Pesticidal character of phytoecdysteroids from Ajuga multiflora Bunge (Labiatae) on larvae of Cryptorrhynchus lapathi L. (Coleoptera: Curculionidae)

Eight kinds of phytoecdysteroids extracted from different parts of Ajuga multiflora Bunge (Labiatae) that were collected from different places at different time were tested for killing effects on the 2-instar larvae of Cryptorrhynchus lapathi L by adding them to the artificial diet of larvae. The experimental results indicated that adding 1-3-mL phytoecdysteroids to the artificial diet could lead 58%-100% of 2-instar larvae of C. lapathi to death within 24 days. The phytoecdysteroids extracted from the whole plant of A. multiflora which was collected before flowering time were much more effective than those extracted from the plants collected at flowering and after flowering periods, and the modified mortality rate of larvae reached 65.22%, 85.07%, and 98.11% at the dosage level of 1-mL, 2-mL, and 3-mL extracts, respectively. The extract made from root of A. multiflora plant was more effective in killing efficiency than those from stem and leaves, and the average death rates of larvae were up to 100%, 98.20% and 98.32% at dosage levels of 1-mL, 2-mL, and 3-mL extracts, respectively. The killing speed of the extracted phytoecdysteroids was slower than that of triflumuron, hexaflumuron or deltamethrin emulsifiable concentrate. The mortality rate of larvae is closely related to the feeding duration on the diets containing phytoecdysteroids. Feeding on the diets with addition of phytoecdysteroids for 16 days, more than 80% of treated 2-instar larvae of C. lapathi were led to death. The killing effect of the extracts was little affected by the growth areas of A. multiflora plant and the adding way to artificial diet.

紫背金盘(Ajuga nipponensis)次生物质对桔全爪螨(Panonychus citri)的驱避作用

研究了紫背金盘Ajuga nipponensisMakino各溶剂提取物和部分化合物对桔全爪螨Panonychus citriMcGregor雌成螨及其产卵的驱避作用。结果表明,石油醚萃取物、乙酸乙酯萃取物具有较强的生物活性。在0.1 g.L-1时,石油醚和乙酸乙酯萃取物对该螨处理1d后的产卵忌避率分别为:84.86%、69.88%;2d后为89.49%、82.19%;对雌成螨驱避率分别为:85.08%、68.66%;2d后为50.96%、69.84%。乙酸乙酯萃取物经分离得到四类化合物,结果表明:馏分Ⅰ为长链脂肪酸混合物,具有较强生物活性,2000μg/ml和1000μg/ml处理1d后,产卵忌避率分别为:80.77%、74.77%;2d后为73.81%、72.59%。2000μg/ml处理1d后对雌成螨的驱避率为:69.88%;2d后为74.24%。刺槐素Ⅱ、新克罗烷化合物Ⅲ和β-蜕皮甾酮Ⅳ在2000μg/ml均不表现活性。对馏分Ⅰ中的4个主要化合物单体进行活性测定,结果表明:十六烷酸、十六烷酸甲酯、十六烷酸乙酯和十八烷酸甲酯在2000μg/ml处理时,1d后,产卵驱避率分别为:75.18%、61.76%、59.18%和66.49%;2d后产卵驱避率为:66.67%、31.15%、46.75%和44.84%;雌成螨驱避率分别为:1d后,67.53%、63.79%、59.26%和68.00;2d后,67.23%、43.96%、48.23%和64.19%。在1000μg/ml处理时,1d后,产卵驱避率分别为:59.21%、59.16%、57.02%和61.40%;1d后,雌成螨驱避率分别为:69.64%、61.43%、55.76%和64.00%。

Inhibitory activities of extracts of Rumex dentatus, Commelina benghalensis, Ajuga bracteosa, Ziziphus mauritiana as well as their compounds of gallic acid and emodin against dengue virus

Objective: To investigate the inhibitory effects against dengue virus serotype 2(DENV-2) by five different fractions(extracted by methanol, ethanol, benzene, chloroform and n-hexane) of Rumex dentatus, Commelina benghalensis, Ajuga bracteosa and Ziziphus mauritiana, as well as their constituents(gallic acid, emodin, and isovanillic acid). Methods: All the samples were tested for cytotoxicity on baby hamster kidney cells by MTT assay and for anti-DENV-2 activity by plaque reduction neutralization assay using two DENV-2 doses(45 and 90 plaqueforming units or PFU). Results: All the samples except isovanillic acid exhibited significant prophylactic effects against DENV-2 infectivity(without cytotoxicity) when administered to cells before infection, but were not effective when given 6 h post-infection. The methanol extract of Rumex dentatus demonstrated the highest antiviral efficacy by inhibiting DENV-2 replication, with IC_(50) of 0.154 μg/mL and 0.234 μg/mL, when added before infection with 45 and 90 PFU of virus, respectively. Gallic acid also exhibited significant antiviral effects by prophylactic treatment prior to virus adsorption on cells, with IC_(50) of 0.191 μg/mL and 0.522 μg/mL at 45 and 90 PFU of DENV-2 infection, respectively. Conclusions: The highly potent activities of the extracts and constituent compounds of these plants against DENV-2 infectivity highlight their potential as targets for further research to identify novel antiviral agents against dengue.

Antiarthritic effects of Ajuga bracteosa Wall ex Benth.in acute and chronic models of arthritis in albino rats

Objective:To evaluate the antiarthritic activity of Ajuga bracteosa using albino rats.Methods: The antiarthritic activity of 70%ethanolic extract of Ajuga bracteosa(EEAB) was evaluated against turpentine oil- and formaldehyde- induced acute non immunological and complete freund's adjuvant(CFA)-induced chronic immunological arthritis in albino rats.Results:EEAB showed a significant(P<0.05) and dose dependent inhibitory effect against acute and chronic models of arthritis.EEAB exhibited better antiarthritic activity than the standard aspirin.Conclusions: EEAB exhibits a significant and promising antiarthritic activity against acute and chronic arthritis and supports the traditional use of Ajuga bracteosa for rheumatism and other inflammatory diseases.

Antioxidant and hepatoprotective effects of Ajuga nipponensis extract by ultrasonic-assisted extraction

Objective: To investigate suitable condition for extraction of the active components from Ajuga nipponensis(A. nipponensis). Methods: Orthogonal experimental design was used to determine the optimal extraction parameters for ecdysterones and flavonoids. Finally, the hepatoprotective abilities of A. nipponensis extracts were evaluated by CCl_4-induced animal models. Results:Maximum yields of flavonoids(7.87±0.10) mg/g and ecdysterones(0.73±0.02) mg/g could be obtained when the extraction time was 50 min, the extraction temperature was 60 ℃, and the ratio of sample to 70%(v/v) ethanol was 1:20(w/w). The antioxidant property of A. nipponensis was correlated to the concentration of its extracts. At 5 mg/m L, A. nipponensisextract scavenged 84.8% of DPPH radical and had absorbance values of 2.43±0.04 reducing power. Upon CCl_4-induced liver injury, glutamic oxaloacetic transaminase and glutamic pyruvic transaminase decreased significantly after the mice were treated with A. nipponensis. Histological researches also explained that A. nipponensis reduced the extent of liver lesions induced by CCl_4. Conclusions: A. nipponensis exhibited potent antioxidant activity in chemical experimental models and hepatoprotective effect against CCl_4-induced liver damage.

国产唇形科筋骨草属(Ajuga)研究概况

筋骨草属(Ajuga)隶属于唇形科,共有40余种,广泛分布于欧亚大陆温带地区,我国产18种.该属植物的多种次生代谢产物具有药用价值和经济价值.综述了国产唇形科筋骨草属多种药用植物的药材鉴别、药用成分及其生物活性分析等方面的研究进展.

Effects of Some Materials Extracted from Ajuga Species on the Larvae of Hyphantria cunea and its Natural Enemies

Six kinds of cxtracts drawn from Ajuga multiflora and .A. multliflora var. brevispicala and A. multiflora var.serotina using methanol and acetone were used in this experiment to test their killing activity to the second instar larvae ofHypantria cunea and their influence on its natural enemics. The average death rate caused by those extracts on the secondinstar larvae was 85.70%. The mortality rate caused by the extracts drawn with methanol was from 88.89% to 96.33%,which was significal1tly l1igl1er tl1a11 tl1at caused by acetol1e extracts. 'I11osc extracts were satt to TrchogranInIa `Ie)uI,xiIinIi,Coccinella septempunctata, the natural enelnies of H. cunea. We did not found any evidence shown that those extracts hadany influence the emergence and the devclopment of T. dendrolimi. Those methanolic extracts gotten from A. multiflora andA. multiflora var. brevispicata had no significant effects on the mortality of the larvae and adults of C. septenrpunctala.Those eXtracts could be used in the control of H cunea sattly.

Study on the Technological Conditions of Ultrasound-assisted Extraction of Polysaccharides from Ajuga ciliata Bunge (Fujian)

[Objectives]To determine the optimum technological conditions of ultrasound-assisted extraction of polysaccharides from Ajuga ciliata Bunge.[Methods]In this study,Ajuga ciliata Bunge was used as raw material,and an orthogonal experiment was designed based on the single factor experiment to investigate the effects of ultrasonic time,solid-liquid ratio,ultrasonic temperature and ultrasonic power on the extraction rate of polysaccharides from A.ciliata Bunge(Fujian).Range analysis,variance analysis and SSR test of significant differences between groups were carried out with SPSS 20.0,and the test results were verified.[Results]Under the conditions of ultrasonic temperature of 85℃,ultrasonic time of 80 min,solid-liquid ratio of 1∶15 g/mL and ultrasonic power of 500 W,the yield of polysaccharides from A.ciliata Bunge(Fujian)was the best.[Conclusions]This study can provide theoretical basis for the application of A.ciliata Bunge(Fujian).

Control Ability of Extracts from Ajuga Plants on Some Pests

Several phytoecdysteroids have been found in the extracts of A. multiflora and A.linearifolia using HPLC analysis. Those were 20-OH ecdysone, cyasterone, 3-acetate-20-OH ecdysone, 2-acetate-20-OH ecdysone, qugalactone. We found out that those phytoecdysteroids could lead the second instar larva of Clostera anastomosis and Stipnotia candida to death. The modified mortality rate was from 44.64% to 96.24%. Those extracts could signiticantly reduce the amount of nymph produced by the female Tuberolachnus salignus, The number of the nymph produced after treating with those extracts was only 20% to 70% of that produced by the untreated group. The death rate of the newly produced nymph which treated was among 33.33% to 58.82%. It was much higher than the death rate of the control group (1l7.57%).

<i>In Vitro</i>Characterization of the Efficacy and Safety Profile of a Proprietary Ajuga Turkestanica Extract

Ajuga Turkestanica, an herbaceous flowering species in the mint family, has been traditionally used in Turkeyand Uzbekistan for heart disease, muscle aches and stomach problems. Due to its high levels of phytoecdysteroids (particularly the characteristic C-11-hydroxylated Turkesterone), anabolic properties have also been reported. The aim of our study was to screen for early signs of efficacy and safety of a proprietary Ajuga turkestanica extract (ATE) using in vitro models. C2C12 mouse myotube cell line was used to study potential effects on viability and gene modulation. Cell viability was evaluated with different concentrations [0.2 - 200 ppm (mg/L)] of ATE. Gene modulation was assessed by quantitative polymerase chain reaction (qRT-PCR) after 6h incubation (ATE vs. the androgenic anabolic steroid methandrostenolone). Total androgenic activity was measured using the A-SCREEN bioassay. Ultra-high performance liquid chromatography analysis showed good correlation between the phytochemical profile of the native plant and our ATE. C2C12 mouse myotube cells treated with ATE experienced no significant loss of viability (concentrations 0.2 - 200 ppm, 1 - 24 hs, p > 0.05). qRT-PCR array analysis showed significant (p regulation of Caspase-3 (2-fold) and Myostatin (4-fold). The extract showed no androgenic activity within the dose range used. Our results indicate the potential for an ATE to support muscle mass without typical androgenic side effects of synthetic anabolic drugs.

A review of therapeutic potential of Ajuga bracteosa:A critically endangered plant from Himalaya

Medicinal plants are the nature’s gift for the humanity to treat various ailments and to spend a prosperous healthy life.There are almost 300 species of Ajuga.Among them,Ajuga bracteosa Wall.ex Benth(A.bracteosa)is an important medicinal plant of Himalaya regions.Its medicinal potential is due to the presence of various pharmacologically active compounds such as neo-clerodane diterpenoids,flavonol glycosides,iridoid glycosides,ergosterol-5,8-endoperoxide and phytoecdysones.The aim of this review article was to gather information about A.bracteosa which is currently scattered in form of various publications.This review article tried to attract the attention from people for therapeutic potential of A.bracteosa.The present review comprises upto date information of botanical aspects,active ingredients,traditional uses,and pharmacological activities such as antitumor,antimicrobial,antimalarial,anti-inflammatory,cardiotonic activity,antiarthritic activity,antioxidant activity and in vitro production of secondary metabolites for pharmaceuticals.Due to remarkable medicinal potential and commercialization,this species is indexed into critically endangered category and it is facing extremely high risk of extinction.Conservation practices and management techniques should be carried out to protect this important species from extinction.Recent biotechnological approaches will be quite helpful for its conservation.

基于UPLC特征图谱和含量测定的不同产地筋骨草质量评价

目的:建立筋骨草超高效液相色谱法(UPLC)特征图谱和其中哈巴苷、乙酰哈巴苷的含量测定方法。方法:采用Waters BEH C18色谱柱(150 mm×2.1 mm,1.7μm),以乙腈-甲醇(4∶1)为流动相A、0.2%磷酸水溶液为流动相B,梯度洗脱,流速为0.30 mL·min^(-1),柱温为30℃,检测波长为202 nm,进样量为2μL,建立筋骨草特征图谱,测定其中哈巴苷、乙酰哈巴苷的含量。结果:17批筋骨草特征图谱有10个共有峰,指认了其中4个成分分别为哈巴苷、乙酰哈巴苷、木犀草素-7-二葡萄糖苷酸、芹菜素-7-二葡萄糖苷酸;17批筋骨草中哈巴苷质量分数为0.33%~0.95%,乙酰哈巴苷质量分数为0.47%~1.93%。结论:建立的UPLC特征图谱和哈巴苷、乙酰哈巴苷含量测定方法可为筋骨草质量评价提供参考。

筋骨草水煎液灌胃对顺铂所致肾损伤的预防作用观察

目的探讨筋骨草水煎液对顺铂所致肾损伤的预防作用。方法取成年雄性昆明小鼠30只,随机分为对照组、顺铂组、筋骨草组,每组各10只。筋骨草组给予筋骨草水煎液灌胃,对照组和顺铂组给予生理盐水灌胃,每天1次,连续12 d;于实验第7天筋骨草水煎液灌胃2 h后,顺铂组和筋骨草组给予10 mg/kg顺铂一次性腹腔注射诱导肾损伤。处死小鼠,取肾脏,用HE染色观察肾组织病理学改变;采集血液,使用全自动生化分析仪测定BUN、Cr、CysC,ELISA法检测血清TNF-α、IL-1β;取肾组织,WST-1法检测SOD,TBA法检测MDA,微板法检测GSH;RT-qPCR法检测氧化应激(Nrf2、HO-1、NQO1)、凋亡(Bcl-2、Caspase-3、Bax)相关mRNA表达。结果与对照组比较,顺铂组肾小球体积增大,肾小管上皮细胞明显肿胀;血清BUN、Cr、CysC、TNF-α、IL-1β水平升高;肾组织MDA含量升高,SOD和GSH含量降低;肾组织Nrf2、HO-1、NQO1、Caspase-3、Bax mRNA表达上调,Bcl-2 mRNA表达下调。与顺铂组比较,筋骨草组肾组织病理损伤减轻;血清BUN、Cr、CysC、TNF-α、IL-1β水平降低;肾组织MDA含量下降、SOD、GSH含量升高,Nrf2、HO-1、NQO1、Bcl-2 mRNA表达升高,Caspase-3、Bax mRNA表达降低(P<0.05或<0.01)。结论筋骨草水煎液对顺铂所致肾损伤具有治疗作用,该作用可能是通过激活Nrf2信号通路、抑制NF-κB和Caspase-3信号通路进而抑制氧化应激、炎症反应和细胞凋亡实现的。

傣药大籽筋骨草乙酸乙酯部位抗炎镇痛作用研究

为了探讨傣药大籽筋骨草乙酸乙酯萃取部位(AMEA)的抗炎镇痛作用,采用角叉菜胶致小鼠足跖肿胀模型,以足跖肿胀度、足跖肿胀抑制率为指标,考察AMEA的抗炎作用;采用ELISA法测定足组织中肿瘤坏死因子-α(TNF-α)和白细胞介素-1β(IL-1β)水平,初步探讨AMEA抗炎作用机制;采用热板法和醋酸扭体法,考察镇痛作用.与模型组比较,致炎后5 h,AMEA低、中、高3个剂量组均对角叉菜胶所致小鼠足跖肿胀有显著抑制作用(P<0.01);各剂量组均能显著降低致炎足组织中TNF-α和IL-1β水平(P<0.05),并能明显减少冰醋酸所致小鼠扭体反应次数(P<0.01).结果发现,AMEA具有较好的抗炎和外周镇痛作用,其抗炎机制可能与TNF-α和IL-1β水平的下调有关.

多花筋骨草在郑州市园林景观中的应用效果初报

为增加郑州市园林地被植物的应用范围,在郑州市开展了多花筋骨草的引种栽培技术研究,结果表明:多花筋骨草在郑州地区可粗放管理,整体表现良好,是一种喜光又耐阴,耐寒、耐热性强,抗性强,繁殖速度快且人工繁殖成活率高的优秀多年生常绿地被植物,观赏效果良好,既可观花又可观叶且花期长,群开效果好,适宜在郑州市园林景观中大量应用。

筋骨草的化学成分研究

目的研究筋骨草A jug a d ecum bens的化学成分。方法采用硅胶柱色谱对筋骨草的甲醇提取浸膏进行分离纯化,得到5个单体,并通过光谱分析鉴定了其结构。结果这5个单体分别被鉴定为1-辛烯-O-α-L-吡喃阿拉伯糖-(1-6)-O-[β-D-吡喃葡萄糖-(1-2)]-β-D-吡喃葡萄糖(Ⅰ)、正丁基-β-D-吡喃果糖苷(Ⅱ)、6,7-二羟基-香豆素(Ⅲ)、5,7-二羟基-4′-甲氧基黄酮(Ⅳ)和谷甾醇-3-O-β-D-吡喃葡萄糖苷(Ⅴ)。结论5个化合物均为首次从该植物中分离得到。

HPLC测定筋骨草中乙酰哈巴苷的含量

目的：建立筋骨草中乙酰哈巴苷的含量测定方法。方法：采用高效液相色谱法。色谱柱：Phenomenex Luna C18（4．6mm×250mm，5μm）；流动相乙腈-水（15：85）；流速1．0mL·min^-1，检测波长197nm。结果：乙酰哈巴苷含量测定的线性范围为0．6-3．6μm（r=0．9993）。平均加样回收率为99．1％，RSD为2．5％。结论：不同产地的筋骨草中乙酰哈巴苷的含量为0．40％。6．39％；本法简便，灵敏准确，可用于筋骨草的质量控制。

筋骨草和茯苓配伍合用抑制乳腺癌细胞侵袭转移作用及初步机制研究

目的研究筋骨草和茯苓联合用药对高转移性乳腺癌MDA-MB-231(三阴型乳腺癌)和SK-BR-3(HER-2过表达乳腺癌)细胞侵袭转移的作用及分子机制。方法以筋骨草有效部位——总环烯醚萜类化合物和茯苓有效部位——三萜类化合物为研究对象。采用细胞黏附实验、细胞划痕和Transwell侵袭实验检测细胞黏附、运动和侵袭能力。Western blot法检测上皮-间质转化(epithelial-mesenchymal transitions,EMT)相关蛋白和MAPK通路蛋白表达。结果筋骨草和茯苓合用对MDA-MB-231和SK-BR-3细胞的黏附、迁移和侵袭能力有明显的抑制作用,配伍比例为10∶1时具有较好的协同效应。两药合用还可逆转乳腺癌细胞EMT,主要表现在上皮性标志物β-catenin、E-cadherin、ZO-1表达增加,间质性标志物Vimentin表达降低。进一步研究发现,两药合用明显降低p-ERK1/2、p-JNK和p-p38的蛋白表达。结论筋骨草和茯苓合用能有效地抑制高转移性乳腺癌MDA-MB-231和SK-BR-3细胞的侵袭和转移,作用机制可能与其调控MAPK通路,逆转肿瘤细胞EMT有关。

齿苞筋骨草的化学成分研究

从齿苞筋骨草 ( Ajuga lupulina var.Major)中分离出 5个化合物。通过光谱数据分析鉴定为 :6-去乙酰筋骨草素 ( 6- deacetyl ajugarin )、香草酸 ( vanillic acid)、木犀草素 ( luteolin)、8-乙酰爪钩草甙 ( 8- acetyl harpagide)和木犀草素 - 7- O-葡萄糖甙( luteolin- 7- O- glucopyranoside)

筋骨草水煎液对急性肺炎的保护作用研究

目的:研究筋骨草水煎液对小鼠急性肺炎的保护作用及机制。方法:用LPS吸入法建立急性肺炎模型,设空白对照组、模型组、筋骨草水煎液组和地塞米松组。观察小鼠肺组织病理,测定肺指数、肺湿/干比,采用酶联免疫吸附试验法检测肺泡灌洗液中肿瘤坏死因子-α、白细胞介素-1β的含量。结果:筋骨草组与模型组比较减轻了急性肺炎小鼠肺组织病变,数据由SPSS 13.0软件分析,小鼠肺指数、肺湿干比明显降低,差异显著(P<0.05),降低肺泡灌洗液中TNF-α、IL-1β的含量,差异显著(P<0.05)。结论:筋骨草水煎液有一定的抗炎作用,可以缓解小鼠急性肺炎症状,其机制可能与降低TNF-α、IL-1β的含量有关。