar medicinal uses in the treatment of psychotic ailments, drug addiction, and also serve as precursors for drug synthesis. V. africana is traditionally used to treat a myriad of diseases including malaria, worm infestation, amoebiasis, ulcers, pain, cardiovascular conditions, depression, fatigue, shortness of breath, diarrhoea, gynaecological conditions, delayed labour, kidney conditions, malaria, asthma and convulsions, however not all these have been investigated. Studies have demonstrate possible efficacy in the treatment of worm infestation, amoebiasis, ulcer, pain and inflammation, cardiovascular condition, depression, diarrhoea, onchocerciasis, mental disorder, and microbial infections. The plant also has CNS, neuro-protective, sedative, anti-microbial, anti-tumor and anti-oxidant activities. Further studies is however needed to verify its activity in the treatment of malaria, fatigue, gynaecological and, labour conditions, respiratory conditions and carious teeth. With respect to safety, the ethanolic leaf extract is reported to be relatively non-toxic with an estimated LD50 of ≥ 5000 mg while the aqueous leaf extract had no significant alteration on the blood biochemistry or histopathology of essential organs in murine models. Some isolated alkaloids from this plant: vobtusine, voacangine and voacamine are however known to exhibit toxicity in the form of cardiac depressor activity, asphyxia and convulsions, hypertension and CNS depressant activities. In addition to alkaloids, the plant is also rich in saponins, tannins, terpenes, steroids, flavonoids, phenols, anthranoids, glycosides, and oils. This review therefore suggests the need for further robust and detailed investigations on the activity of the extracts and compounds of this plant and their potential toxicities.

Voacanga africana 是一种在许多非洲国家广泛使用的药用植物。这种植物的各个部分都被使用,但种子尤其受到推崇,因为它含有生物碱伊博格碱、塔巴索宁和瓦康碱,具有额外的经济价值。这些生物碱具有特殊的药用价值,可用于治疗精神疾病和毒瘾,还可作为药物合成的前体。传统上,非洲鹅膏草可用于治疗多种疾病,包括疟疾、蠕虫感染、阿米巴病、溃疡、疼痛、心血管疾病、抑郁、疲劳、气短、腹泻、妇科疾病、难产、肾脏疾病、疟疾、哮喘和抽搐,但并非所有这些疾病都得到了研究。研究表明,它对治疗蠕虫感染、阿米巴病、溃疡、疼痛和炎症、心血管疾病、抑郁症、腹泻、盘尾丝虫病、精神失常和微生物感染有一定疗效。该植物还具有中枢神经系统、神经保护、镇静、抗微生物、抗肿瘤和抗氧化活性。不过,还需要进一步的研究来验证它在治疗疟疾、疲劳、妇科疾病、劳动条件、呼吸道疾病和龋齿方面的活性。在安全性方面,据报道乙醇叶提取物相对无毒,估计半数致死剂量≥ 5000 毫克,而水叶提取物对小鼠模型的血液生化和重要器官的组织病理学没有明显改变。不过,从这种植物中分离出来的一些生物碱:沃布图辛、沃阿康辛和沃阿敏具有毒性,表现为心脏抑制活性、窒息和抽搐、高血压和中枢神经系统抑制活性。除生物碱外,该植物还富含皂甙、单宁、萜类、甾体、黄酮类、酚类、蒽类、苷类和油类。因此,本综述认为有必要对这种植物的提取物和化合物的活性及其潜在毒性进行进一步深入细致的研究。
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引用次数: 0
Anti-inflammatory effects of coumarins on a murine model of acute lung injury (ALI): a brief systematic review 香豆素对急性肺损伤(ALI)小鼠模型的抗炎作用:简要系统综述
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-30 DOI: 10.1007/s13596-023-00707-0
Gustavo Oliveira dos Reis, Ziliani da Silva Buss, Tainá Larissa Lubschinski, Eduarda Talita Bramorski Mohr, Mariano Felisberto, Thais Elisete Pilatti Ribeiro, Júlia Salvan da Rosa, Filipe Carvalho Matheus, Eduardo Monguilhott Dalmarco

Acute lung injury (ALI) is one of most critical inflammatory conditions. It is produced by different scenarios, which poses a challenge for its clinical management and treatment. Coumarins, a class of natural and synthetic compounds, identified as important candidates for new drugs due to their anti-inflammatory action, could be an alternative for the development of new medicines to manage ALI. In this article, we compile the results of a literature review to conclude whether coumarins are as effective as anti-inflammatory compounds when used in LPS-induced ALI in mice. The outcomes used as parameters to answer this question were: the ability to reduce the influx of inflammatory cells, and edema in inflamed lungs. A total of eight manuscripts were reviewed that unanimously addressed the anti-inflammatory efficacy of coumarin compounds in inhibiting the formation of edema and the influx of leukocytes into the lungs in LPS-induced ALI in mice. Most of the studies also highlighted the role of compounds in decreasing the production of pro-inflammatory cytokines, and these effects were associated with interference in the cell signaling pathways, which were investigated by some of the studies included in this review. The assessment of methodological quality showed that the studies evaluated in this review had moderate to high risk of bias, related to the lack of data on randomization of the animals, and the blinding of the investigators, compromising the reliability of the experimental results of the published works. Leading the results of the manuscripts is possible affirm that coumarins have important anti-inflammatory effects in LPS-induced ALI in mice, and the effect is comparable to the reference anti-inflammatory drug dexamethasone.

Graphical abstract

急性肺损伤(ALI)是最严重的炎症之一。急性肺损伤是最严重的炎症之一,可在不同情况下发生,这给临床管理和治疗带来了挑战。香豆素是一类天然和合成化合物,因其具有抗炎作用而被认为是新药的重要候选成分,可以作为开发治疗急性肺损伤新药的替代品。在本文中,我们对文献综述的结果进行了梳理,以得出结论:香豆素用于 LPS 诱导的小鼠 ALI 是否与抗炎化合物一样有效。回答这一问题的参数是:减少炎症细胞流入和炎症肺水肿的能力。共审查了 8 篇手稿,这些手稿一致论述了香豆素化合物在 LPS 诱导的小鼠 ALI 中抑制水肿形成和白细胞涌入肺部的抗炎功效。大多数研究还强调了香豆素化合物在减少促炎细胞因子产生方面的作用,这些作用与干扰细胞信号通路有关,本综述中的一些研究对此进行了调查。方法学质量评估显示,本综述所评估的研究存在中度至高度的偏倚风险,这与缺乏动物随机化数据和研究人员的盲法有关,从而影响了已发表作品实验结果的可靠性。根据这些手稿的结果,可以肯定香豆素对LPS诱导的小鼠ALI有重要的抗炎作用,其效果与抗炎参考药物地塞米松相当。
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引用次数: 0
Argania spinosa essential oil ameliorates colonic damage and extraintestinal alterations in a rat model of acetic acid-induced colitis by suppressing oxidative stress and inflammation 刺阿干树精油通过抑制氧化应激和炎症,改善醋酸诱导的大鼠结肠炎模型中的结肠损伤和肠外改变
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-27 DOI: 10.1007/s13596-023-00708-z
Folake Olayinka Olojo, Akinleye Stephen Akinrinde, Stella Ajedawun Ogundairo, Vincetia Chinwendu Ubochi

The present study was designed to elucidate the prophylactic and therapeutic potential of argan oil (AO) (from the kernels of the argan tree, Argania spinosa) against acetic acid (AA)-induced colitis and associated alterations in the liver and kidneys of rats. Colitis was induced by intra-rectal administration of 4% AA solution for 3 consecutive days. Some groups of rats were treated orally with AO (5 mL/kg) for 5 consecutive days before and after AA administration, while other groups were treated with either the vehicle or AO alone. Macroscopic and microscopic lesions in the tissues were assessed, while oxidative stress, antioxidant parameters and myeloperoxidase (MPO) activity were determined by biochemical methods. Haematological and serum chemistry parameters were also evaluated. Administration of AO before or after AA induction produced improvements in body weight gain, faecal consistency, macroscopic and histologic scores of the colonic mucosa compared to rats treated with AA alone. Furthermore, AO treatment caused significant reduction in colonic levels of hydrogen peroxide (H2O2), malondialdehyde (MDA), advanced oxidation protein products (AOPP) and serum MPO activity, while glutathione S-transferase (GST) and superoxide dismutase (SOD) activities were increased in the colon and kidneys, compared to the colitis control. Acetic acid treatment resulted in significant reduction in erythrocyte and leucocyte indices in relation to healthy controls. Taken together, treatment of rats with AO protected colonic tissues from acetic acid-induced inflammation and suggests that the oil may be considered for preventive and therapeutic purposes against inflammatory bowel diseases.

本研究旨在阐明摩洛哥坚果油(取自摩洛哥坚果树的果核)对醋酸(AA)诱导的大鼠结肠炎以及肝脏和肾脏相关变化的预防和治疗潜力。连续 3 天通过直肠内注射 4% AA 溶液诱发结肠炎。在给予 AA 之前和之后,一些大鼠组连续 5 天口服 AO(5 mL/kg),而另一些大鼠组则只用载体或 AO 治疗。对大鼠组织的宏观和微观病变进行了评估,并通过生化方法测定了氧化应激、抗氧化参数和髓过氧化物酶(MPO)活性。此外,还评估了血液学和血清化学参数。与单独使用 AA 的大鼠相比,在 AA 诱导之前或之后施用 AO 可改善大鼠的体重增加、粪便稠度、结肠粘膜的宏观和组织学评分。此外,与结肠炎对照组相比,AO 治疗可显著降低结肠中过氧化氢(H2O2)、丙二醛(MDA)、高级氧化蛋白产物(AOPP)的水平和血清 MPO 活性,同时提高结肠和肾脏中谷胱甘肽 S 转移酶(GST)和超氧化物歧化酶(SOD)的活性。与健康对照组相比,醋酸治疗导致红细胞和白细胞指数显著下降。综上所述,用 AO 治疗大鼠可保护结肠组织免受醋酸诱发的炎症影响,这表明该油可用于预防和治疗炎症性肠病。
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引用次数: 0
Anti-hyperuricemic potential of caryophyllene from Syzygium aromaticum essential oil: SiO2-AgNO3-based column chromatography purification, antioxidant, and xanthine oxidase inhibitory activities 芳香植物精油中的茶叶烯抗高尿酸血症的潜力:基于 SiO2-AgNO3 的柱层析纯化、抗氧化和黄嘌呤氧化酶抑制活性
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-27 DOI: 10.1007/s13596-023-00710-5
Arif Setiawansyah, Muh Ikhlas Arsul, Sukrasno Sukrasno, Sophi Damayanti, Muhamad Insanu, Irda Fidrianny

Xanthine oxidase is an enzyme that plays an essential role in the biosynthesis of uric acid. Inhibiting this enzyme can diminish the production of uric acid. Caryophyllene is a type 2 cannabinoid agonist receptor widely distributed in all plants' essential oil and provides plentiful biological activities. This research was carried out to isolate and evaluate the antioxidant and xanthine oxidase inhibitory activities of caryophyllene. Caryophyllene was isolated from Syzygium aromaticum essential oil using SiO2-AgNO3-based column chromatography. The xanthine oxidase inhibitory activity was assessed by molecular docking and in vitro assay using a spectrophotometer in 96-well plates below the aerobic conditions, while the antioxidant activity was tested to DPPH and measured as AAI. Our study revealed that the SiO2-AgNO3-based column chromatography technique provides caryophyllene with a purity of 98%. The biological evaluation showed that caryophyllene could inhibit the xanthine oxidase in silico and in vitro with an IC50 value of 4.79 ± 0.25 µg/mL. Caryophyllene also exhibits very strong antioxidant activity. In conclusion, caryophyllene shows a promising potential to be developed as a novel candidate for uric acid-lowering agents.

Graphical abstract

黄嘌呤氧化酶是一种在尿酸的生物合成过程中发挥重要作用的酶。抑制这种酶可以减少尿酸的产生。茶碱是一种 2 型大麻素激动剂受体,广泛分布于所有植物的精油中,具有丰富的生物活性。这项研究旨在分离和评估茶叶烯的抗氧化和黄嘌呤氧化酶抑制活性。采用基于 SiO2-AgNO3 的柱层析技术,从芳香植物精油中分离出了茶叶烯。黄嘌呤氧化酶抑制活性是通过分子对接和在有氧条件下使用分光光度计在 96 孔板中进行体外检测来评估的,而抗氧化活性则是通过 DPPH 测试并以 AAI 度量的。我们的研究表明,基于 SiO2-AgNO3 的柱层析技术可提供纯度为 98% 的石竹烯。生物评估表明,在硅学和体外实验中,茶碱能抑制黄嘌呤氧化酶,其 IC50 值为 4.79 ± 0.25 µg/mL。此外,茶碱还具有很强的抗氧化活性。总之,茶叶烯显示出作为新型降尿酸剂候选物的开发潜力。
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引用次数: 0
The ethanolic extract of Aframomum angustifolium seeds protects against tamoxifen-induced side effects in rats with breast cancer Aframomum angustifolium 种子乙醇提取物可防止他莫昔芬诱发的乳腺癌大鼠副作用
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-14 DOI: 10.1007/s13596-023-00705-2
Inelle Makamwe, Françoise Raïssa Ntentie, Mary-Ann Angie Mbong, Anne Pascale Nouemsi Kengne, Huiny Miriane Fotso Tienoue, Guy Roussel Nguemto Takuissu, Ulrich Aimée Ngankam Onsi, Stéphane Zingue, Julius Enyong Oben

Long-term use of tamoxifen (TAM) is associated with severe side effects. The present study aimed at evaluating the protective effect of the ethanolic extract of Aframomum angustifolium seeds (EEAA) against some adverse effects of TAM in female Wistar rats with 7,12-dimethybenz-(a)-anthracene (DMBA)-induced breast cancer. Breast cancer was induced through the subcutaneous administration of 50 mg/kg, bw of DMBA while normal rats constituted the control group. Twelve weeks later, breast cancer rats were randomised 5 per group and treated or not with 3.3 mg/kg, bw of tamoxifen alone, or tamoxifen plus either 150 or 300 mg/kg, bw of EEAA during 28 days, after which all animals were sacrificed under anaesthesia. The effects of the treatment on the uterus, body weight, lipid profile, liver and kidneys were evaluated. The EEAA at 300 mg/kg, bw significantly prevented tamoxifen-induced uterus’s hyperplasia by reducing serum estradiol level from 896.85 ± 54.57 (tamox alone) to 639.81 ± 43.41 pg/L. The extract at both doses prevented metabolic disturbance by increasing body weight, lowering triglyceride and total cholesterol levels and also prevented lipids accumulation in the liver. Catalase activity and TBARS levels were ameliorated (p < 0.05) in the liver and kidneys leading to the improvement of the integrity of these organs. Also, an amelioration of plasmatic activities of transaminases alkaline phosphatase and uric acid levels was noted. The ethanolic extract of Aframomum angustifolium seeds can be considered a potential source of bioactive compounds for the management of the side effects of TAM among breast cancer patients.

长期服用他莫昔芬(TAM)会产生严重的副作用。本研究旨在评估阿福木种子乙醇提取物(EEAA)对7,12-二甲基苯并(a)-蒽(DMBA)诱导的雌性Wistar大鼠乳腺癌的保护作用。对照组为正常大鼠,通过皮下注射 50 毫克/千克体重的 DMBA 诱发乳腺癌。12 周后,乳腺癌大鼠被随机分为每组 5 只,分别接受或不接受 3.3 毫克/千克(体重)他莫昔芬单独治疗,或他莫昔芬加 150 或 300 毫克/千克(体重)EEAA 治疗 28 天。评估了治疗对子宫、体重、血脂、肝脏和肾脏的影响。300 毫克/千克体重的雌二醇提取物能显著防止他莫昔芬诱导的子宫增生,使血清雌二醇水平从 896.85 ± 54.57(单独他莫昔芬)降至 639.81 ± 43.41 pg/L。两种剂量的提取物都能通过增加体重、降低甘油三酯和总胆固醇水平来防止代谢紊乱,还能防止肝脏中的脂质积累。肝脏和肾脏的过氧化氢酶活性和 TBARS 水平均有所改善(p < 0.05),从而改善了这些器官的完整性。此外,转氨酶碱性磷酸酶和尿酸水平的浆液活性也有所改善。可以认为,Aframomum angustifolium 种子的乙醇提取物是一种潜在的生物活性化合物来源,可用于控制乳腺癌患者服用 TAM 后产生的副作用。
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引用次数: 0
Long-term oral administration of curcumin is effective in preventing short-term memory deterioration and prolonging lifespan in a mouse model of Alzheimer’s disease 长期口服姜黄素能有效预防阿尔茨海默病小鼠模型的短期记忆衰退并延长寿命
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2023-09-09 DOI: 10.1007/s13596-023-00706-1
Hiroko Maruyama, Takahito Ooizumi, Fumitaka Kawakami, Thet-Thet Lwin, Hisanao Akita, Takuya Kunii, Ryota Shirai, Tohoru Takeda

Curcumin (Curc) has been shown to have the potential to ameliorate or prevent the development of Alzheimer's disease (AD). However, most of them are in vitro and in vivo short-term studies. This study was conducted to investigate whether long-term, low-dose dietary Curc intake in mouse of AD might suppress short-term memory retention, amyloid-beta (Aβ) deposition and tau phosphorylation, delaying the onset of AD and prolonging the lifespan of the animals. Short-term memory was examined by the Y-maze method after 6 months old. Immunohistochemical analysis was performed at 10 months old to determine changes in Aβ deposition, tau phosphorylation, and glial cell number in brain tissue. Furthermore, we investigated the survival rate for 12 months old and evaluated the AD prevention effect. The alternation rates of short-time memory in the wild type and AD mice were 56.2% and 25.9%, respectively. These rates in the experimental groups (0.02% and 0.5% Curc) were in the range of 44.4–45.7%. The area of Aβ42 deposition in AD mice was approximately 25,000 µm2, while the experimental groups had a significantly reduced area of 5000–10,000 µm2. Survival rate was 34% in the AD control group, 100% in the 0.02% Curc, and 83% in the 0.5% Curc group, significantly longer in the Curc groups than the AD control group. This study demonstrates that long-term intake of low concentrations of Curc may act on the tau- phosphorylation, suppress brain inflammation, delay the onset of AD, and prolong the lifespan of the mouse.

姜黄素(Curc)已被证明具有改善或预防阿尔茨海默病(AD)发展的潜力。然而,这些研究大多是体外和体内的短期研究。本研究旨在探讨长期低剂量膳食姜黄是否能抑制AD小鼠的短期记忆保持、淀粉样β(Aβ)沉积和tau磷酸化,从而延缓AD的发病并延长动物的寿命。6个月后,用Y迷宫法检测动物的短期记忆。在动物10个月大时进行免疫组化分析,以确定脑组织中Aβ沉积、tau磷酸化和胶质细胞数量的变化。此外,我们还调查了12个月大时的存活率,并评估了AD预防效果。野生型小鼠和AD小鼠的短时记忆交替率分别为56.2%和25.9%。实验组(0.02% 和 0.5% Curc)的短时记忆交替率在 44.4%-45.7% 之间。AD小鼠的Aβ42沉积面积约为25,000 µm2,而实验组的Aβ42沉积面积显著减少,仅为5000-10,000 µm2。AD对照组的存活率为34%,0.02% Curc组为100%,0.5% Curc组为83%,Curc组的存活时间明显长于AD对照组。这项研究表明,长期摄入低浓度的Curc可抑制tau-磷酸化,抑制脑部炎症,延缓AD的发病,延长小鼠的寿命。
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引用次数: 0
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Advances in Traditional Medicine
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