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1.
2.

Aim of the study

To investigate the antihypertensive fractions of Eucommia ulmoides Oliv. and their underlying mechanisms in spontaneously hypertensive rats (SHRs).

Materials and methods

In vivo study, Eucommia ulmoides lignans (EuL) and Eucommia ulmoides iridoids (EuI) were administrated to Sprague–Dawley (SD) rats and SHRs, and their blood pressures were measured. Plasma level of nitric oxide (NO) was measured by colorimetric method, and renin activity (RA) and plasma concentration of angiotensin II (Ang II) were measured by radioimmunoassay. In vitro study, rat mesenteric artery was treated with EuL and the vessel relaxation responses were determined.

Results

EuL could lower blood pressures of both SD rats and SHR dose-dependently by either intravenous (i.v.) or intragastric (i.g.) administration, but EuI failed to affect blood pressure in the two kinds of rats. Meanwhile, no synergistic effect was observed with the combination of EuL and EuI. The plasma level of NO in SHR treated with EuL 300 mg/kg twice a day was markedly increased. Both plasma RA and Ang II level were decreased with long-term oral treatment of EuL 150 and 300 mg/kg twice a day. In perfusion experiment, EuL relaxed mesenteric artery quickly and dose-dependently and the effect on the artery with and without endothelium was the same.

Conclusions

EuL may be the effective fraction to lowering blood pressure and its antihypertensive effect is probably associated with regulating NO and renin–angiotensin system (RAS) and directly relaxing artery.  相似文献   

3.
杜仲皮、杜仲叶和杜仲雄花均来源于杜仲,三者在成分构成、药理作用方面的差异尚不明确。然而阐明杜仲不同部位的作用功效差异对于杜仲产品的开发具有重大的意义,而这种差异功效对应的物质基础也为不同部位的质量控制提供了依据。为了探讨杜仲不同部位的作用功效差异,该研究以不同部位的化学成分为研究对象,采用化合物靶标预测和靶标分析的策略,探讨杜仲(皮)、杜仲叶和杜仲花在药理作用方面的差异。其次为了阐明导致不同部位功效差异的物质基础,该研究通过构建"成分-靶标-功能"的关联网络,挖掘特异性功效对应的不同部位特异性成分,探讨导致功效差异的物质基础。根据靶标预测以及功能分析,杜仲可能的药理作用集中在抗氧化、神经调控、血压调控、心肌收缩、抗凋亡等。而杜仲的不同部位作用存在差异,杜仲叶特异性地参与成骨细胞分化、骨矿化等涉及骨发育的过程,此外还可能通过调控维生素D的代谢影响钙的吸收进而影响骨发育等过程。杜仲叶还可能特异性地作用于雌激素受体参与的雌激素及雌二醇的应答等过程。而关于肝脏的保护功能,杜仲叶可能通过调控维生素A相关的通路来发挥作用。相较于杜仲叶而言,杜仲(皮)特异性的药理作用可能是与泌尿系统的发育相关。杜仲雄花特异性参与疼痛的感受、谷氨酸信号通路以及兴奋性突出后电位等过程有关的功能。基于"成分-靶点-通路"的层次网络发现,杜仲不同部位特异性的功效与其特异性的化学成分密切相关,其中杜仲叶中特有的苯丙素类、萜类、环烯醚萜类、黄酮类及其他类成分靶向作用于杜仲叶特异性的功能,而杜仲(皮)中的黄酮类成分以及杜仲花中的萜类成分则可能是发挥它们特异性功效的物质基础。该研究中针对于杜仲不同部位的作用预测为后续杜仲产品开发的侧重点和差异性提供了新的依据;同时基于差异化功效的物质基础研究也为杜仲差异化产品的质量控制提供了依据。  相似文献   

4.
该研究采用正相硅胶柱色谱,反相柱色谱(RP-18),凝胶色谱(Sephadex LH-20)以及重结晶等多种分离纯化手段,从杜仲雄花中分离得到9个化合物,通过化合物的理化性质和光谱数据鉴定其结构分别为:3-oxo-12-en-ursane-28-O-α-Larabinofuranosyl(1→6)-β-D-glucopyranoside(1),2α,3β-dihydroxyurs-12-en-28-oic acid(28→1)-β-D-glucopyranosyl ester(2),熊果酸(3),α-香树脂醇(4),熊果醇(5),3-O-乙酰基熊果酸乙酸酯(6),3-O-乙酰基齐墩果酸(7),白桦脂酸(8),白桦脂醇(9)。其中化合物1为新化合物,化合物2,4~7为首次从该科植物中分离得到。采用MTT法对所分离的9个化合物进行抗肿瘤活性测试,结果表明仅有化合物3对K562和Hep G2细胞显示出一定的抗肿瘤活性,其余化合物对所选的2种细胞均无明显活性。  相似文献   

5.

Ethnopharmacological relevance

The present study systematically investigate the in vivo and in vitro effect of total lignans (TL) extracted from Eucommia ulmoides Oliv. barks on bone formation using ovariectomy rat model and primary cultures of rat osteoblasts.

Materials and methods

Eighty 3-month-old female Sprague-Dawley rats were used and randomly assigned into sham-operated group (SHAM) and five ovariectomy (OVX) subgroups, i.e. OVX with vehicle (OVX); OVX with 17α-ethinylestradiol (E2, 25 μg/kg/day); OVX with TL of graded doses (20, 40, or 80 mg/kg/day). The treatment began 4 weeks after the surgery and lasted for 16 weeks. in vitro experiments were performed to determine the potential mechanisms of the anti-osteoporotic effect of TL.

Results

Treatment with TL significantly prevent OVX-induced decrease in biomechanical quality of femur such as maximum stress and Young?s modulus. The mechanical changes were associated with the prevention of a further BMD decrease or even with some improvements in microarchitecture. TL inhibited BMD decrease in the femur caused by OVX, which was accompanied by a significant decrease in skeletal remodeling, as was evidenced by the decreased levels of the bone turnover markers. μCT analysis of the femoral metaphysis showed how to prevent the deterioration of trabecular microarchitecture. TL induced primary osteoblastic cell proliferation and differentiation, inhibition of osteoclastogenesis through an increase in osteoprotegrin (OPG) and a decrease in NF-κB ligand (RANKL) expression in vitro.

Conclusions

We concluded that TL treatment can effectively suppress the loss of bone mass induced by OVX and in vitro evidence suggests this could be through actions on both osteoblasts and osteoclasts.  相似文献   

6.
杜仲叶中绿原酸的提取纯化研究   总被引:4,自引:0,他引:4  
目的研究杜仲叶中绿原酸的提取纯化方法。方法采用水提、絮凝脱色、树脂吸附、重结晶工艺提取纯化。结果杜仲叶的水浸提液浓缩后用1%壳聚糖絮凝去杂、活性碳脱色得到进样液,进样液用NKA-9树脂吸附,50%乙醇解吸,洗脱液浓缩后的粗品经甲醇重结晶得到纯度≥97%的绿原酸,提取率≥65%。结论优化完善了杜仲叶中绿原酸的提取纯化方法,为杜仲资源的充分综合利用和产业化开发提供了参考。  相似文献   

7.
杜仲叶来源于杜仲科植物杜仲Eucommia ulmoides的干燥叶。为了深入了解杜仲叶中的活性成分,该研究采用D-101大孔树脂,MCI树脂,反相ODS,Sephadex LH-20,Rp-HPLC制备柱色谱法和重结晶等方法,从杜仲叶乙醇提取物的正丁醇萃取部位中分离得到10个化合物,通过MS和NMR等谱学方法,鉴定结构为山柰素-3-O-β-D-葡萄糖苷(1),槲皮素-3-O-β-D-葡萄糖苷(2),槲皮素(3),槲皮素-3-O-β-D-木糖基-(1→2)-β-D-葡萄糖苷(4),山柰酚-3-O-α-L-鼠李糖基-(1→6)-β-D-葡萄糖苷(5),(2S,3S)-(-)-花旗松素-3-O-β-D-葡萄糖苷(6),4-羟基肉桂酸(7),(+)-环橄榄脂素(8),松脂素-β-D-葡萄糖苷(9),角鲨烯(10),其中化合物1,5~7,10为首次从该属植物中分离得到。采用DPPH自由基清除法对分离得到的化合物进行抗氧化活性研究。结果显示,其中化合物 2 表现出显著的自由基清除能力(IC50为13.7 μmol·L-1),活性强于Vit C(IC50为59.9 μmol·L-1);化合物1,3,9显示中等强度自由基清除能力(IC50分别为161,137,214 μmol·L-1),活性弱于Vit C,但强于2,6-二羟丁基对甲酚(IC50为236 μmol·L-1);化合物4,6自由基清除能力较弱(IC50分别为264,299 μmol·L-1);提示杜仲的药理作用,可能与其黄酮和木脂素类化学成分具有能够体内清除体内活性氧及抗氧化成分有关。  相似文献   

8.
目的:研究杜仲抗紫外线致ESF-1细胞光老化作用,并初步探讨其作用机制。方法:杜仲70%乙醇提取物上D101大孔树脂制备不同浓度乙醇梯度洗脱部位,采用40 J.cm-2的UVA或70 mJ.cm-2的UVB照射ESF-1细胞后,立即加入不同浓度的杜仲50%乙醇洗脱部位,24 h后MTT法测定细胞活性,试剂盒法测定细胞培养液中乳酸脱氢酶(LDH)、超氧化歧化酶(SOD)活力及丙二醛(MDA)含量。结果:杜仲50%乙醇大孔树脂洗脱部位250,500 mg.L-1的给药浓度能使UVA诱导的光老化细胞活性明显增强(P<0.05),细胞培养液中LDH活力明显降低(P<0.05),其中250 mg.L-1的给药浓度能使细胞培养液中SOD活力明显升高(P<0.05),MDA含量明显降低(P<0.05);125,250,500 mg.L-1的给药浓度能使UVB诱导的光老化细胞活性明显增强,其中125 mg.L-1的给药浓度能使细胞培养液中LDH活力明显降低(P<0.05),SOD活力明显升高(P<0.05),MDA含量明显降低(P<0.05)。结论:杜仲50%乙醇大孔树脂洗脱部位对UVA和UVB致ESF-1细胞光老化具有良好的保护作用,推测其机制为通过提高SOD活力、加速氧自由基的清除和减少氧自由基的产生,使细胞的脂质过氧化损伤程度降低;同时,可能通过抗氧化作用,维持了细胞膜结构和功能的完整性,使LDH的漏出减少。  相似文献   

9.
杜仲对成骨样细胞增殖的作用   总被引:11,自引:0,他引:11  
杜仲的水提液及水提液的不同萃取物和UMR106成骨样细胞体外共同培养,用MTT法检测细胞增殖,结果水提液在0.4mg/ml培养48小时具有最强的促进细胞增殖作用,其乙酸乙酯萃取物和正丁醇萃取物对细胞增殖有一定促进作用,但无显著性差异,而乙酸乙酯和正丁醇萃取后的剩余水层仍保留与原水提液相似的促进细胞增殖作用。表明杜仲中极性大部位可能含有直接作用于成骨细胞的活性成分。  相似文献   

10.
基于系统药理学的厚朴药理作用机制探究   总被引:1,自引:0,他引:1  
王艳艳  王团结  丁琳琳 《中草药》2019,50(24):6024-6031
目的 运用系统药理学的方法探究中药厚朴的药理作用机制。方法 以中药成分数据库和大量文献检索,建立厚朴成分数据库。运用ADME筛选厚朴的活性成分,并利用数据库和内部软件进行靶点的识别。最后通过网络分析和通路分析等系统药理学方法对厚朴药理作用机制进行分析。结果 建立厚朴成分数据库,共包含144种厚朴活性成分。经过活性成分的筛选,得到7个满足筛选条件的厚朴活性成分,并且识别出54个相互作用靶点。经过网络分析,发现这些靶点主要与肠动力、炎症、糖尿病和血栓疾病相关。通过通路分析,发现厚朴的靶点共涉及152条生物通路,且这些通路涉及除了上述疾病外,还参与到癌症的相关机制。结论 本研究不仅运用系统药理学的方法揭示了厚朴对肠动力、炎症、糖尿病、血栓和癌症的药理机制,还体现出厚朴"多成分-多靶点-多通路"的典型中药特点,更为今后探究中药药理作用机制供了一个新的思路。  相似文献   

11.
不同采收期杜仲叶和果实中总黄酮和多糖含量比较   总被引:1,自引:1,他引:1  
目的:明确杜仲叶和果实中的总黄酮和总多糖的含量,为杜仲叶和果实的最佳采收期的确定以及开发提供科学的依据。方法:不同采收期杜仲叶和果实,分别用70%乙醇加热回流提取3次,紫外分光光度法(506 nm)对其总黄酮的含量进行测定,进行系统的分析统计,得出总黄酮含量最高的月份。不同采收期杜仲叶和果实,分别用水加热回流提取3次,用苯酚-硫酸显色,用紫外分光光度法(481 nm)对其总多糖的含量进行测定,进行系统的分析统计,得出总多糖含量最高的月份。结果:紫外分光度法测得不同季节的杜仲叶和果实中总黄酮和总多糖的含量有显著差异,叶和果实中总黄酮含量以4月份为最高。叶和果实中总多糖含量均以3月份为最高,但是果实中总多糖的含量在6月份会达到最低,7月份又有显著回升;而叶的这个过程不明显,5月份后总多糖含量一直缓慢下降。结论:杜仲叶和果实中的总黄酮和总多糖的含量均比较高,其最佳采收期均为4月份。  相似文献   

12.

Ethnopharmacological relevance:

Abelmoschus manihot (L.) Medik. var. manihot is one of the most commonly used Chinese medicines and has played an important role in treating chronic glomerulonephritis and diabetic nephropathy.

Aim of the study:

Metabolites identification of traditional Chinese medicine (TCM) is a complex and time-consuming process due to the complicity of TCM and subsequent large number of detected ions. In this paper, UPLC–MS combined with pattern recognition analysis approach were used to simplify and quicken the identification of the metabolites of Abelmoschus Manihot.

Materials and methods:

Rat urine samples were collected before (as control sample) and after Abelmoschus Manihot administration. Pattern recognition analysis method was used to differentiate components between Abelmoschus Manihot-treated group and its controlled comparison. These components could be considered as Abelmoschus Manihot-related metabolites in vivo.

Results:

LC–MS based metabolomics could be an advanced tool to help us find metabolites with regards to its capacity of processing large datasets, differentiating and classifying of sample groups, as well as its indiscriminative nature of biomarker and metabolite identification. Using this method, seven metabolites were identified, which are flavonoid aglycone glucuronidation, sulfatation, and methylation metabolites.

Conclusion:

Our results showed that UPLC–MS based- pattern recognition analysis approach can be used to quickly identify Abelmoschus Manihot related metabolites in biological fluids. Furthermore, this work demonstrates the potential application of combining the UPLC–MS approach with the metabolomics approach in identifying the metabolites of TCM.  相似文献   

13.

Aim of the study

Eucommia ulmoides Oliv. leaf is a traditional Chinese medicine that exhibits an anti-diabetic action. This study was designed to investigate whether long-term administration of Eucommia ulmoides Oliv. leaves extract (ELE) ameliorates pre-diabetic state of insulin resistance and abnormal perivascular innervation in the hyperinsulinemic state.

Materials and methods

ELE at doses of 500 and 1000 mg/kg was administered orally once daily for 4 weeks in fructose-drinking rats (FDRs). Plasma levels of insulin, blood glucose levels, and perivascular innervation were assessed using biochemical and immunohistochemical methods.

Results

FDR showed significant increase in plasma levels of insulin, an index for insulin resistance (Homeostasis Model Assessment ratio—HOMA-IR) and systolic blood pressure (SBP), but not blood glucose levels, as compared with control rats. Immunohistochemical study showed significantly greater density of tyrosine hydroxylase (TH)-like immunoreactivity (LI)-containing nerves and significantly lower density of calcitonin gene-related peptide (CGRP)-LI-containing nerves in mesenteric arteries of FDR than those in control. A 4-week treatment with ELE (500 and 1000 mg/kg, p.o.) significantly decreased plasma levels of insulin and HOMA-IR without affecting blood glucose levels and significantly lowered SBP in FDR. ELE treatment in FDR resulted in significant increase in CGRP-LI never fiber density and significant decrease in TH-LI never fiber density in mesenteric arteries of FDR.

Conclusions

These results suggest that long-term ELE treatment effectively prevents insulin resistance development and ameliorates abnormal perivascular innervation in FDR.  相似文献   

14.

Aim of the study

To investigate the effects of lignans extracted from Eucommia ulmoides and epalrestat on vascular remodeling in spontaneously hypertensive rats.

Materials and methods

Ten-week-old male spontaneously hypertensive rats were randomly divided into 3 groups (12 rats each group), and treated orally with 100 mg/kg/d of captopril (an angiotensin-converting enzyme inhibitor), 100 mg/kg/d of epalrestat (an aldose reductase inhibitor) and 300 mg/kg/d of lignans by gavage daily for 16 weeks, respectively. Sex-, age-, and number-matched spontaneously hypertensive rats and normotensive Wistar Kyoto rats, were treated with distilled water (vehicle) as controls. The rats were weighed weekly. Mean arterial blood pressure and heart rate were measured periodically by non-invasive blood pressure monitoring. They were sacrificed at the end of experiment (26-week-old). Superior mesenteric artery and aorta were isolated for determination of histomorphometry and the expression of aldose reductase by immunohistochemistry.

Results

Captopril and lignans, but not epalrestat, decreased mean arterial blood pressure in spontaneously hypertensive rats. Vascular remodeling was improved in all three treated groups by histomorphometry.

Conclusions

Both lignans and epalrestat reversed hypertensive vascular remodeling. Aldose reductase played a vital role in the pathologic process of hypertensive vascular remodeling rather than elevation of blood pressure. These data suggested that aldose reductase could be a new therapeutic target for the treatment of cardiovascular diseases.  相似文献   

15.
为准确鉴定柴胡与大叶柴胡,该研究共48份柴胡、大叶柴胡药材,扩增ITS2 序列并进行测序,采用CodonCode Aligner软件进行序列拼接,用软件MEGA5.0分析比对确定不同的单倍型,并基于K2P模型进行遗传距离等分析。采用相似性搜索法、最近距离法、构建邻接树(NJ树)法对柴胡与大叶柴胡进行鉴定。结果显示柴胡与大叶柴胡种间最小K2P距离为0.049,远远大于柴胡种内最大K2P距离0.013。NJ树显示大叶柴胡独自聚为一支,可明显与柴胡区分。因此应用ITS2条形码可以准确鉴定柴胡及大叶柴胡。  相似文献   

16.
白贞芳  刘勇  王晓琴 《中国中药杂志》2014,39(23):4548-4552
通过野外资源调查、整理各大标本馆标本原始记录和查阅文献记载等方法,系统整理、总结、归纳了列当属、肉苁蓉属和草苁蓉属民族药用植物种类、功效及民间使用情况,结果表明列当属6种药用植物在4个少数民族间作为7种民族药应用,草苁蓉属2种药用植物在8个少数民族间作为10种民族药应用,肉苁蓉属2种药用植物在3个少数民族间作为3种民族药应用,且同种药用植物常作不同民族药;发现3属植物的传统疗效主要集中在补肾壮阳、止血和止痛3个方面,并且该传统疗效与现代药理研究结果基本吻合。因此深入研究植物种类丰富的列当属植物资源对缓解肉苁蓉植物资源匮乏局面和扩大药源具有积极意义。  相似文献   

17.
目的:采用网络药理学-分子对接预测杜仲叶防治骨质疏松症的作用机制。方法:利用中药系统药理学数据库与分析平台(TCMSP)及SwissTargetPrediction分析平台对杜仲叶活性成分及作用靶点进行筛选,使用GeneCards、在线人类孟德尔遗传(OMIM)数据库、治疗靶点数据库(TTD)对骨质疏松症的对应靶标进行筛选,将中药靶基因与疾病靶基因相交集,将交集靶点导入Cytoscape软件构建成分靶点网络,使用STRING分析平台及Cytoscape软件构建蛋白质-蛋白质相互作用(PPI)网络,筛选核心靶点。对中药-疾病共同靶标进行基因本体(GO)功能富集分析和京都基因和基因组百科全书(KEGG)功能富集分析,得出中药-疾病共同靶标相关的信号通路,最后运用AutoDock与Pymol软件对预测靶标与其对应的成分进行分子对接。结果:筛选后得到杜仲叶治疗防治骨质疏松症的有效成分7个,杜仲叶-骨质疏松症共同靶标231个,并推断其作用机制可能与动脉粥样硬化信号通路的下游核因子κB信号通路,MAPK信号通路、TNF、PI3K-AKT、IL-17及HIF-1信号通路等有关,且MAPK1、STAT...  相似文献   

18.
追风伞中黄酮类成分的研究   总被引:2,自引:1,他引:2  
目的:对追风伞中的黄酮类成分进行分离、鉴定。方法:追风伞干燥全草用95%乙醇溶液加热回流提取,减压回收乙醇,浓缩液依次用石油醚、氯仿萃取后,水层部分利用大孔吸附树脂、硅胶柱色谱、反相Rp-18柱色谱及重结晶等方法进行分离及纯化,并通过1H-NMR,13C-NMR,EI-MS及理化常数对分离化合物进行结构鉴定。结果:从追风伞提取物中分离鉴定9个黄酮类化合物,分别为:木犀草素(1),木犀草素-4′-O-β-D-葡萄糖苷(2),刺槐素-7-O-β-D-葡萄糖苷(3),芦丁(4),刺槐素(5),槲皮素(6),槲皮素-3-O-β-D-葡萄糖苷(7),山柰酚-3-O-β-D-葡萄糖苷(8),异鼠李素-3-O-β-D-葡萄糖苷(9)。结论:所得化合物均为首次从追风伞中分离鉴定。  相似文献   

19.
甘遂为有毒中药,临床上常经醋制后入药以降低其毒性。该文采用代谢组学方法比较生甘遂和醋甘遂对正常大鼠的损伤情况,研究醋制对甘遂毒性的缓解作用。连续7 d以生甘遂(EK)、醋甘遂(VEK)的水提取物对大鼠灌胃给药,药量均为9 g·kg-1·d-1(按生药量计),对照组给予生理盐水。停止灌胃后继续观察7 d,收集14 d白天尿液,用于1H-NMR检测;于第8天将每组大鼠处死一半,第15天处死另一半,采集肝脏,一部分用于1H-NMR检测,另一部分用于病理学切片检测。病理学切片检测结果显示在本实验剂量下甘遂及醋制甘遂对大鼠肝脏没有造成损伤,但代谢组学方法分析发现在实验的第2周甘遂造成大鼠肝、肾及消化系统内部内源性代谢产物谱的紊乱;同时发现醋甘遂的毒性要比生甘遂低得多,传统醋制可以降低甘遂的毒性。该研究显示代谢组学方法有助于评价甘遂的毒性及醋制对甘遂的解毒作用。  相似文献   

20.

Ethnopharmacological relevance

Scientific validation of ethnopharmacologically used plants and their utilization for therapeutic interventions can be a source of affordable treatment especially for neglected diseases in endemic areas. Conyza sumatrensis is a plant which finds its use in treating malaria like fevers but lacks proper scientific validation. Our study has tried to address this gap by authenticating its traditional use for the treatment of malaria.

Aim of the study

Evaluate the antimalarial activity of extracts derived from Conyza sumatrensis for its ethnopharmacological validation.

Materials and methods

Shade dried leaves were extracted with varying concentrations of ethanol and concentrated for bio-evaluation. Swiss albino mice infected with 1×106 parasitized red blood cells, were orally administered with test extracts for 7 days in two sets of experiments. The first set was used to evaluate alcoholic, hydroalcoholic and aqueous extracts while the second set was used to evaluate the dose response of alcoholic extract ranging from 500–1600 mg/kg. Mean survival time, parasitaemia and haemoglobin levels were considered to interpret the antimalarial potential. Phytochemical analysis for the presence of flavonoids, alkaloids tannins, total phenolics, riboflavin and thiamine was also carried out.

Results

Among the three extracts administered at 1000 mg/kg, chemo suppression was significantly (p<0.001) observed in the alcoholic extract (62.59±12.52%) followed by hydroalcoholic (41.81±19.04%, p<0.01) and aqueous (32.04±19.04%, P<0.05) indicating that the active constituents leach out in ethanol. The dose response study involving the ethanol extract concluded the optimum dose to be 1000 mg/kg, as also evidenced by the haemoglobin levels.

Conclusion

The plant exhibits moderate antimalarial activity which can be further prospected for active fractions or pure molecules for adjunctive therapy.  相似文献   

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