Caesalpinia

  • 文章类型: Journal Article
    牙龈炎是牙龈的炎症,是通过核因子-κB(NF-κB)的活性引起牙周病发展的最初原因,白细胞介素-1β(IL-1β),白细胞介素-6(IL-6),p38和肿瘤坏死因子-α(TNF-α)。未解决的慢性炎症可导致身体其他部位的持续紊乱。巴西林是一种天然存在的植物化学物质,可能具有抗菌和抗炎作用。基于天然植物化合物的处理,巴西林,以易于应用的局部乳膏的形式开发。
    目的是通过免疫组织化学(IHC)方法开发局部乳膏形式的天然化合物brazilin作为抗炎剂,以减少NF-κB的表达,和促炎基因IL-1β的表达,IL-6、p38和TNF-α。
    用牙龈卟啉单胞菌诱导雄性Sprague-Dawley大鼠牙龈炎。观察组包括用单次施用巴西林膏治疗的大鼠和用两次施用巴西林膏治疗的大鼠。治疗施用15天。在第3、6、9、12和15天,使用苏木精-伊红和Masson三色染色进行解剖伤口观察和伤口组织学。使用IHC方法分析NF-κB蛋白表达。牙龈炎症基因NF-κB的表达,IL-1β,使用q-RTPCR测量IL-6、p38和TNF-α。
    单双应用brazilin乳膏可增加血管生成并降低NF-κB蛋白表达,除了IL-1β,IL-6、p38和TNF-α基因表达。
    在大鼠牙龈炎模型中,Brazilin乳膏可以在牙龈组织中用作抗炎剂。
    UNASSIGNED: Gingivitis is an inflammation of the gums that is the initial cause of the development of periodontal disease by the activity of Nuclear Factor-kappa B (NF-κB), Interleukin-1β (IL-1β), Interleukin-6 (IL-6), p38, and Tumor Necrosis Factor-α (TNF-α). Unaddressed chronic inflammation can lead to persistent disturbances in other parts of the body. Brazilin is a naturally occurring plant chemical that may have antibacterial and anti-inflammatory effects. Treatment based on the natural plant compound, brazilin, is developed in the form of a topical cream for easy application.
    UNASSIGNED: The aim is to develop the natural compound brazilin in the form of a topical cream as an anti-inflammatory agent to reduce NF-κB expression through Imunohistochemistry (IHC) methods, and the expression of pro-inflammatory genes IL-1β, IL-6, p38, and TNF-α.
    UNASSIGNED: Male Sprague-Dawley rats were induced with gingivitis using P. gingivalis bacteria. The observed groups included rats treated with a single application of brazilin cream and rats treated with two applications of brazilin cream. The treatment was administered for 15 days. On days 3, 6, 9, 12, and 15, anatomical wound observations and wound histology using hematoxylin-eosin and Masson\'s Trichrome staining were performed. NF-κB protein expression was analyzed using the IHC method. Gingival inflammation gene expression of NF-κB, IL-1β, IL-6, p38, and TNF-α was measured using q-RTPCR.
    UNASSIGNED: Single and double applications of brazilin cream increased angiogenesis and decreased NF-κB protein expression, in addition to the IL-1β, IL-6, p38, and TNF-α gene expressions.
    UNASSIGNED: In a rat gingivitis model, Brazilin cream may function as an anti-inflammatory agent in the gingival tissue.
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  • 文章类型: Clinical Trial Protocol
    背景:乳腺癌的化疗是有效的,但可以产生明显的毒性并导致肿瘤耐药。使用标准化植物提取物的联合治疗可以是改善反应并允许抗肿瘤免疫反应的有效激活的替代方案,这有利于短期和长期的恢复。刺槐P2Et提取物在乳腺癌细胞和动物模型中具有抗肿瘤活性,改善肿瘤微环境,并诱导针对肿瘤的特异性免疫反应的激活,并且与蒽环类药物一起使用时具有协同作用,这使得它成为患者评估的一个很好的候选人。
    方法:在单个中心进行,这个第二阶段的研究是随机的,双盲,安慰剂对照试验旨在评估P2Et提取物在诊断为II期和III期乳腺癌患者中的安全性和有效性,谁有资格接受新辅助治疗。该研究旨在确定I期试验中先前确定的最佳生物剂量的安全性,同时研究各种疗效结果。这些结果包括生活质量的改善,免疫调节,代谢概况,微生物组,以及肿瘤减少等临床指标,无病生存,和病理反应,在治疗方案的不同阶段进行评估。
    结论:假设在乳腺癌患者中使用P2Et提取物治疗可以提高总体幸福感,积极影响他们的生活质量,同时也引发抗肿瘤免疫反应和增强免疫浸润。这些联合效应有可能有助于改善接受植物药和新辅助化疗治疗的患者的长期生存结果。
    背景:该试验在美国国家医学图书馆注册,标识符为NCT05007444。首次注册于8月16日,2021年。最后更新时间:8月9日,2022年。
    BACKGROUND: Chemotherapy in breast cancer is effective but can generate significant toxicity and lead to tumor resistance. Joint treatment with standardized plant extracts can be an alternative to improve the response and allow an effective activation of the antitumor immune response that favors recovery in the short and long term. The P2Et extract of Caesalpinia spinosa presents antitumor activity in cells and animal models of breast cancer, improves the tumor microenvironment, and induces activation of the specific immune response against the tumor and is synergistic when used together with anthracyclines, which makes it a good candidate for evaluation in patients.
    METHODS: Conducted at a single center, this phase II study is a randomized, double-blind, placebo-controlled trial aimed at assessing the safety and efficacy of P2Et extract in patients diagnosed with stage II and III breast cancer, who are eligible for neoadjuvant treatment. The study aims to determine the safety profile at the previously established optimal biological dose from phase I trial while investigating various efficacy outcomes. These outcomes include improvements in quality of life, immunomodulation, metabolic profile, microbiome, as well as clinical indicators such as tumor reduction, disease-free survival, and pathological response, assessed at different stages of the treatment regimen.
    CONCLUSIONS: Treatment with the P2Et extract in breast cancer patients is hypothesized to enhance overall well-being, positively influencing their quality of life, while also triggering an antitumor immune response and enhancing immune infiltration. These combined effects have the potential to contribute to improved long-term survival outcomes for patients receiving the phytomedicine alongside neoadjuvant chemotherapy treatment.
    BACKGROUND: This trial was registered in the US National Library of Medicine with identifier NCT05007444. First Registered August 16th, 2021. Last Updated: August 9th, 2022.
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  • 文章类型: Journal Article
    该研究报告了一种新型的19.6kDa蛋白酶抑制剂(PIs)的生化特征和作用机理,该抑制剂是从属于豆科的七叶树种子中分离出来的。进行了系统研究以确定纯度,特异性,生化和结构表征,及其在体外条件下抑制炎症的潜力。使用两步色谱技术来纯化PI。采用十二烷基硫酸钠聚丙烯酰胺凝胶电泳和基质辅助激光解吸电离飞行时间来检测蛋白质的分子质量。抑制剂的N-末端序列分析显示与Kunitz家族PIs的序列相似性。进行体外试管测定以确定抗炎活性,并且抑制剂对巨噬细胞(RAW264.7)和肺癌细胞系(A549)具有抗增殖作用。有效减少炎症介质的释放(NO,在用PI处理的巨噬细胞系(RAW264.7)中观察到IL-6,TNF-α)和弹性蛋白酶的活性。纯化的抑制剂显示了对炎症的有希望的结果。
    The study reports the biochemical characterization and mechanism of action of a novel 19.6 kDa protease inhibitor (PIs) isolated from the seeds of Caesalpinia decapetala belonging to the Fabaceae family. A systematic study was performed to ascertain the purity, specificity, biochemical and structural characterization, and its potential in curbing inflammation in vitro conditions. A two-step chromatography technique was used to purify the PIs. Sodium dodecyl sulfate polyacrylamide gel electrophoresis and matrix-assisted laser desorption ionization time of flight were employed to detect the molecular mass of the protein. N-terminal sequence analysis of the inhibitor showed sequence similarity with the Kunitz family PIs. The in vitro test tube assay was performed for determining the anti-inflammatory activity and the inhibitor is antiproliferative against macrophage (RAW264.7) and lung cancer cell lines (A549). An effective decrease in the release of inflammatory mediators (NO, IL-6, TNF-α) and on the activity of elastase was observed in macrophage cell lines (RAW264.7) which were treated with PIs. The purified inhibitor shows promising results against inflammation.
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  • 文章类型: Journal Article
    Caesalpinia bonduc is among the traditionally used plant in Benin, for its enhancement of male sexual activity. This study was undertaken to investigate the potential effect of C. bonduc root extracts on sexual behaviour of male Wistar rats. For that, thirty-six rats were allocated into six groups and orally treated with dimethyl sulfoxide (control), Sildenafil citrate (standard) and C. bonduc root extracts (hexane, ethyl acetate, ethanol and methanol) orally for twenty-eight days. Sexual behaviour parameters such as intromission frequency, intromission latency, mount latency and mount frequency were evaluated on day 0, 14 and 28. After the study completion, the body and reproductive organ weights as well as testicular histology and testosterone level were recorded. C. bonduc root extracts treatments had no significant effect on the body weight of rats. Enhancement in sexual behaviour was observed in ethanolic extract treated rats. An significant increase in mount frequency and intromission frequency as well as significant reduction in mount latency and intromission latency were noticed for ethanolic extract. The same extract caused an improvement in testosterone levels, relative testes weight and histological architecture. The findings demonstrate the aphrodisiac potential of C. bonduc root and lend support to the folkloric use as aphrodisiac.
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  • 文章类型: Journal Article
    Caesalpinia sappan L. (Caesalpiniaceae) has been traditionally used as blood tonic, expectorant, and astringent by boiling with water. Searching for HIV-1 integrase (IN) inhibitors from this plant is a promising approach. The EtOH extract of C. sappan and its isolated compounds were tested for their anti-HIV-1 IN effect using the multiplate integration assay, and the active compounds were determined for their mechanisms by molecular docking technique. Extraction from the heartwoods and roots of C. sappan led to the isolation of nine compounds. Among the compounds tested, sappanchalcone (2) displayed the strongest effect against HIV-1 IN with an IC50 value of 2.3 μM followed by protosappanin A (9, IC50  = 12.6 μM). Structure-activity relationships of compounds from C. sappan were found, in which the vicinal hydroxyl moiety were essential for anti-HIV-1 IN effect of compounds 2 and 9 by binding with the amino acid residues Gln148 and Thr66 in the core domain of the HIV- 1 IN enzyme, respectively.
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  • 文章类型: Journal Article
    BACKGROUND: The heartwood of Caesalpinia sappan L. (Leguminosae), a widely used Chinese medicine in folk, has been used for the treatment of traumatic injury, stasis pain, amenorrhea, dysmenorrheal, as well as stabbing pain in the chest, abdomen and so on. Protosappanin B and brazilin, as the major bioactive homoisoflavones of Sappan Lignum, are used as the marker components for the quality control of the herb in China Pharmacopoeia.
    OBJECTIVE: To establish a sensitive LC/MS/MS method for investigating the pharmacokinetic properties of protosappanin B and brazilin in rats after oral administration of Sappan Lignum extract, and compare their pharmacokinetics difference between normal and streptozotocin-treated rats.
    METHODS: A rapid, selective and sensitive LC/MS/MS method was developed and validated for the simultaneous quantification of protosappanin B and brazilin in rat plasma. Normal and streptozotocin-treated rats were orally administered with the Sappan Lignum extract at the same dose of 2.83 g extract/kg body weight (equivalent to 35.56 mg/kg of protosappanin B and 52.25 mg/kg of brazilin), respectively.
    RESULTS: After oral administration of Sappan Lignum extract, a remarkable increase (p<0.05) in the value of AUC0-24h, AUC0-∞, Cmax and T1/2 associated with protosappanin B and brazilin was observed in the streptozotocin-treated group. Compared with the normal rats, elimination of both compounds in the streptozotocin-treated rats was slower.
    CONCLUSIONS: The established method was successfully applied to compare the pharmacokinetic behaviors of protosappanin B and brazilin in rat plasma after oral administration of Sappan Lignum extract between normal and streptozotocin-treated groups; the results might suggest the accumulation of both compounds in diabetic pathologic states and the adverse reaction should be considered when it was used.
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  • 文章类型: Journal Article
    Morphological changes in the sperm of albino rats observed under scanning electron microscope illustrate the disturbance in the plasma membrane, as well as in the acrosomal membrane upon treatment with graded doses of an alcoholic seed extract of Caesalpinia bonducella. Considerable changes in the shape and size of the sperm head were observed, with the middle region of the sperm head being slightly constricted dorsoventrally. Most sperm appeared morphologically abnormal in the head region showing the distortion at the anterior region and bulging of the acrosomal membrane when compared with the control. The results of this study suggest that such effects might have resulted from general disturbance in proteins and alteration in the cauda epididymal milieu, probably due to an androgen deficiency consequent to the treatment with Caesalpinia bonducella.
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  • 文章类型: Journal Article
    BACKGROUND: The importance/study of community-based ethnobotanical traditional knowledge is ever-increasing for designing strategies for conservation and sustainable use, appropriate drugs and dose-illness relationship.
    OBJECTIVE: Present study aims to document ethnobotanical attributes of diverse medicinal plants used by the Taungya community to cure ailments in Terai Arc Landscape of India.
    METHODS: Ethnobotanical data was recorded by opting peoples\' participation approach involving interviews, semi-structured meetings, group discussions and filling of questionnaires.
    RESULTS: Total 116 medicinal plant species comprising 97 genera and 48 families have been recorded, out of which 16% used externally, 39% used internally and 45% used both externally and internally. Various plant parts were used in form of powder, paste, juice, decoction, infusion, poultice and oral consumption to cure a variety of ailments. Twenty-three species are used as remedies against skin problems, 17 species against rheumatism and 14 species against fever.
    CONCLUSIONS: Taungya community provided vast ethnobotanical knowledge in form of detail description of 116 medicinal plants (including 82 species with new phytomedicinal claims). Further, investigation on these species may lead to the discovery of novel bioactive molecules.
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  • 文章类型: Journal Article
    Brazilein (6a,7-dihydro-3,6a,10-trihydroxy-benz[b]indeno[1,2-d]pyran-9(6H)-one) is a compound obtained in a large amount from Caesalpinia sappan ethanol extracts with a high purity of about 98%. In isolated cardiac tissues, we found that brazilein exhibited a positive inotropic action in a concentration-dependent manner with little effect on heart rate and coronary perfusion. To study its possible mode of action, isolated rat hearts were treated with propranolol. This treatment did not alter the cardiotonic effect of brazilein, suggesting that this effect does not involve stimulation of beta-adrenoceptors. On the other hand, an analysis of the interaction between Na(+),K(+)-ATPase and brazilein was carried out. Albino guinea pig erythrocytes (mainly alpha1-Na(+),K(+)-ATPase isoforms) enriched with Na(+),K(+)-ATPase isoforms were utilized to compare the inhibition promoted by brazilein with that of classical inhibitors such as the cardiac glycoside deslanoside. Analysis of inhibition curves revealed that unlike deslanoside, brazilein had a relatively low affinity for erythrocyte isoforms and failed to completely inhibit the Na(+),K(+)-ATPase activity. The extent of the maximum inhibition rate was about 50%. The inhibitory effect of brazilein was not antagonized by 10 mmol/l K(+), as observed with deslanoside. Electrocardiogram research in vivo showed that brazilein did not induce the ventricular arrhythmias observed with deslanoside, suggesting that brazilein might have a less adverse effect and higher therapeutic index than cardiac glycosides. In light of all the above-mentioned observations, it can be concluded that brazilein, a molecule with a non-steroidal skeleton, produced its positive inotropic effect through inhibiting Na(+),K(+)-ATPase and could thus serve as a structural paradigm to develop new inotropic drugs.
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