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In-vitro and in-silico analysis of phytoconstituents of Enhydra fluctuans as an antidiabetic agent 水仙花抗糖尿病药植物成分的体外和计算机分析
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-03-14 DOI: 10.1007/s13596-025-00821-1
Shahnaz Alom, Farak Ali, Rajashri Bezbaruah, Bibhuti Bhusan Kakoti

Medicinal plants or herbs act as reservoirs of therapeutic agents and become source of traditional or conventional treatment of various health issues. Enhydra fluctuans Lour. is one such plant belongs to Asteraceae family, mostly using traditionally as vegetable or its decoction to treat hyperglycaemia, although scientific exploration for this claim is very limited. In this study, we evaluated the hypoglycaemic activity of E. fluctuans Lour. along with their phytochemical screening, in-silico study and anti-oxidant activity. Phytoconstituents belongs to alkaloids, flavonoids, terpenoids, phenolic compounds, carbohydrates, etc. were found in preliminary phytochemical investigations. In-silico study has been performed on its phytoconstituents and it has been found that two compound C5 (8-Desacyl enhydrin- [4- hydroxytiglate]) and C8 (Baicalein 7-O-glucoside) bind with all three proteins i.e. 7K9N, 3BC9 and 5ISO with binding energy of − 188.31, − 243.57; − 169.90, − 202.13 and − 296.05, − 271.38 kcal/mol respectively as compared to standard acarbose voglibose and metformin − 152.993, 142.19 and − 215.55 kcal/mol respectively. In-vitro antidiabetic study was performed for methanolic extract against α-glucosidase and α-amylase inhibition, where IC50 value was found to be 123.79 ± 3.522 and 155.52 ± 5.890 µg/ml as compared to standard acarbose 206. 75 ± 5.082 and 120.38 ± 3.687 µg/ml respectively. Both the antioxidant and enzymatic inhibition study revealed that methanolic extract of Enhydra fluctuans have potential to reduce DPPH and hydroxyl free radical. It has also been observed that methanolic extract exhibit better α-glucosidase inhibition as compared to acarbose but lesser inhibition against α-amylase which indicate that methanolic extract might have good antidiabetic potential. Moreover, in silico study revealed that, both the compound C5 and C8 might be responsible for enzymatic inhibition. Overall findings demonstrate that E. fluctuans Lour. have significant antioxidant and antidiabetic activity.

药用植物或草药作为治疗剂的储藏库,成为各种健康问题的传统或常规治疗的来源。Enhydra是波动的。是一种菊科植物,传统上主要用作蔬菜或其煎剂来治疗高血糖,尽管对这一说法的科学探索非常有限。在这项研究中,我们评估了波动E. Lour的降糖活性。随着他们的植物化学筛选,硅研究和抗氧化活性。植物化学初步研究发现植物成分包括生物碱、类黄酮、萜类、酚类化合物、碳水化合物等。对其植物成分进行了硅晶化研究,发现两种化合物C5(8-去acyl enhydrin- [4- hydroxytiglate])和C8(黄芩苷7-O-glucoside)与7K9N、3BC9和5ISO三种蛋白结合,结合能分别为- 188.31、- 243.57;分别为- 169.90,- 202.13和- 296.05,- 271.38 kcal/mol,而标准阿卡糖伏糖和二甲双胍分别为- 152.993,142.19和- 215.55 kcal/mol。体外研究甲醇提取物对α-葡萄糖苷酶和α-淀粉酶的抑制作用,与标准阿卡波糖206相比,IC50值分别为123.79±3.522和155.52±5.890µg/ml。分别为75±5.082和120.38±3.687µg/ml。抗氧化和酶促抑制实验表明,水仙醇提物具有降低DPPH和羟基自由基的作用。甲醇提取物对α-葡萄糖苷酶的抑制作用优于阿卡波糖,但对α-淀粉酶的抑制作用较弱,表明甲醇提取物可能具有良好的抗糖尿病潜力。此外,在计算机上的研究表明,化合物C5和C8可能都有抑制酶的作用。总体研究结果表明,E.波动Lour。具有显著的抗氧化和抗糖尿病活性。
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引用次数: 0
Samul-tang promotes in vitro follicle development by regulating inflammation in healthy, non-diseased young mice Samul-tang通过调节健康、未患病的年轻小鼠的炎症来促进体外卵泡发育
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-03-12 DOI: 10.1007/s13596-025-00825-x
Inyoung Kang, Myoungjoo Koo, Wonmo Lee, Sooseong You, Jin Hyun Jun, Jaewang Lee

Samul-tang (SMT) is a well-known traditional herbal medicine. Recent studies have reported that SMT exhibits protective biological effects against inflammation, oxidative stress, and cancer. It is commonly used to treat gynecological disorders, including irregular menstruation, pre-eclampsia, and postmenopausal syndrome. However, its therapeutic mechanisms are still under investigation, and its effects on gynecologically healthy women remain unknown. This study was conducted to investigate whether and how SMT influences ovarian follicle development by culturing early follicles in vitro and stimulating the ovulation process. SMT dissolved in DPBS was applied at concentrations of 0.1, 1 and 10 µg/mL in in vitro maturation medium. Secondary follicles isolated from ovaries of fourteen-day-old female ICR mice were cultured for 8 days in the in vitro maturation medium supplemented with follicle-stimulating hormone. Ovulation was induced in follicles that reached a diameter of 380–450 μm. Ovulated oocytes were retrieved, and their spindles and chromosomes were stained to observe meiotic maturation. SMT had no effect on follicle diameter, hormone levels, or survival rates during ovarian follicle development. However, ovulation and the production of mature oocytes were enhanced when SMT was applied during in vitro culture. Additionally, the expression of genes related to progesterone production (lhcgr and hsd3b) was elevated, while the ptgs2 gene, which regulates inflammation, was decreased in the SMT-treated group. This study demonstrated that SMT may influence ovarian follicle development by regulating progesterone production and the inflammatory response. Consequently, SMT administration may have the potential to enhance reproductive function, even in non-diseased, fertile women.

Samul-tang (SMT)是一种著名的传统草药。最近的研究表明,SMT对炎症、氧化应激和癌症具有保护作用。它通常用于治疗妇科疾病,包括月经不调、先兆子痫和绝经后综合征。然而,其治疗机制仍在调查中,其对妇科健康妇女的影响仍不清楚。本研究通过体外培养早期卵泡和刺激排卵过程,探讨SMT是否以及如何影响卵巢卵泡发育。将溶解在DPBS中的SMT分别以0.1、1和10µg/mL的浓度作用于体外成熟培养基中。从14日龄雌性ICR小鼠卵巢中分离出二次卵泡,在添加促卵泡激素的体外成熟培养基中培养8天。卵泡直径为380 ~ 450 μm,可诱导排卵。取出排卵的卵母细胞,染色其纺锤体和染色体,观察减数分裂成熟。在卵泡发育过程中,SMT对卵泡直径、激素水平或存活率没有影响。然而,SMT在体外培养过程中可以促进排卵和成熟卵母细胞的产生。此外,与孕酮产生相关的基因(lhcgr和hsd3b)表达升高,而调节炎症的ptgs2基因在smt治疗组中表达降低。本研究表明SMT可能通过调节黄体酮的产生和炎症反应来影响卵泡发育。因此,SMT的施用可能有增强生殖功能的潜力,甚至在没有患病的,有生育能力的妇女。
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引用次数: 0
Hwangkeumjakyak-tang protects against hepatocyte damage via oxidative stress inhibition and affects the altered gut microbiome pattern in acetaminophen-induced liver injury 黄芩汤通过抑制氧化应激来保护肝细胞损伤,并影响对乙酰氨基酚诱导的肝损伤中肠道微生物群模式的改变
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-03-11 DOI: 10.1007/s13596-025-00822-0
Sam Seok Cho, So Hi Kang, Jeon Kyung Kim, Yu Bin Lee, Hong Seok Son, Jae Min Kim, Chang Su Na, Ji Hye Yang

Hwangkeumjakyak-tang (HJT), a Korean traditional herbal medicine, is known to clear phlegm, relieve congestion, and reduce inflammation. However, there is a lack of research on the efficacy of HJT in other diseases. The present study aimed to investigate whether HJT could protect against liver injury. We first examined the effects of HIT in vitro by assessing its toxicity and the phosphorylation and nuclear translocation of nuclear factor erythroid 2-related factor 2 (Nrf2) in human HepG2 cells. Additionally, we investigated whether HJT inhibited oxidative stress by measuring reactive oxygen species (ROS) production and intracellular levels of reduced glutathione (GSH). We further assessed the effects of HJT in vivo by analyzing liver damage parameters using an acetaminophen (APAP)-induced liver damage mouse model. Treatment with HJT significantly reduced the elevated serum levels of ALT and AST and the cytokine release induced by APAP injection. Furthermore, we verified that treatment with HJT suppressed APAP-induced ROS production and GSH depletion in the mouse liver, suggesting that HJT inhibited APAP-induced liver injury by blocking oxidative stress in vivo. To identify the potential relationship between the liver and intestine for liver disease therapy, we also performed 16S rRNA amplicon sequencing to analyze the gut microbiome and confirmed that HJT regulated APAP-induced changes in the gut microbiome pattern. In conclusion, HJT, a Nrf2 activation inducer, exhibits a cytoprotective effect on APAP-induced liver injury and can regulate the gut microbiome altered by the administration of APAP.

黄芩泻汤具有清痰、消肿、消炎的功效。然而,HJT在其他疾病中的疗效研究尚缺乏。本研究旨在探讨HJT是否对肝损伤有保护作用。我们首先通过评估HIT的体外毒性和核因子红细胞2相关因子2 (Nrf2)在人HepG2细胞中的磷酸化和核易位来研究HIT的作用。此外,我们通过测量活性氧(ROS)的产生和细胞内还原性谷胱甘肽(GSH)的水平来研究HJT是否抑制氧化应激。我们使用对乙酰氨基酚(APAP)诱导的肝损伤小鼠模型,通过分析肝损伤参数进一步评估HJT在体内的作用。HJT治疗显著降低了APAP注射引起的血清ALT和AST水平升高及细胞因子释放。此外,我们验证了HJT抑制了apap诱导的小鼠肝脏中ROS的产生和GSH的消耗,这表明HJT在体内通过阻断氧化应激来抑制apap诱导的肝损伤。为了确定肝脏和肠道在肝病治疗中的潜在关系,我们还进行了16S rRNA扩增子测序来分析肠道微生物组,并证实HJT调节了apap诱导的肠道微生物组模式的变化。综上所述,Nrf2激活诱导剂HJT对APAP诱导的肝损伤具有细胞保护作用,并可调节APAP引起的肠道微生物组改变。
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引用次数: 0
Enhanced pain threshold with the addition of neiguan and Hegu to cervical Jiaji electroacupuncture: a pre-post study 颈椎夹脊电针加内关、合谷增强痛阈的前后研究
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-03-08 DOI: 10.1007/s13596-025-00823-z
Oanh Thi Kim Ngo, Thanh Tran Van Nguyen, Nguyen Lam Vuong, Dieu-Thuong Thi Trinh

The analgesic effects of 100-Hz electroacupuncture (EA) are well-documented. Jiaji C1-C4 (Ex-B2 C1-C4) have been shown to increase pressure pain threshold (PPT) across V1, V2, V3, C2-C7 dermatomes, corresponding to the cranial, facial, cervical, and upper limb regions. Hegu (LI4) and Neiguan (PC6) are located on dermatomes influenced by Ex-B2 C1-C4. This study investigates the effects of 100-Hz EA at the combination of PC6, LI4, Ex-B2 C1-C4 versus Ex-B2 C1-C4 alone. A total of 120 healthy volunteers were assigned to receive either right-sided (RE) or bilateral electroacupuncture (BE). Both groups underwent 100-Hz EA at Ex-B2 C1-C4 in stage 1 and the combination of PC6, LI4, Ex-B2 C1-C4 in stage 2, with a 7-day interval between interventions. The main outcome was the post-intervention PPT at each stage, measured at 18 locations across V1, V2, V3, C2-C7 dermatomes. After stage 1, RE group showed significant PPT increases at the right V3, C2-C7, and left V2, C3, C4, C7 dermatomes, while BE group improved across all dermatomes. Following stage 2, RE group had significant PPT increases at the right V1, V2, V3, C2, C3, C6, C7 dermatomes compared to stage 1 but not on the left, whereas BE group showed improvements across all dermatomes. No significant PPT differences were found between the groups. EA at 100-Hz on PC6, LI4, Ex-B2 C1-C4 effectively increases PPT, with BE producing more widespread effects than RE. This supports its clinical for managing pain in the cranial, facial, cervical, and upper limb regions.

100赫兹电针(EA)的镇痛作用是有据可查的。jia - ji C1-C4 (Ex-B2 C1-C4)可增加V1、V2、V3、C2-C7皮节的压痛阈值(PPT),对应于颅、面、颈和上肢区域。河谷(LI4)和内关(PC6)位于Ex-B2 C1-C4影响的皮节上。本研究考察了100 hz EA对PC6、LI4、Ex-B2 C1-C4与单独Ex-B2 C1-C4联合作用的影响。共有120名健康志愿者被分配接受右侧(RE)或双侧电针(BE)。两组均在第一阶段进行100 hz Ex-B2 C1-C4 EA,在第二阶段联合PC6、LI4、Ex-B2 C1-C4,干预间隔7天。主要结果是干预后每个阶段的PPT,在V1, V2, V3, C2-C7皮节的18个位置测量。1期后,RE组右侧V3、C2-C7及左侧V2、C3、C4、C7皮节PPT明显升高,BE组所有皮节PPT均改善。2期后,与1期相比,RE组右侧V1、V2、V3、C2、C3、C6、C7皮节PPT明显增加,但左侧没有,而BE组所有皮节PPT均有改善。两组间PPT无明显差异。100 hz EA对PC6、LI4、Ex-B2 C1-C4有效增加PPT, BE比RE产生更广泛的效果。这支持其临床治疗颅、面部、颈部和上肢区域的疼痛。
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引用次数: 0
An assessment of the phytochemical constituents, antimicrobial and antioxidant activities of Juniperus macropoda Boiss 大足杜松的植物化学成分及其抗菌和抗氧化活性的研究
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-02-28 DOI: 10.1007/s13596-025-00820-2
Jagriti Rana, Anand Sagar, Jyoti Rana, Pooja Bharti
<div><p><i>Juniperus macropoda</i> Boiss. (Himalayan Pencil Cedar) is utilized as an incense, sacred and medicinal plant by inhabitants of the Lahaul-Spiti district, found in the cold desert areas of the western Himalayan region. The medicinal plants contain diverse varieties of bioactive compounds that may combat the increased threat of antimicrobial resistance and oxidative stress. In the presented study, the phytochemical constituents as well as the antimicrobial and antioxidant activities of the selected plant part have been screened. After extracting plant material (twigs with appressed leaves) in acetone and methanol solvents, the phytocomponents were initially studied by preliminary tests and later by estimating total phenol content, total flavonoid content and total tannin content. The gas chromatography-mass spectrometry (GCMS) analysis of both extracts and the liquid chromatography mass spectrometry (LC/MS) of methanol solvent extract were also conducted. The dried extracts of the plant material dissolved in dimethyl sulfoxide were screened for their antimicrobial activity by adopting disk diffusion and broth microdilution assays against four bacteria and one fungus. Further, the antioxidant potential of both extracts was screened by following 1,1-Diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging and reducing power assays. In the results, preliminary tests for phytocomponents revealed the presence of alkaloids, flavonoids, tannins and terpenoids. A little higher contents of phenol, flavonoid and tannin were recorded in acetone extract than methanol. Also, GCMS revealed a higher percentage of Abietol, Abietal < 4-epi > and 1 H-3a,7-Methanoazulen-6-ol, octahydro-3,6,8,8-tetramethyl-,[3R-(3.α.,3a.β.,6.α.,7.β.,8a.α.)] in both extracts. The presence of phenolics and flavonoids was also supported by LC/MS. Furthermore, for the disk diffusion method, both extracts of the selected plant displayed the highest zones of inhibition (ZOI) against <i>Bacillus cereus</i>, while both extracts displayed the least activity against <i>Escherichia coli</i>. However, in the results of the broth microdilution method, the highest antimicrobial activity, with the least minimum inhibitory concentrations (MIC), was recorded against <i>Pseudomonas putida</i>, and again, the highest MIC values were documented against <i>Escherichia coli</i>. Thus, the <i>E. coli</i> was found to be least sensitive to both extracts. For DPPH free radical inhibition, acetone extract displayed an IC<sub>50</sub> (half inhibitory concentration) value of 434.10 µg/mL and methanol extract displayed 390.83 µg/mL, while for the reducing power method, acetone extract displayed an effective concentration (EC) value of 1245.00 µg/mL and methanol displayed 1260.75 µg/mL for reduction of iron. Overall, plant extract displayed some extent of antimicrobial activity against <i>B. cereus</i> and <i>P. putida.</i> However, it remained inactive against <i>E. coli</i>. Also, plant unveil
大足杜松。(喜马拉雅铅笔雪松)被拉哈尔-斯皮提地区的居民用作熏香,神圣和药用植物,发现于喜马拉雅西部地区的寒冷沙漠地区。药用植物含有多种生物活性化合物,可以对抗抗菌素耐药性和氧化应激增加的威胁。在本研究中,对所选植物部位的植物化学成分以及抗菌和抗氧化活性进行了筛选。在丙酮和甲醇溶剂中提取植物材料(贴附叶片的嫩枝),通过初步试验和测定总酚含量、总黄酮含量和总单宁含量对植物成分进行初步研究。对两种提取物进行气相色谱-质谱(GCMS)分析和甲醇溶剂提取物的液相色谱-质谱(LC/MS)分析。采用圆盘扩散法和肉汤微量稀释法对四种细菌和一种真菌的抑菌活性进行了筛选。此外,通过1,1-二苯基-2-苦味酰肼(DPPH)自由基清除和还原能力测定,筛选了两种提取物的抗氧化潜力。结果显示,对植物成分的初步测试显示存在生物碱,类黄酮,单宁和萜类化合物。丙酮提取物中苯酚、类黄酮和单宁的含量略高于甲醇。此外,GCMS还显示,两种提取物中Abietol、Abietal <; 4-epi >;和1 H-3a,7-甲氧唑烯-6-醇、八氢-3,6,8,8-四甲基- [3R-(3.α.,3 . a.β.,6.α.,7.β.,8 . a.α.)]的含量均较高。液相色谱/质谱分析也证实了酚类物质和类黄酮的存在。此外,对于圆盘扩散法,所选植物的两种提取物对蜡样芽孢杆菌的抑制区(ZOI)最高,而对大肠杆菌的抑制区(ZOI)最低。然而,在肉汤微量稀释法的结果中,对恶臭假单胞菌的抑菌活性最高,最低抑菌浓度(MIC)最低,对大肠杆菌的MIC值最高。因此,发现大肠杆菌对这两种提取物最不敏感。对于DPPH自由基的抑制,丙酮提取物的IC50值为434.10µg/mL,甲醇提取物的IC50值为390.83µg/mL;对于还原力法,丙酮提取物的EC值为1245.00µg/mL,甲醇提取物的EC值为1260.75µg/mL。结果表明,植物提取物对蜡样芽孢杆菌和恶臭杆菌均有一定的抑菌活性。然而,它对大肠杆菌没有活性。此外,植物揭示了抗氧化潜力,这可能归因于两种提取物中记录的植物成分。
{"title":"An assessment of the phytochemical constituents, antimicrobial and antioxidant activities of Juniperus macropoda Boiss","authors":"Jagriti Rana,&nbsp;Anand Sagar,&nbsp;Jyoti Rana,&nbsp;Pooja Bharti","doi":"10.1007/s13596-025-00820-2","DOIUrl":"10.1007/s13596-025-00820-2","url":null,"abstract":"&lt;div&gt;&lt;p&gt;&lt;i&gt;Juniperus macropoda&lt;/i&gt; Boiss. (Himalayan Pencil Cedar) is utilized as an incense, sacred and medicinal plant by inhabitants of the Lahaul-Spiti district, found in the cold desert areas of the western Himalayan region. The medicinal plants contain diverse varieties of bioactive compounds that may combat the increased threat of antimicrobial resistance and oxidative stress. In the presented study, the phytochemical constituents as well as the antimicrobial and antioxidant activities of the selected plant part have been screened. After extracting plant material (twigs with appressed leaves) in acetone and methanol solvents, the phytocomponents were initially studied by preliminary tests and later by estimating total phenol content, total flavonoid content and total tannin content. The gas chromatography-mass spectrometry (GCMS) analysis of both extracts and the liquid chromatography mass spectrometry (LC/MS) of methanol solvent extract were also conducted. The dried extracts of the plant material dissolved in dimethyl sulfoxide were screened for their antimicrobial activity by adopting disk diffusion and broth microdilution assays against four bacteria and one fungus. Further, the antioxidant potential of both extracts was screened by following 1,1-Diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging and reducing power assays. In the results, preliminary tests for phytocomponents revealed the presence of alkaloids, flavonoids, tannins and terpenoids. A little higher contents of phenol, flavonoid and tannin were recorded in acetone extract than methanol. Also, GCMS revealed a higher percentage of Abietol, Abietal &lt; 4-epi &gt; and 1 H-3a,7-Methanoazulen-6-ol, octahydro-3,6,8,8-tetramethyl-,[3R-(3.α.,3a.β.,6.α.,7.β.,8a.α.)] in both extracts. The presence of phenolics and flavonoids was also supported by LC/MS. Furthermore, for the disk diffusion method, both extracts of the selected plant displayed the highest zones of inhibition (ZOI) against &lt;i&gt;Bacillus cereus&lt;/i&gt;, while both extracts displayed the least activity against &lt;i&gt;Escherichia coli&lt;/i&gt;. However, in the results of the broth microdilution method, the highest antimicrobial activity, with the least minimum inhibitory concentrations (MIC), was recorded against &lt;i&gt;Pseudomonas putida&lt;/i&gt;, and again, the highest MIC values were documented against &lt;i&gt;Escherichia coli&lt;/i&gt;. Thus, the &lt;i&gt;E. coli&lt;/i&gt; was found to be least sensitive to both extracts. For DPPH free radical inhibition, acetone extract displayed an IC&lt;sub&gt;50&lt;/sub&gt; (half inhibitory concentration) value of 434.10 µg/mL and methanol extract displayed 390.83 µg/mL, while for the reducing power method, acetone extract displayed an effective concentration (EC) value of 1245.00 µg/mL and methanol displayed 1260.75 µg/mL for reduction of iron. Overall, plant extract displayed some extent of antimicrobial activity against &lt;i&gt;B. cereus&lt;/i&gt; and &lt;i&gt;P. putida.&lt;/i&gt; However, it remained inactive against &lt;i&gt;E. coli&lt;/i&gt;. Also, plant unveil","PeriodicalId":7613,"journal":{"name":"Advances in Traditional Medicine","volume":"25 4","pages":"891 - 902"},"PeriodicalIF":1.3,"publicationDate":"2025-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145449704","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Investigating the antiproliferative properties of Amaryllidaceae plant species and their bioactive compounds on brain tumour cell lines 探讨amarylliaceae植物种类及其活性化合物对脑肿瘤细胞系的抗增殖作用
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-02-27 DOI: 10.1007/s13596-025-00818-w
Sylvester I. Omoruyi, Tanya N. Augustine, Lawrence Mabasa, Ahmed A. Hussein, Vuyo Mavumengwana

Glioblastoma multiforme is considered the most aggressive type of brain tumour due to its highly invasive properties that make complete surgical resection almost impossible and treatment very challenging. The current treatment for glioblastoma involves surgery followed by radiotherapy and chemotherapy. Despite these treatment options, tumour recurrence and toxicity from the chemotherapeutic agents remain problematic, which calls for novel treatment approaches. In this study, we investigate the antiproliferative activities of three Amaryllidaceae plant species, Crossyne flava, Amaryllis belladonna, and Boophone haemanthiodes, as well as their isolated bioactive compounds on U87 and U251 glioblastoma cell lines, with H9C2 cardiac myocyte used as a normal cell line. The effect of plant extracts and compounds on cell viability and long-term survival was determined using the MTT [3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide] and clonogenic assay, respectively. Additionally, the ATP levels and apoptosis-inducing potential of the plant extracts and compounds were determined using the Promega Mitochondrial ToxGlo™ and Caspase-Glo™ 3/7 assay kits, respectively. The results reveal that both plant extracts and compounds induce cytotoxicity in glioblastoma cell lines, and the extracts also inhibit the long-term survival of U87 and U251 cells. The extracts were also selective to the cancer cells when the selectivity index was calculated. Furthermore, the plant extracts and compounds inhibited ATP production in the cancer cells, while induction of apoptosis was only evident in the compound-treated cells. Overall, our findings suggest that the Amaryllidaceae plant family could be a rich source of botanicals and phytochemicals that might be effective against glioblastoma.

多形性胶质母细胞瘤被认为是最具侵袭性的脑肿瘤类型,因为它的高度侵袭性使得完全手术切除几乎是不可能的,治疗非常具有挑战性。目前对胶质母细胞瘤的治疗包括手术加放疗和化疗。尽管有这些治疗方案,但肿瘤复发和化疗药物的毒性仍然存在问题,这需要新的治疗方法。本研究以H9C2心肌细胞为正常细胞系,研究了三种amarylidaceae植物Crossyne flava、Amaryllis belladonna和Boophone haemanthiodes及其分离得到的活性物质对U87和U251胶质母细胞瘤细胞的抑制作用。采用MTT[3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四唑]和克隆实验分别测定植物提取物和化合物对细胞活力和长期存活的影响。此外,分别使用Promega线粒体ToxGlo™和Caspase-Glo™3/7检测试剂盒检测植物提取物和化合物的ATP水平和诱导细胞凋亡的潜力。结果表明,植物提取物和化合物均能诱导胶质母细胞瘤细胞系的细胞毒性,并且提取物还能抑制U87和U251细胞的长期存活。在计算选择性指数时,提取物对癌细胞也具有选择性。此外,植物提取物和化合物抑制了癌细胞中ATP的产生,而诱导凋亡仅在化合物处理的细胞中明显。总之,我们的研究结果表明,Amaryllidaceae植物家族可能是一个丰富的植物药物和植物化学物质的来源,可能对胶质母细胞瘤有效。
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引用次数: 0
Exploring the cognitive benefits of Eleusine Indica (L.) Gaertn in alleviating scopolamine-induced dementia in wistar rats 探索莲属植物的认知益处葛尔坦减轻东莨菪碱所致wistar大鼠痴呆的作用
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-02-20 DOI: 10.1007/s13596-025-00819-9
Neelakanth M. Jeedi, Reenal R. Naik, Shrishail K. Nimbal, Santosh B. Patil

The loss of cognitive abilities, such as reasoning, memory, and thinking, is known as dementia. The therapeutic value of medicinal plants often arises from their antioxidants. Eleusine indica’s antioxidant activity in the extract is attributed to its phenolic components and abundant secondary metabolites. This study aims to discover the influence of Eleusine indica extract at 100 and 200 mg/kg on cognitive enhancement in scopolamine induced memory impairment in Wistar rats. Hydroethanolic extract of Eleusine indica was made using cold maceration followed by Soxhlet instrument, and phytochemical tests were analyzed. Dementia was induced by administration of scopolamine at the dose of 3 mg/kg. The efficacy of the extract 100 and 200 mg/kg, p.o and the standard drug piracetam 400 mg/ kg p.o. in enhancing information recall in animals was assessed through a range of experimental models, including the elevated plus maze, Morris Water Maze, and light-dark model. Biomarkers such as acetylcholinesterase and dopamine in the brain were measured along with various oxidative stress markers. Histopathology of the brain cortex and hippocampus were studied. Treatment with Eleusine indica extract at 200 mg/kg significantly reversed the pathogenesis induced by scopolamine, leading to an increase in acetylcholinesterase and dopamine levels. It is evident that decreases in transfer latency in elevated plus maze and Step through latency in Morris Water Maze. Eleusine indica extract showed strong antioxidant potency. Phytoconstituents in extract possesses free radical scavenging ability and protecting the brain structure and functions.

认知能力的丧失,如推理、记忆和思考,被称为痴呆症。药用植物的治疗价值往往来自其抗氧化剂。芦荟提取物的抗氧化活性主要来源于其酚类成分和丰富的次生代谢物。本研究旨在探讨100和200 mg/kg香莲提取物对东莨菪碱致Wistar大鼠记忆障碍认知增强的影响。采用冷浸法和索氏仪提取香莲水乙醇提取物,并进行植物化学试验。给药剂量为3 mg/kg的东莨菪碱诱导痴呆。通过抬高+迷宫、Morris水迷宫、光暗模型等实验模型,考察了提取物100、200 mg/kg p.o和标准药物吡拉西坦400 mg/kg p.o.对动物信息回忆的增强作用。大脑中的生物标志物如乙酰胆碱酯酶和多巴胺与各种氧化应激标志物一起被测量。观察大鼠大脑皮层和海马的组织病理学变化。200 mg/kg的印度莲提取物可显著逆转东莨菪碱诱导的发病机制,导致乙酰胆碱酯酶和多巴胺水平升高。在Morris水迷宫中,跳台迷宫和阶梯迷宫的传递潜伏期均明显降低。鸢尾提取物具有较强的抗氧化能力。提取物中的植物成分具有清除自由基和保护大脑结构和功能的作用。
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引用次数: 0
Chemical composition and biological activity of ethanolic leaf extract from Tillandsia usneoides in a murine model of acute myeloid leukemia 莲叶乙醇提取物对急性髓性白血病小鼠模型的化学成分及生物活性研究
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-31 DOI: 10.1007/s13596-024-00807-5
Laura Rojas, Paola Lasso, Natalia Murillo, Geison M. Costa, Susana Fiorentino

Medicinal plants constitute a valuable reservoir for discovering novel therapeutic compounds that target leukemia and various other forms of cancer. Plants of the genus Tillandsia, such as T. recurvata, have different ethnobotanical uses, including the treatment of hemorrhoids, gastritis, arthritis, ulcers, sore throats, cancer, and diabetes. Specifically, T. usneoides has been used by the indigenous Zenúes in the Urabá region for diabetes management. However, few studies have been published on T. usneoides. The aim of this work was to determine the chemical composition of T. usneoides extracts and evaluate their biological activity in vitro and in vivo in a murine model of acute myeloid leukemia. The chemical composition of the extracts and fractions were analyzed by chromatographic techniques revealed the presence of cycloartane-type triterpenes and methoxylated flavonoids. The in vitro cytotoxic effects on the breast cancer (4T1 and MCF-7), melanoma (B16-F10), and leukemia (K562 and DA-3/ER-GM) cell lines of the ethanolic extract and fractions were evaluated. Furthermore, T. usneoides extract decreased the proliferation rate of DA-3/ER-GM cells, as well as their glucose consumption, and exerted a pro-oxidant effect. Despite the in vitro cytotoxic effects exerted on the murine leukemia cell line, the ethanolic extract of T. usneoides did not exhibit antitumor activity in a murine model of acute myeloid leukemia, which suggests that ex vivo analysis has no direct correlation with the in vivo effect. This observation also highlights the role of the microenvironment in regulating the activity of antitumor molecules, particularly the extract studied here. Therefore, for the development of phytomedicines, as for other antitumor molecules, extensive in vitro and in vivo analyzes are warranted to demonstrate the various interactions necessary to control tumor growth.

药用植物为发现针对白血病和各种其他形式癌症的新型治疗化合物提供了宝贵的资源。龙舌兰属植物,如龙舌兰,有不同的民族植物学用途,包括治疗痔疮、胃炎、关节炎、溃疡、喉咙痛、癌症和糖尿病。具体地说,乌拉伯地区的土著Zenúes已经使用T. usneoides治疗糖尿病。然而,关于褐叶蝉的研究很少发表。本研究的目的是测定金针叶提取物的化学成分,并评价其体外和体内对急性髓系白血病小鼠模型的生物活性。通过层析技术对提取物和馏分的化学成分进行分析,发现其中含有环artane型三萜和甲氧基黄酮类化合物。研究了乙醇提取物及其组分对乳腺癌(4T1和MCF-7)、黑色素瘤(B16-F10)和白血病(K562和DA-3/ER-GM)细胞系的体外细胞毒作用。此外,金银花提取物可降低DA-3/ER-GM细胞的增殖速率,降低细胞的葡萄糖消耗,并具有促氧化作用。尽管在体外对小鼠白血病细胞系有细胞毒作用,但在小鼠急性髓系白血病模型中,金针叶乙醇提取物没有表现出抗肿瘤活性,这表明离体分析与体内作用没有直接关联。这一观察结果也强调了微环境在调节抗肿瘤分子活性中的作用,特别是这里研究的提取物。因此,对于植物药物的开发,就像其他抗肿瘤分子一样,有必要进行大量的体外和体内分析,以证明控制肿瘤生长所必需的各种相互作用。
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引用次数: 0
Enhancement of intestinal tight junction assembly by Coffea arabica pulp aqueous extract: mechanism of action and role of SIRT-1 阿拉比卡咖啡浆水提物增强肠道紧密结组装:SIRT-1的作用机制和作用
IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-20 DOI: 10.1007/s13596-025-00817-x
Pichayapa Sukmak, Laongdao Thongnak, Wanapas Wachiradejkul, Jakkapong Inchai, Nichapa Chindaduangratn, Natnicha Kitti-udom, Thaam Limwattananon, Nuttakritta Choksukchalalai, Wilasinee Satianrapapong, Sunisa Hankan, Doungporn Amornlerdpison, Atcharaporn Ontawong, Nattaphong Akrimajirachoote, Chanat Aonbangkhen, Chatchai Muanprasat, Chutima S. Vaddhanaphuti, Pawin Pongkorpsakol

Intestinal tight junction disruption is considered as one of key pathogenic factors of several diseases including inflammatory bowel diseases. At present, there is no FDA-approved drug targeting intestinal tight junction recovery. Coffea arabica pulp is an agricultural waste but its aqueous extract contains a number of polyphenol-rich, bioactive compounds. The main aim of this study was to elucidate the pharmacological effects of Coffea arabica pulp aqueous extract (CPE) on intestinal tight junction re-assembly. Transepithelial electrical resistance (TER) measurement indicated that CPE significantly enhanced TER across the intestinal epithelial-like T84 cell monolayers in a time- and dose-dependent manner with a maximal effect being observed at 1,000 µg/ml. MTT assay and nuclear staining indicated that CPE had no cytotoxic effect on T84 cells. Fluorescein isothiocyanate (FITC)-dextran permeability assay demonstrated that CPE suppressed intestinal tight junction-dependent leak pathway permeability. In addition, the effect of CPE on enhancing intestinal tight junction assembly was not affected by inhibitors of calcium/calmodulin-dependent protein kinase kinase β (CaMKKβ), AMP-activated protein kinase (AMPK), and extracellular signal-regulated kinase (ERK). Surprisingly, sirtuin-1 (SIRT-1) inhibitors abrogated CPE-induced tight junction assembly in T84 cell monolayers. Furthermore, immunostaining indicated that CPE enhanced re-distribution of occludin and zonula occludens-1 (ZO-1) to cell junction region via SIRT-1-dependent mechanism. Collectively, CPE may be useful in the treatment of diseases related to intestinal tight junction disruption.

肠紧密连接破坏被认为是炎症性肠病等多种疾病的关键致病因素之一。目前,还没有fda批准的针对肠道紧密连接恢复的药物。阿拉比卡咖啡的果肉是一种农业废弃物,但其水提取物含有许多富含多酚的生物活性化合物。本研究的主要目的是阐明阿拉比卡咖啡浆水提取物(CPE)对肠道紧密连接重组的药理作用。经上皮电阻(TER)测量表明,CPE显著增强肠上皮样T84细胞单层的TER,并呈时间和剂量依赖性,在1000µg/ml时效果最大。MTT试验和细胞核染色显示CPE对T84细胞无细胞毒作用。异硫氰酸荧光素(FITC)-葡聚糖渗透性试验表明,CPE抑制肠道紧密连接依赖性泄漏通路的渗透性。此外,CPE增强肠道紧密连接组装的作用不受钙/钙调素依赖性蛋白激酶β (CaMKKβ)、amp活化蛋白激酶(AMPK)和细胞外信号调节激酶(ERK)抑制剂的影响。令人惊讶的是,sirtuin-1 (SIRT-1)抑制剂消除了cpe诱导的T84细胞单层的紧密连接组装。此外,免疫染色表明CPE通过sirt -1依赖性机制增强了occludin和zonula occluden -1 (ZO-1)在细胞连接区域的再分布。总的来说,CPE可能有助于治疗与肠紧密连接破坏相关的疾病。
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引用次数: 0
Integrated yoga and naturopathy treatments in enhancing motor and sensory recovery in Guillain Barre syndrome- a case study 综合瑜伽和自然疗法在增强运动和感觉恢复格林巴利综合征-一个案例研究
IF 1.3 Q3 PHARMACOLOGY & PHARMACY Pub Date : 2025-01-15 DOI: 10.1007/s13596-025-00816-y
Geethashree Poojary, Shivaprasad Shetty, Prashanth Shetty

Guillain-Barre syndrome (GBS) is a severe, rapidly progressing paralytic neuropathy that typically develops after infections. The aim of this case report was to provide an integrative approach to the management of GBS. A male patient of 35 years old diagnosed with GBS presented with sensory and motor deficits was administered Naturopathy and Yoga therapies(N&Y) for 10 days in Nature Care Hospital (NCH) in the southern part of India. For the rehabilitation of patients with persistent neurological illnesses. Notable results were observed in the improvement of sensory and motor (muscle power, strength, general condition, and daily activities) along with quality of life. These findings suggest that N&Y has positive impacts on the management of GBS, further research with a larger scale is needed.

格林-巴利综合征(GBS)是一种严重的、进展迅速的麻痹性神经病变,通常在感染后发生。本病例报告的目的是为GBS的管理提供一种综合方法。一位35岁的男性患者被诊断为GBS,表现为感觉和运动障碍,在印度南部的自然护理医院(NCH)接受了10天的自然疗法和瑜伽疗法(N&;Y)。用于持续性神经系统疾病患者的康复。在感觉和运动(肌肉力量、力量、一般状况和日常活动)以及生活质量的改善方面观察到显著的结果。这些发现表明,N&;Y对GBS的管理有积极影响,需要进一步进行更大规模的研究。
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引用次数: 0
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Advances in Traditional Medicine
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