Dehydroandrographolide succinate
(Synonyms: 脱水穿心莲内酯琥珀酸半酯) 目录号 : GC35830
Dehydroandrographolide succinate (DAS), extracted from herbal medicine Andrographis paniculata (Burm f) Nees, has antibacterial and antiviral effects.
Cas No.:786593-06-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Dehydroandrographolide succinate (DAS), extracted from herbal medicine Andrographis paniculata (Burm f) Nees, has antibacterial and antiviral effects.
| Cas No. | 786593-06-4 | SDF | |
| 别名 | 脱水穿心莲内酯琥珀酸半酯 | ||
| Canonical SMILES | O=C(OC[C@]1(C)[C@H](OC(CCC(O)=O)=O)CC[C@@]2(C)[C@H](/C=C/C3=CCOC3=O)C(CC[C@]12[H])=C)CCC(O)=O | ||
| 分子式 | C28H36O10 | 分子量 | 532.58 |
| 溶解度 | DMSO: 250 mg/mL (469.41 mM) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8777 mL | 9.3883 mL | 18.7765 mL |
| 5 mM | 0.3755 mL | 1.8777 mL | 3.7553 mL |
| 10 mM | 0.1878 mL | 0.9388 mL | 1.8777 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Potassium Dehydroandrographolide succinate injection for treat- ment of infantile pneumonia: a systematic review and Meta-analysis
J Tradit Chin Med 2015 Apr;35(2):125-33.PMID:25975044DOI:10.1016/s0254-6272(15)30019-4.
Objective: To evaluate systematically the clinical efficacy and safety of potassium Dehydroandrographolide succinate injection (PDS) in treatment of infantile pneumonia. Methods: Randomized controlled trials (RCTs) of infantile pneumonia treated by PDS were searched in China National Knowledge Infrastructure Database, China Science and Technology Journal Database, Wanfang Database, Chinese Biomedical Literature Database, PubMed, and Cochrane Library, from January 1979 to July 2013. Two reviewers independently retrieved the RCTs and extracted the information. The quality of included studies was assessed by the Cochrane risk of bias, and a Meta-analysis was conducted with Review Manager 5.2 software. Results: A total of 9 studies with 1056 participants were included. The quality of the studies was generally no high, only one study mentioned the random method. The Meta-analysis indicated that PDS was significantly superior to the conventional therapy in the total effective rate [relative risk (RR) = 1.21, 95% CI (1.14, 1.27), P < 0.000 01], the time of temperature recovery [mean difference (MD) = -1.43, 95% CI (-1.75, -1.11), P < 0.000 01], rale disappeared and cough relieving [MD = -1.44, 95% CI (-1.93, -0.90), P < 0.000 01]. Six adverse drug reactions from five studies mainly represented rash and diarrhea, and no serious ADRs were reported. Conclusion: Based on this systematic review, PDS was proved effective and relatively safe in treatment of infantile pneumonia. However the articles enrolled in the study were not high in quality, studies with higher quality should be conducted for assessment of efficacy and safety of PDS in treatment of infantile pneumonia.
Potassium Dehydroandrographolide succinate Injection for the treatment of child epidemic parotitis: A systematic review and meta-analysis
Chin J Integr Med 2015 Nov;21(11):866-73.PMID:25491538DOI:10.1007/s11655-014-1895-2.
Objective: To systematically evaluate the clinical efficacy and safety of Potassium Dehydroandrographolide succinate Injection (PDSI) in the treatment of child epidemic parotitis (EP). Methods: Randomized controlled trials (RCTs) regarding PDSI in the treatment of child EP were searched in China National Knowledge Infrastructure, Wanfang Database, Chinese Biomedical Literature Database, PubMed, and Cochrane Library from inception to July 30, 2013. Two reviewers independently retrieved RCTs and extracted information. The Cochrane risk of bias method was used to assess the quality of included studies, and a meta-analysis was conducted with RevMan 5.2 software. Results: A total of 11 studies with 818 participants were included. The quality of the studies was generally low, among which only one study mentioned the random method. The meta-analysis indicated that PDSI was more effective than the conventional therapy with Western medicine for EP in the outcomes of the total effective rate [relative risk (RR)=1.23, 95% confidence interval (CI) [1.14, 1.33], P<0.01], the time of temperature return to normal, the time of detumescence [mean difference (MD)=-2.10, 95% CI [-2.78,-1.41], P<0.01], and the incidence of complications (RR=0.14, 95% CI [0.03, 0.72], P=0.02). There were 6 adverse drug reactions (ADRs) in this systematic review, 2 of which were mainly represented rash and diarrhea in the experiment group, while another 4 ADRs occurred in the control group. Conclusions: Based on the systematic review, PDSI was effectiveness and relatively safety in the treatment of child EP. But further rigorously designed trials are warranted to determine its effectiveness.
The antithrombosis effect of Dehydroandrographolide succinate: in vitro and in vivo studies
Pharm Biol 2022 Dec;60(1):175-184.PMID:35014931DOI:10.1080/13880209.2021.2021948.
Context: Dehydroandrographolide succinate (DAS) is mainly used in the clinical treatment of various infectious diseases. Its potential effects on platelet aggregation and blood coagulation systems have not been reported systematically. Objective: To explore whether DAS exerts an antithrombotic effect and its internal mechanism. Materials and methods: Human blood samples and Sprague-Dawley (SD) rats divided into control, aspirin (30 mg/kg), and DAS groups (200, 400 and 600 mg/kg) were used to measure the platelet aggregation rate, coagulation function, coagulation factor activity, and contents of thromboxane B2 (TXB2) and 6-keto-prostaglandin F1α (6-keto-PGF1α). The histopathology of the SD rat gastric mucosa was also observed. All rats were administered intragastric or intraperitoneal injections once a day for 3 consecutive days. Results: Compared to control group, DAS significantly inhibited the platelet aggregation rate (ED50 = 386.9 mg/kg) by decreasing TXB2 levels (1531.95 ± 649.90 pg/mL to 511.08 ± 411.82 pg/mL) and activating antithrombin III (AT-III) (103.22 ± 16.22% to 146.46 ± 8.96%) (p < 0.05). In addition, DAS significantly enhanced the coagulation factors FV (304.12 ± 79.65% to 443.44 ± 75.04%), FVII (324.19 ± 48.03% to 790.66 ± 225.56%), FVIII (524.79 ± 115.47% to 679.92 ± 143.34%), FX (34.90 ± 7.40% to 102.76 ± 29.41%) and FXI (38.12 ± 10.33% to 65.47 ± 34.08%), increased the content of Fg (2.18 ± 0.39 to 3.61 ± 0.37 g/L), shorten the PT (10.42 ± 0.44 to 9.22 ± 0.21 s), APTT (16.43 ± 1.4 to 14.07 ± 0.75 s) and TT time (37.04 ± 2.13 to 32.68 ± 1.29 s) (p < 0.05), while the aspirin group showed no such effect on these items but showed reduced activity of FII (89.21 ± 21.72% to 61.83 ± 8.95%) and FVIII (524.79 ± 115.47% to 306.60 ± 29.96%) (p < 0.05). Histopathological changes showed aspirin-induced gastric mucosa haemorrhage and the protective effect of DAS in the gastric mucosa. Conclusions: DAS is more suitable than aspirin in thromboprophylaxis treatment, which provides a reliable theoretical and experimental basis for its clinical application.
Comparison of pulmonary availability and anti-inflammatory effect of Dehydroandrographolide succinate via intratracheal and intravenous administration
Eur J Pharm Sci 2020 Apr 30;147:105290.PMID:32135270DOI:10.1016/j.ejps.2020.105290.
Dehydroandrographolide succinate (DAS) injection, which was approved in China for the treatment of viral pneumonia and upper respiratory tract infections, is often off-label used for nebulization therapy to avoid the adverse drug reactions associated with the injection. However, the aerodynamic properties and pulmonary fate of nebulized DAS was largely uninvestigated. In this study, the main objectives were to evaluate the in vitro aerodynamic deposition profiles of nebulizer generated aerosols and comparatively investigate the local drug availability and anti-inflammatory efficacy of DAS between intratracheal and intravenous dosing. The in vitro evaluation of aerodynamic characteristics and droplet size distribution showed more than 50% aerosol particles with size being <5 μm, allowing the aerosols to reach the lower respiratory tract. Following intratracheal administration, the drug underwent pulmonary absorption into the bloodstream, rendering an absolute bioavailability of 47.3%. Compared to the intravenous delivery, the intratracheal administration dramatically increased the drug availability in the lung tissue in rats by more than 80-fold, leading to an improved and prolonged local anti-inflammatory efficacy in a lipopolysaccharide induced lung injury model in mice. The present results demonstrated that inhalation delivery of DAS is a convenient and effective alternative to intravenous injections.
Pharmacokinetics and tolerance of Dehydroandrographolide succinate injection after intravenous administration in healthy Chinese volunteers
Acta Pharmacol Sin 2012 Oct;33(10):1332-6.PMID:22902987DOI:10.1038/aps.2012.79.
Aim: Dehydroandrographolide succinate (DAS) is extracted from herbal medicine Andrographis paniculata (Burm f) Nees. DAS injection is used in China for the treatment of viral pneumonia and upper respiratory tract infections. The aim of this study is to investigate the pharmacokinetics and tolerance of DAS injection in healthy Chinese volunteers. Methods: This was a single-center, randomized, single-dose, three-way crossover design study. Nine eligible subjects were randomly divided into 3 groups, and each group sequentially received 80, 160, or 320 mg of DAS infusion according to a three-way Latin square design. Plasma and urine samples were collected and determined using an LC-MS/MS method. Safety and tolerability were determined via clinical evaluation and adverse event monitoring. Results: For the 80, 160, and 320 mg dose groups, the mean C(max) were 4.82, 12.85, and 26.90 mg/L, respectively, and the mean AUC(0-12) were 6.18, 16.95, and 40.65 mg·L(-1)·h, respectively. DAS was rapidly cleared, with a mean T(max) of 0.94-1.0 h and a t(1/2) of approximately 1.51-1.89 h. Approximately 10.1%-15.5% of the intravenous DAS dose was excreted unchanged in urine within 24 h in the 3 groups, and more than 90% of unchanged DAS was excreted between 0 and 4 h. The pharmacokinetic profile was similar between male and female subjects. No serious or unexpected adverse events were found during the study, but one mild adverse event (stomachache) was reported. Conclusion: This study shows that DAS has nonlinear pharmacokinetic characteristics. To guarantee the effective concentration, mul¬tiple small doses are recommended in clinical regimens.