• 【西洋参叶和茎中的三萜皂苷。】 复制标题 收藏 收藏
    DOI:10.1080/10286020108041379 复制DOI
    作者列表:Wang JH,Li W,Sha Y,Tezuka Y,Kadota S,Li X
    BACKGROUND & AIMS: :In the chemical investigation on the saponin composition of leaves and stems of Panax quinquefolium L., two new minor dammarane saponins, quinquenoside L1 (1) and L2 (2) have been isolated. By means of physico-chemical evidences and spectral analysis their structures were established as 3-O-[beta-D-glucopyranosyl-(1-2)-beta-D-glucopyranosyl]-20-O-beta-D-glucopyranosyl-dammara-23,25-diene-3beta, 12beta, 20(S)-triol (1) and 3-O-[beta-D-glucopyranosyl-(1-2)-beta-D-glucopyranosyl]-20-O-beta-D-glucopyranosyl-(24Z)-dammar-24-ene-3beta, 12beta, 20(S), 26-tetraol (2).
    背景与目标: :在对西洋参叶和茎的皂苷成分进行化学研究时,已分离出两种新的小金刚烷皂苷,喹诺酮苷L1(1)和L2(2)。通过理化证据和光谱分析,将其结构确定为3-O- [β-D-吡喃葡萄糖基-(1-2)-β-D-吡喃葡萄糖基]-20-O-β-D-吡喃葡萄糖基-dammara -23,25-二烯-3beta,12beta,20(S)-三醇(1)和3-O- [β-D-吡喃葡萄糖基-(1-2)-β-D-吡喃葡萄糖基] -20-O-beta -D-吡喃葡萄糖基-(24Z)-dammar-24-ene-3beta,12beta,20(S),26-tetraol(2)。
  • 【白头翁Regel皂苷对蜗牛钉螺的杀软体动物活性的实验室评估。】 复制标题 收藏 收藏
    DOI:10.3967/0895-3988.2012.02.015 复制DOI
    作者列表:Chen YQ,Xu QM,Liu YL,Li XR,Yang SL,Zhuge HX
    BACKGROUND & AIMS: OBJECTIVE:To observe the toxicity of Pulsatilla chinensis (Bunge) Regel saponins (PRS) against Oncomelania hupensis (O. hupensis). METHODS:O. hupensis snails were exposed to 40% and 80% of 24 h LC50 of PRS for 24 h, and then choline esterase (CHE), alanine aminotransferase (ALT), alkaline phosphatase (ALP), lactate dehydrogenase (LDH) activities in cephalopodium and liver of snails were determined. Niclosamide (NIC) was used as the reference molluscicide. Zebra fish lethality test was evaluated to non-target aquatic species of PRS. RESULTS:The molluscicidal activity of PRS (LC50 at 24 h: 0.48 mg/L) was similar to that of NIC (LC50 at 24 h: 0.16 mg/L). Significant alterations about CHE, ALP, and ALT activities both in the cephalopodium and the liver of snails were observed when O. hupensis was exposed to 40% and 80% LC50 of PRS or NIC for 24 h. PRS and NIC could not affect LDH activity in the cephalopodium and the liver. Lower toxicity to fish of PRS was observed up to the highest concentration tested than NIC. CONCLUSION:PRS, as compared with the reference molluscicide NIC, is thought to be used for the control of harmful vector snails safely.
    背景与目标: 目的:观察白头翁Regel皂苷(PRS)对钉螺(O. hupensis)的毒性。
    方法:O。将hupensis蜗牛暴露在24小时的PRS LC50的40%和80%中24小时,然后将头皮和肝脏中的胆碱酯酶(CHE),丙氨酸氨基转移酶(ALT),碱性磷酸酶(ALP),乳酸脱氢酶(LDH)活性暴露确定蜗牛的数量。尼氯酰胺(NIC)用作参比杀软体动物剂。斑马鱼致死性测试被评估为非目标PRS水生物种。
    结果:PRS的杀软体动物活性(24小时LC50:0.48 mg / L)与NIC相似(24小时LC50:0.16 mg / L)。当将猪链球菌分别暴露于40%和80%的PRS或NIC LC50 24小时后,蜗牛的头足类和肝脏中的CHE,ALP和ALT活性均发生了显着变化。 PRS和NIC不会影响头皮和肝脏中LDH的活性。在最高测试浓度下,与NIC相比,PRS对鱼类的毒性较低。
    结论:与参考杀软体动物NIC相比,PRS被认为可安全地用于控制有害媒介蜗牛。
  • 【人参皂苷对大鼠海马片中β-淀粉样蛋白抑制的乙酰胆碱释放的影响。】 复制标题 收藏 收藏
    DOI:10.1055/s-2001-17366 复制DOI
    作者列表:Lee TF,Shiao YJ,Chen CF,Wang LC
    BACKGROUND & AIMS: In view of the facts that ginseng has been shown to improve age-related memory deficits and beta-amyloid-related peptides have been suggested to play a significant role in memory degeneration in the elderly, the present study was carried out to examine the effect of various ginsenosides on beta-amyloid peptides-modulated acetylcholine (ACh) release, a key neurotransmitter in memory processing, from the hippocampal slices. Addition of beta-amyloid fragment(25 - 35) (0.01 - 1 microM) in the superfusion medium suppressed the K(+)-evoked [(3)H]-ACh release from the rat hippocampal slices in a concentration-related manner and about 40 % reduction in ACh outflow was observed when incubating with the highest concentration of an amyloid fragment (1 microM). Inclusion of the ginsenoside components Rb(1) (0.1 microM), but not Rg(1), caused a rightward shift of the concentration-response curve of beta-amyloid. The reversal of the beta-amyloid-inhibited ACh release by Rb(1) was not blocked by tetrodotoxin (1 microM) indicating that an interaction occurs at the cholinergic synapse. These results suggest that Rb(1) may elicit its anti-amnesic effect by minimizing the inhibitory effect of beta-amyloid peptides.

    背景与目标: 鉴于人参已被证明可以改善与年龄有关的记忆缺陷,而与β-淀粉样蛋白有关的肽被认为在老年人的记忆退化中起着重要的作用,因此本研究旨在探讨人参的作用。 β-淀粉样肽调节的乙酰胆碱(ACh)释放出各种人参皂甙,这是海马切片中记忆过程中的关键神经递质。在灌注培养基中添加β-淀粉样蛋白片段(25-35)(0.01-1 microM)以浓度相关的方式抑制了大鼠海马切片中K()诱发的[(3)H] -ACh的释放,且浓度相关。当与最高浓度的淀粉样蛋白片段(1 microM)一起孵育时,观察到ACh流出减少40%。人参皂苷成分Rb(1)(0.1 microM)而不是Rg(1)的加入导致β-淀粉样蛋白的浓度-反应曲线向右移动。 Rb(1)逆转β-淀粉样蛋白抑制的ACh释放并未被河豚毒素(1 microM)阻止,表明相互作用发生在胆碱能突触上。这些结果表明,Rb(1)可能通过最小化β-淀粉样肽的抑制作用而引起其抗记忆删除作用。

  • 【皂苷佐剂结构的影响。】 复制标题 收藏 收藏
    DOI:10.1021/acs.jmedchem.9b02063 复制DOI
    作者列表:Wang P,Ding X,Kim H,Michalek SM,Zhang P
    BACKGROUND & AIMS: :We have prepared a number of saponin-based vaccine adjuvant candidates. These unnatural saponins have a different terminal-functionalized side chain incorporated into the glucuronic acid unit that is attached to a triterpenoid core at its C3 position. The semisynthetic saponin adjuvants have shown significantly different immunostimulatory activities, suggesting that the structure of the side chain, triterpenoid core, and oligosaccharide domain together orchestrate saponin adjuvant's potentiation of immune responses. Among these new adjuvant candidates, VSA-2 (5b), a derivative of Momordica saponin (MS) II, showed consistent enhancement of immunoglobulin G2a (IgG2a) production when it was in formulation with either ovalbumin or recombinant hemagglutinin B (rHagB) antigen. With rHagB antigen, it induced a significantly higher IgG2a response than the positive control GPI-0100, a well-studied semisynthetic saponin adjuvant mixture derived from Quillaja saponaria Molina saponins, known for its ability to induce a balanced Th1/Th2 immunity. These results confirm that Momordica saponins are a viable natural source to provide potent saponin adjuvants after simple chemical derivatization and identify VSA-2 (5b) as another MS-based promising immunostimulant lead owing to its distinctive ability in potentiating the IgG2a response.
    背景与目标: :我们已经准备了许多基于皂苷的疫苗佐剂。这些非天然皂苷具有结合到葡糖醛酸单元中的不同的末端官能化侧链,所述葡糖醛酸单元在其C3位连接至三萜类核。半合成皂苷佐剂显示出明显不同的免疫刺激活性,表明侧链,三萜类核心和寡糖结构域的结构共同协调了皂苷佐剂的免疫应答增强作用。在这些新的佐剂候选物中,苦瓜皂苷(MS)II的衍生物VSA-2(5b)在与卵白蛋白或重组血凝素B(rHagB)抗原配制成制剂时显示出免疫球蛋白G2a(IgG2a)产生的持续增强。与rHagB抗原相比,它诱导的IgG2a反应明显高于阳性对照GPI-0100,这是一种经过充分研究的半合成皂苷佐剂混合物,得自Quillaja saponaria Molina皂苷,以其诱导平衡的Th1 / Th2免疫力而闻名。这些结果证实了苦瓜皂苷是可行的天然来源,可在简单的化学衍生化后提供有效的皂苷佐剂,并由于其独特的增强IgG2a反应能力而将VSA-2(5b)鉴定为另一种基于MS的有希望的免疫刺激剂。
  • 【凤仙花DC根中皂苷的抗炎活性。】 复制标题 收藏 收藏
    DOI:10.1080/14786419.2018.1519708 复制DOI
    作者列表:Grabowska K,Wróbel D,Żmudzki P,Podolak I
    BACKGROUND & AIMS: :Two triterpene saponins (IPS-1, IPS-2) for the first time were isolated from the roots of Impatiens parviflora DC. (Balsaminaceae). Their anti-inflammatory activity was evaluated by means of two in vitro models: anti-hyaluronidase and anti-denaturation assays. Both saponins were shown to be potent hyaluronidase inhibitors that affect the enzyme in a dose-dependent manner. The anti-hyaluronidase effect of IPS-2 (IC50 = 286.7 µg/mL) was higher than that of the reference drug: escin (IC50 = 303.93 µg/mL). Both saponins protected bovine serum albumin from heat-induced denaturation in a dose-dependent manner. IPS-1 demonstrated higher anti-denaturation effect (IC50 = 86.7 µg/ml) than IPS-2 (IC50 = 109.76 µg/mL) or the standard drug: acetylsalicylic acid (IC50 = 262.22 µg/mL). In conclusion, potent activity of IPS-1, IPS-2 in both in vitro assays shows that saponins from I. parviflora have anti-inflammatory activity. The obtained results allow to suggest that such compounds may be beneficial in inflammatory conditions, especially associated with excessive degradation of hyaluronic acid.
    背景与目标: :首次从小凤仙花DC的根中分离出两个三萜皂苷(IPS-1,IPS-2)。 (鼠尾草科)。通过两种体外模型评估它们的抗炎活性:抗透明质酸酶和抗变性测定。两种皂苷均被证明是有效的透明质酸酶抑制剂,以剂量依赖的方式影响该酶。 IPS-2(IC50- = 286.7ICµg / mL)的抗透明质酸酶作用高于参考药物七叶皂苷(IC50 = 303.93 µg / mL)。两种皂苷均以剂量依赖性方式保护牛血清白蛋白免于热诱导的变性。 IPS-1具有比IPS-2(IC50 = 109.76µg / mL)或标准药物乙酰水杨酸(IC50 = 262.22µg / mL)更高的抗变性作用(IC50 = 86.7(µg / mL)。总之,在两种体外测定中,IPS-1,IPS-2的有效活性均显示小花伊豆中的皂苷具有抗炎活性。所获得的结果表明,这类化合物在炎性疾病中可能是有益的,特别是与透明质酸的过度降解有关。
  • 【棕榈叶(Trevesia palmata)叶片中的新的卢潘型和乌烷型三萜皂苷。】 复制标题 收藏 收藏
    DOI:10.1080/14786419.2019.1696797 复制DOI
    作者列表:Yen PH,Doan VV,Lien GTK,Chuong NTH,Thanh NTV,Trang DT,Dung DT,Nhiem NX,Tai BH,Minh CV,Kiem PV
    BACKGROUND & AIMS: :Three new triterpene saponins including two lupane-types and an ursane-type were isolated from the leaves of Trevesia palmata. Their structures were determined as 2α,3β,23-trihydroxylup-20(29)-en-28-oic acid 3-O-α-L-arabinopyranoside (1), 2α,3β,23-trihydroxylup-20(29)-en-28-oic acid 3-O-[α-L-arabinopyranoside]-28-O-[β-D-glucopyranosyl] ester (2), and 2α,3β,23-trihydroxyurs-12-en-28-oic acid 3-O-[α-L-arabinopyranoside]-28-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl] ester (3) by analysis of their HR-ESI-MS, 1D and 2D NMR spectra. The 2α,3β,23-trioxygenated pentacyclic triterpenes were uncommonly found in the nature. At concentration of 100 µM, compounds 1-3 inhibited NO production in LPS activated BV2 cells with inhibitory rates of 17.4 ± 1.8%, 33.1 ± 1.2%, and 11.7 ± 2.2%, respectively. But, they did not significantly inhibit yeast α-glucosidase activity.
    背景与目标: :从Trevesia palmata的叶片中分离出三个新的三萜皂苷,包括两个Lupane型和一个Ursane型。它们的结构被确定为2α,3β,23-trihydroxylup-20(29)-en-28-oic acid3-O-α-L-arabinopyranoside(1),2α,3β,23-trihydroxylup-20(29)- en-28-oic acid 3-O- [α-L-阿拉伯吡喃糖苷] -28-O- [β-D-吡喃吡喃糖基]酯(2)和2α,3β,23-trihydroxyurs-12-en-28-oic通过对其HR-ESI-MS,1D进行分析,发现酸3-O- [α-L-阿拉伯吡喃糖苷] -28-O- [β-D-吡喃葡萄糖基(1→2)-β-D-吡喃葡萄糖基]酯(3)和2D NMR光谱。在自然界中不常见的有2α,3β,23-三加氧五环三萜。在浓度为100μm时,化合物1-3抑制LPS激活的BV2细胞中NO的产生,抑制率分别为17.4±1.8%,33.1±1.2%和11.7±2.2%。但是,它们没有显着抑制酵母α-葡萄糖苷酶的活性。
  • 【海参中的皂苷通过激活BMP2 / Smads途径促进MC3T3-E1细胞的成骨细胞分化。】 复制标题 收藏 收藏
    DOI:10.2174/1389201021666200519135446 复制DOI
    作者列表:Li Z,Tian Y,Ma H,Wang M,Yan Z,Xue C,Wang J
    BACKGROUND & AIMS: BACKGROUND:Several studies have shown that plant saponins promoted osteoblast differentiation and improved osteoporosis. In current study, sea cucumber saponins (SCS) with a purity of 80% was extracted from Filipino sea cucumber, with a similar structure to plant saponins. OBJECTIVE:This study aims to investigate the effects of SCS on bone formation in vitro and ex vivo. RESULTS:SCS significantly promoted osteogenic differentiation and mineralization of MC3T3-E1 cells, as well as new osteoid formation in neonatal mouse calvarias ex vivo. qRT-PCR results indicated that SCS markedly down-regulated the expression of C/EBPα* and PPARγ at the levels of transcription, which demonstrate that SCS inhibit the trans-differentiation of MC3T3-E1 cells to an adipocytic phenotype. What is more, further studies revealed that SCS increased the expression levels of Runx2 and OSX. The mechanism revealed that SCS induced the expression of BMP2 and p-Smad1/5, which indicated that SCS facilitated osteogenesis via activating the BMP2/Smads signaling pathway. CONCLUSION:SCS promoted osteogenic differentiation of pre-osteoblasts by activating BMP2/Smads molecular pathway, providing theoretical basis for the development of sea cucumber saponins for the treatment to bone loss diseases such as osteoporosis.
    背景与目标: 背景:多项研究表明,植物皂素可促进成骨细胞分化并改善骨质疏松症。在当前的研究中,从菲律宾海参中提取了纯度为80%的海参皂苷(SCS),其结构与植物皂苷相似。
    目的:本研究旨在探讨SCS对体外和离体骨形成的影响。
    结果:SCS显着促进了新生小鼠颅盖骨MC3T3-E1细胞的成骨分化和矿化,以及新的类骨质形成。 qRT-PCR结果表明,SCS在转录水平上显着下调了C /EBPα*和PPARγ的表达,这表明SCS抑制了MC3T3-E1细胞向脂肪表型的转分化。此外,进一步的研究表明,SCS增加了Runx2和OSX的表达水平。该机制揭示了SCS诱导BMP2和p-Smad1 / 5的表达,这表明SCS通过激活BMP2 / Smads信号通路促进了成骨。
    结论:SCS通过激活BMP2 / Smads分子途径促进成骨细胞的成骨分化,为开发海参皂苷治疗骨质疏松等骨质疏松疾病提供了理论依据。
  • 【Kalopanax pictus茎皮中的齐墩果烷型三萜和皂苷对LPS刺激的骨髓源性树突状细胞促炎性细胞因子产生的抑制作用。】 复制标题 收藏 收藏
    DOI:10.1007/s12272-013-0031-8 复制DOI
    作者列表:Quang TH,Ngan NT,Van Minh C,Van Kiem P,Nhiem NX,Tai BH,Thao NP,Chae D,Mathema VB,Koh YS,Lee JH,Yang SY,Kim YH
    BACKGROUND & AIMS: :Kalopanax pictus (Araliaceae) is a deciduous tree distributed in Korea, Japan, and China. The stem bark of K. pictus has been functionally used as a traditional crude drug for the treatment of various inflammatory diseases. In the present study, we describe the inhibitory effects of oleanane-type triterpenes and saponins isolated from the stem bark of K. pictus on production of pro-inflammatory cytokines in LPS-stimulated bone marrow-derived dendritic cells. Of the compounds tested, 16,23,29-trihydroxy-3-oxo-olean-12-en-28-oic acid (1), 4,23,29-trihydroxy-3,4-seco-olean-12-en-3-oate-28-oic acid (2), 3β,6β,23-trihydroxyolean-12-en-28-oic acid 28-O-β-D-glucopyranoside (3), nipponogenin E (6), 3β,6β,23-trihydroxyolean-12-en-28-oic acid (7), and caulophyllogenin (19) significantly inhibited the production of IL-12 p40 and IL-6 with IC50 values ranging from 3.3 to 9.1 μM. Compounds 2, 3, 7, and 19 significantly suppressed the secretion of TNF-α with IC50 ranging from 8.8 to 20.0 μM. These data provide scientific support for the use of K. pictus stem bark and its triterpene and saponin components in the inhibition of pro-inflammatory cytokine secretion, including IL-12 p40, IL-6, and TNF-α, and for prevention and treatment of inflammatory diseases.
    背景与目标: :Kalopanax pictus((科)是分布在韩国,日本和中国的落叶乔木。 Pic。K. pictus的茎皮已在功能上用作治疗各种炎性疾病的传统原料药。在本研究中,我们描述了从苦参根茎皮中分离得到的齐墩果烷型三萜和皂苷对LPS刺激的骨髓源性树突状细胞促炎性细胞因子产生的抑制作用。在测试的化合物中,16,23,29-三羟基-3-氧代-油酸-12-en-28-油酸(1),4,23,29-三羟基-3,4-seco-油酸-12-en -3-oate-28-oic acid(2),3β,6β,23-trihydroxyolean-12-en-28-oic acid28-O-β-D-glucopyranoside(3),nipponogenin E(6),3β, 6β,23-三羟基油酸酯-12-en-28-油酸(7)和花椰菜素(19)显着抑制IL-12 p40和IL-6的产生,IC50值在3.3至9.1μM之间。化合物2、3、7和19显着抑制TNF-α的分泌,IC50为8.8至20.0μM。这些数据提供了对K. pictus茎皮及其三萜和皂苷成分在抑制促炎性细胞因子分泌(包括IL-12 p40,IL-6和TNF-α)以及预防和治疗中的用途的科学支持。炎性疾病。
  • 【盐生植物盐柳中新型抗氧化剂三萜皂苷的评价。】 复制标题 收藏 收藏
    DOI:10.1016/j.bmcl.2012.05.017 复制DOI
    作者列表:Kim YA,Kong CS,Lee JI,Kim H,Park HY,Lee HS,Lee C,Seo Y
    BACKGROUND & AIMS: :As a part of an ongoing search for novel antioxidants from the salt marsh plants, bioactivity-isolation and structure determination of constituents from Salicornia herbacea were performed. One new triterpenoid saponin (4), along with three known saponins (1-3), has been isolated from n-BuOH fraction of S. herbacea. On the basis of the spectroscopic methods, the structure of the new saponin 4 was elucidated as 3β-hydroxy-23-oxo-30-noroleana-12, 20(29)-diene-28-oic acid 3-O-β-D-glucuronopyranosyl-28-O-β-d-glucopyranoside. Scavenging effects of saponins 1-4 were examined on 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical and peroxynitrite. Particularly, saponin 3 exerted significant antioxidant activity on both authentic peroxynitrite and peroxynitrite generated from morpholinosydnonimine (SIN-1).
    背景与目标: :作为对盐沼植物中新型抗氧化剂进行持续搜索的一部分,生物活性的分离和结构测定来自柳叶草(Salicornia herbacea)的成分。一种新的三萜皂苷(4),以及三种已知的皂苷(1-3),已从S. herbacea的n-BuOH馏分中分离出来。在光谱学方法的基础上,阐明了新的皂苷4的结构为3β-羟基-23-氧代-30-noroleana-12、20(29)-二烯-28-油酸3-O-β-D -葡萄糖醛酸吡喃糖基-28-O-β-d-吡喃葡萄糖苷。研究了皂苷1-4对1,1-二苯基-2-吡啶基-肼基(DPPH)自由基和过氧亚硝酸盐的清除作用。特别地,皂苷3对纯正亚硝酸盐和由吗啉代亚砜亚胺(SIN-1)产生的过氧亚硝酸盐均具有显着的抗氧化活性。
  • 【大豆皂苷对乙氧基甲烷诱导的小鼠结肠癌前病变的作用。】 复制标题 收藏 收藏
    DOI:10.1080/01635589709514526 复制DOI
    作者列表:Koratkar R,Rao AV
    BACKGROUND & AIMS: The effect of saponins isolated from soya bean flour on the incidence of aberrant crypt foci (ACF) induced by azoxymethane (AOM) in the colonic wall of CF1 mice was investigated. Four weekly injections of AOM, a known colon carcinogen, were administered to mice. One week after the last injection, mice were placed on an AIN-76 diet supplemented with 3% soya bean saponins or continued on the basal AIN-76 diet. Another group of mice was placed on the saponin diet without AOM initiation to observe the effect of saponins on the growth characteristics of mice. Dietary intake of soya saponins significantly reduced the incidence of ACF at the end of 14 weeks (postinitiation). Noninitiated mice maintained on a similar soya bean saponin-supplemented diet did not show any adverse effects on the growth and overall health of the animals. These findings suggest that soya bean saponins can play an important role in inhibiting the incidence of ACF in the colon of mice.

    背景与目标: 研究了从大豆粉中分离得到的皂苷对CF1小鼠结肠壁中由甲氧甲烷(AOM)诱导的异常隐窝病灶(ACF)发生率的影响。对小鼠进行每周四次的AOM注射,AOM是一种已知的结肠致癌物。在最后一次注射后一周,将小鼠置于补充有3%大豆皂苷的AIN-76日粮中,或继续接受基础AIN-76日粮。将另一组小鼠置于没有AOM引发的皂素饮食上,以观察皂素对小鼠生长特性的影响。在第14周结束时(开始后),饮食中摄入大豆皂苷的剂量可显着降低ACF的发生率。维持以相似的大豆皂素补充饮食的未启动小鼠对动物的生长和整体健康没有显示出任何不利影响。这些发现表明,大豆皂苷可以在抑制小鼠结肠中ACF的发生中发挥重要作用。

  • 【烫伤小鼠巨噬细胞改变TNF-α表达的机制和三七总皂苷的调节作用。】 复制标题 收藏 收藏
    DOI:10.1016/j.burns.2006.02.001 复制DOI
    作者列表:Wang Y,Peng D,Huang W,Zhou X,Liu J,Fang Y
    BACKGROUND & AIMS: AIM:To explore the mechanism of altered tumor necrosis factor-alpha (TNF-alpha) expression by peritoneal macrophages (PMPhi) and Panax notoginseng saponins (PNS) modulation in light of NF-kappaB signal transduction in severely scalded mice. METHODS:Eighteen percent total body surface area (TBSA) full-thickness scalded mice were used. PMPhi was collected at different time intervals (0, 2, 6, 12, 24 and 48 post-burn hour (PBH)) separately. The following parameters were measured: TNF-alpha mRNA and IL-10 mRNA expression (reverse transcription-polymerase chain reaction, RT-PCR), protein kinase C (PKC) activity (isotope incorporation analysis), NF-kappaB activity (electrophoretic mobility shift assay, EMSA), IkappaB-alpha expression (Western blot). RESULTS:After scald, increased expression of TNF-alpha mRNA of PMPhi peaked at 12 PBH. Meanwhile, expression of IL-10 mRNA dropped to the lowest level at 12 PBH. NF-kappaB activity was markedly activated and reached its peak at 2 PBH. Membrane PKC activity was up-regulated after scald and showed a positive correlation with the change of TNF-alpha mRNA. Expression of IkappaB-alpha first decreased at 2 PBH and then increased to high level at 24 PBH. When 12 PBH was chosen as the time point for in vitro intervention with the application of specific NF-kappaB inhibitor pyrrolidine dithiocarbamate (PDTC), PKC inhibitor H-7 and PNS, both TNF-alpha mRNA expression and NF-kappaB activity decreased significantly. CONCLUSIONS:These results indicate that abnormal expression of TNF-alpha mRNA of macrophages might be regulated by PKC-NF-kappaB signaling following severe burn. PNS might play an anti-inflammatory effect by inhibiting NF-kappaB activity and TNF-alpha mRNA expression.
    背景与目标: 目的:探讨严重烫伤小鼠的腹膜巨噬细胞(PMPhi)和三七总皂苷(PNS)调节改变肿瘤坏死因子-α(TNF-α)表达的机制。
    方法:使用百分之十八的全身表面积(TBSA)全层烫伤小鼠。在不同的时间间隔(燃烧后小时(PBH)分别为0、2、6、12、24和48)收集PMPhi。测量以下参数:TNF-αmRNA和IL-10 mRNA表达(逆转录-聚合酶链反应,RT-PCR),蛋白激酶C(PKC)活性(同位素掺入分析),NF-κB活性(电泳迁移率变化)分析,EMSA),IkappaB-alpha表达(蛋白质印迹)。
    结果:烫伤后,PMPhi的TNF-αmRNA表达增加,在12 PBH时达到峰值。同时,IL-10 mRNA的表达在12 PBH时降至最低水平。 NF-κB活性被明显激活,并在2 PBH达到峰值。结垢后膜PKC活性上调,并与TNF-αmRNA的变化呈正相关。 IkappaB-α的表达首先在2 PBH时降低,然后在24 PBH时升高至高水平。当12 PBH在体外干预选择作为时间点与特定NF-κB的抑制剂吡咯烷二硫代氨基甲酸的应用(PDTC),PKC抑制剂H-7和PNS,二者的TNF-αmRNA的表达和NF-κB活性显著降低。
    结论:这些结果表明,严重烧伤后巨噬细胞TNF-αmRNA的异常表达可能受到PKC-NF-κB信号传导的调节。 PNS可能通过抑制NF-κB活性和TNF-αmRNA表达发挥抗炎作用。
  • 【三七总皂甙可通过诱导AKT / Nrf2信号传导的氧化还原途径来保护听觉细胞免受顺铂诱导的耳毒性。】 复制标题 收藏 收藏
    DOI:10.3892/mmr.2020.11390 复制DOI
    作者列表:Fei B,Liu Z,Xie L,Lv L,Zhu W,Liu J,Dai Y,She W
    BACKGROUND & AIMS: :Cisplatin‑induced cytotoxicity, such as nephrotoxicity, neurotoxicity and ototoxicity, restricts the clinical application of this compound. Panax notoginseng Saponins (PNS) exhibit potent free radical scavenging and antioxidant activity. PNS have been demonstrated to reduce cisplatin‑induced nephrotoxicity and neurotoxicity. The present study investigated the ability of PNS to protect the auditory HEI‑OC1 cell line against ototoxicity induced by cisplatin. PNS induced activation of the AKT/nuclear factor erythroid 2‑related factor 2 (Nrf2) signaling pathway. Following pretreatment with PNS, HEI‑OC1 cells were treated with cisplatin and cultured for 24 h. The viability of HEI‑OC1 cells was examined using a Cell Counting Kit‑8 assay. Double staining analysis was used to measure cell apoptosis. The ability of PNS to reduce reactive oxygen species (ROS) levels was assessed by flow cytometry. The levels of phosphorylated (p)‑AKT, heme oxygenase 1 (HO‑1), NAD(P)H quinone dehydrogenase 1 (NQO1), glutamate‑cysteine ligase catalytic (GCLC) and Nrf2 were measured by western blotting. HEI‑OC1 cells that were pretreated with PNS exhibited significantly increased cell viability compared with that noted in cells treated only with cisplatin. In addition, PNS suppressed the induction of apoptosis and ROS production following cisplatin treatment. The upregulation of NQO1, HO‑1 and GCLC expression in PNS‑pretreated cells was associated with p‑AKT levels and the activation of Nrf2. These findings suggested that PNS protected auditory cells against ototoxicity induced by cisplatin by activating AKT/Nrf2 signaling. PNS may serve as a potential candidate in regulating cisplatin‑induced cytotoxicity.
    背景与目标: :顺铂诱导的细胞毒性,例如肾毒性,神经毒性和耳毒性,限制了该化合物的临床应用。三七总皂甙(PNS)具有很强的清除自由基和抗氧化的作用。已证明PNS可以减少顺铂引起的肾毒性和神经毒性。本研究调查了PNS保护听觉HEI-OC1细胞系免受顺铂诱导的耳毒性的能力。 PNS诱导AKT /核因子红系2相关因子2(Nrf2)信号通路的激活。用PNS预处理后,用顺铂处理HEI-OC1细胞并培养24小时。使用Cell Counting Kit-8分析法检查了HEI‑OC1细胞的生存能力。双重染色分析用于测量细胞凋亡。通过流式细胞仪评估PNS降低活性氧(ROS)水平的能力。通过蛋白质印迹法测量了磷酸化(p)-AKT,血红素加氧酶1(HO-1),NAD(P)H醌脱氢酶1(NQO1),谷氨酸半胱氨酸连接酶催化(GCLC)和Nrf2的水平。与仅用顺铂处理的细胞相比,经PNS预处理的HEI‑OC1细胞显示出明显提高的细胞活力。此外,PNS抑制顺铂治疗后细胞凋亡的诱导和ROS的产生。 PNS预处理的细胞中NQO1,HO-1和GCLC表达的上调与p-AKT水平和Nrf2的激活有关。这些发现表明,PNS通过激活AKT / Nrf2信号传导保护听觉细胞免受顺铂诱导的耳毒性。 PNS可能是调节顺铂诱导的细胞毒性的潜在候选药物。
  • 【三七总皂甙对精子活力和体外进程的影响。】 复制标题 收藏 收藏
    DOI:10.1016/S0944-7113(98)80068-8 复制DOI
    作者列表:Chen JC,Xu MX,Chen LD,Chen YN,Chiu TH
    BACKGROUND & AIMS: :In this present study we investigated the effects of a saponin fraction prepared from the roots of Panax notoginseng (Burt.) F. H. Chen (Family Araliaceae), on human sperm motility and progression in vitro. Fifteeen human semen samples were collected and qualified according to the criteria of W.H.O. The saponin fraction was evaluated at 1.0 mg/ml and 2.0 mg/ml respectively. The results demonstrate that the fraction increased motility as well as progression of sperm at the 60(th) minute or the 120(th) minute.
    背景与目标: :在本研究中,我们调查了由三七(Burax。F. H. Chen)(五加科)的根制备的皂苷组分对人精子运动性和体外生长的影响。根据W.H.O.的标准收集50种人类精液样品并进行鉴定。皂苷分数分别评估为1.0 mg / ml和2.0 mg / ml。结果表明,该分数在60(th)分钟或120(th)分钟时增加了活力以及精子的进程。
  • 【来自Quillaja saponaria Molina的皂苷:分离,鉴定和形成免疫刺激复合物(ISCOM)的能力。】 复制标题 收藏 收藏
    DOI:10.2174/156720106778559092 复制DOI
    作者列表:Pham HL,Ross BP,McGeary RP,Shaw PN,Hewavitharana AK,Davies NM
    BACKGROUND & AIMS: :ISCOMs have received much attention as vaccine adjuvants due to their immunostimulatory effects. They are colloidal particles typically comprised of phospholipids, cholesterol and Quil A, a crude mixture of saponins extracted from the bark of Quillaja saponaria Molina. We have previously shown that ISCOMs can be prepared by ether injection wherein an ether solution of phospholipids and cholesterol in a mass ratio of 5:2 is injected into a solution of Quil A at a mass ratio of 7 lipids: 3 Quil A. The aim of this study was firstly to isolate and characterise discrete fractions of Quil A and secondly to investigate which of these fractions were able to form ISCOMs by the method of ether injection. Six fractions of Quil A were isolated by semi-preparative reverse phase high performance liquid chromatography (RP-HPLC) and characterised by analytical HPLC, liquid chromatography tandem mass spectrometry (LC-MS) and the qualitative Liebermann-Burchard and Molisch tests for triterpenoids and carbohydrates respectively. ISCOMs were subsequently prepared from the isolated fractions by the method of ether injection and the resulting preparations characterized by photon correlation spectroscopy (PCS) and negative stain transmission electron microscopy (TEM). The molecular weights of the major compounds in the fractions ranged from approximately 1200 to approximately 2300 Da; all fractions tested positive for triterpenoids and saccharides and four of the fractions were identified as QS-7, QS-17, QS-18 and QS-21 by analysis (LC-MS and analytical HPLC). Injection of ether solutions of lipids into aqueous solutions of QS-17, QS-18 or QS-21 all resulted in homogeneous ISCOM dispersions. The combination of lipids and QS-7 by ether injection produced lamellae and liposomes as the prominent structures and a minor amount of ISCOMs. The remaining two hydrophilic, low molecular weight fractions of Quil A did not produce ISCOMs, instead liposomes and helical structures predominated in the samples.
    背景与目标: 由于其免疫刺激作用,ISCOM作为疫苗佐剂已受到广泛关注。它们是通常由磷脂,胆固醇和Quil A(一种从Quillaja saponaria Molina的树皮中提取的皂苷的粗混合物)组成的胶体颗粒。先前我们已经表明,可以通过醚注入制备ISCOM,其中将质量比为5:2的磷脂和胆固醇的醚溶液以质量比为7的脂质:3 Quil A注入到Quil A的溶液中。这项研究的目的是首先分离和表征Quil A的离散部分,其次研究通过醚注入的方法,其中哪些部分能够形成ISCOM。通过半制备反相高效液相色谱(RP-HPLC)分离出六部分Quil A,并通过分析HPLC,液相色谱串联质谱(LC-MS)以及定性的Liebermann-Burchard和Molisch试验对三萜类化合物和碳水化合物分别。随后通过醚注入法从分离的级分中制备ISCOM,并通过光子相关光谱(PCS)和负染色透射电子显微镜(TEM)对所得制剂进行表征。馏分中主要化合物的分子量为约1200至约2300Da;通过分析(LC-MS和分析型HPLC),所有三萜类和糖类呈阳性的所有馏分均被鉴定为QS-7,QS-17,QS-18和QS-21。将脂质的醚溶液注射到QS-17,QS-18或QS-21的水溶液中均产生均匀的ISCOM分散体。通过醚注射将脂质和QS-7结合在一起,可形成片状和脂质体,这是其主要结构和少量ISCOM。 Quil A的其余两个亲水性低分子量级分不产生ISCOM,而是在样品中占主导地位的脂质体和螺旋结构。
  • 【番茄皂素转化为孕烷衍生物。】 复制标题 收藏 收藏
    DOI:10.1248/cpb.c14-00004 复制DOI
    作者列表:Nohara T,Manabe H,Fujiwara Y,Ikeda T,Ono M,Murakami K,Nakano D,Kinjo J,Kajimoto T
    BACKGROUND & AIMS: :Here reports new conversions methods of tomato saponins, esculeoside A (1) and a mixture of esculeosides B-1 (2) and B-2 (3), (the latter two were obtained from tomato cans) into pregnane derivative (5) by an alkal treatment followed by acid treatment. Compound 1 or a mixture of 2 and 3 were each refluxed with 1 N KOH to afford a characteristic pyridine steroidal glycoside (4), which was then treated with 2 N HCl-MeOH to afford a pregnane derivative, 3β-hydroxy-5α-pregn-16-en-20-one (5). The results of the above two reactions indicated that tomato saponins are chemically closely related to pregnane hormones. We assume that the assimilated tomato saponins via the small intestine are metabolized into pregnane derivatives, demonstrating various bioactivities such as anti-cancer, anti-osteoporosis, and anti-menopausal disorder activities.
    背景与目标: :这里报道了将番茄皂苷,七叶皂甙A(1)和七叶皂甙B-1(2)和B-2(3)的混合物(后两者是从番茄罐中获得)转化为孕烷衍生物的新方法(5)通过碱处理,然后进行酸处理。将化合物1或2和3的混合物分别与1 N KOH回流以提供特征性的吡啶甾体糖苷(4),然后将其用2 N HCl-MeOH处理以提供孕烷衍生物3β-羟基-5α-孕烯-16-en-20-one(5)。上述两个反应的结果表明,番茄皂苷在化学上与孕激素具有密切的关系。我们假设通过小肠吸收的番茄皂苷被代谢成孕烷衍生物,表现出各种生物活性,例如抗癌,抗骨质疏松和抗更年期疾病活动。

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