Continentalic acid
(Synonyms: 长白楤木酸) 目录号 : GC35729
A diterpenic acid with diverse biological activities
Cas No.:19889-23-7
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
Continentalic acid is a diterpenic acid that has been found in A. continentalis and has diverse biological activities.1,2,3,4 It is active against methicillin-susceptible S. aureus (MSSA) and clinical isolates of methicillin-resistant S. aureus (MRSA; MICs = 8 and 8-16 ?g/ml, respectively).1 Continentalic acid (200 ?M) induces apoptosis in U-2932, OCI-LY1, and Ramos (RA 1) B cell lymphoma cells.2 In vivo, continentalic acid (50 mg/kg) decreases blood glucose levels, total body weight, and serum triglyceride, total cholesterol, and LDL levels, as well as increases serum HDL levels in a rat model of diabetes induced by alloxan .3 It also improves renal function and decreases renal malondialdehyde (MDA) and peroxidase levels, nitric oxide (NO) production, and neutrophil infiltration in a mouse model of E. coli- and LPS-induced renal injury.4
1.Jeong, S.-I., Han, W.-S., Yun, Y.-H., et al.Continentalic acid from Aralia continentalis shows activity against methicillin-resistant Staphylococcus aureusPhytother. Res.20(6)511-514(2006) 2.Jeon, B.-E., Kwon, C.-S., Lee, J.-E., et al.Anticancer activity of continentalic acid in B-cell lymphomaMolecules26(22)6845(2021) 3.Liaquat, I., Khan, A.-U., and Khan, S.Pharmacological evaluation of continentalic acid for antidiabetic potentialBiomed. Pharmacother.138111411(2021) 4.Khan, A.M., Khan, A.U., Ali, H., et al.Continentalic acid exhibited nephroprotective activity against the LPS and E. coli-induced kidney injury through inhibition of the oxidative stress and inflammationInt. Immunopharmacol.80106209(2020)
| Cas No. | 19889-23-7 | SDF | |
| 别名 | 长白楤木酸 | ||
| Canonical SMILES | C[C@]12[C@@](CCC3=C[C@](C=C)(C)CC[C@@]23[H])([H])[C@@](C)(CCC1)C(O)=O | ||
| 分子式 | C20H30O2 | 分子量 | 302.45 |
| 溶解度 | DMSO : 100 mg/mL (330.63 mM; Need ultrasonic) | 储存条件 | Store at -20°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 | 3.3063 mL | 16.5317 mL | 33.0633 mL |
| 5 mM | 0.6613 mL | 3.3063 mL | 6.6127 mL |
| 10 mM | 0.3306 mL | 1.6532 mL | 3.3063 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。
Pharmacological evaluation of Continentalic acid for antidiabetic potential
Biomed Pharmacother 2021 Jun;138:111411.PMID:33711550DOI:10.1016/j.biopha.2021.111411.
Background: Diabetes is a complex endocrine and metabolic disorder. Continentalic acid is a natural drug product found in roots of Aralia continentalis (family Araliaceae), which used in traditional medicine for treatment of rheumatic arthritis, lumbag, lameness, inflammation, gastritis, nephritis and diabetes mellitus. Purpose: This study is aim to investigate the Continentalic acid anti-diabetic potential. Methods: In-silico, in-vitro, in-vivo and molecular techniques were used to investigate various effects of Continentalic acid by Auto Doc Vina, α-amylase and α-glucosidase inhibitory assay and alloxan-induced diabetes rats model. Results: In-silico results revealed that Continentalic acid exhibits binding energy values of - 5 to - 9.3Kcal/mol against selected targets. In-vitro assay showed that Continentalic acid caused α-amylase and α-glucosidase enzymes inhibition. In-vivo finding exhibits that Continentalic acid (50 mg/kg) decreased blood glucose level, body weight, oral glucose tolerance overload, glycosylated hemoglobin, triglycerides, total cholesterol, low density lipoprotein, aspartate transaminase, aspartate aminotransferase, alkaline phosphate, total bilirubin and increased high density lipoprotein (P < 0.05, P < 0.01, P < 0.001 vs. diabetic control group). In animals pancreas and liver tissues, Continentalic acid enhanced glutathione-s-transferase, reduced glutathione, catalase and decreased lipid hydroperoxide level, improved cellular architecture in histopathological examination and decrease expression of inflammatory markers: cyclooxygenase 2, tumor necrosis factor alpha, phosphorylated-nuclear factor kappa B, prostaglandins E2, interleukin-18 and increased heme oxygenase-1, as evidenced in immunohistochemistry and enzyme-linked immunosorbent assay molecular investigations. Conclusions: This study shows that Continentalic acid exhibited binding affinities against the different targets and anti-diabetic action, mediated possibly through α-amylase and α-glucosidase inhibition, anti-hyperlipidemic, hepatoprotection, antioxidant and anti-inflammatory pathways.
Anticancer Activity of Continentalic acid in B-Cell Lymphoma
Molecules 2021 Nov 12;26(22):6845.PMID:34833935DOI:10.3390/molecules26226845.
Aralia continentalis has been used in Korea as a folk remedy for arthralgia, rheumatism, and inflammation. However, its anti-lymphoma effect remains uncharacterized. Here, we demonstrate that A. continentalis extract and its three diterpenes efficiently kill B-lymphoma cells. Our in vitro and in vivo results suggest that the cytotoxic activities of Continentalic acid, a major diterpene from A. continentalis extract, are specific towards cancer cells while leaving normal murine cells and tissues unharmed. Mechanistically, Continentalic acid represses the expression of pro-survival Bcl-2 family members, such as Mcl-1 and Bcl-xL. It dissociates the mitochondrial membrane potential, leading to the stimulation of effector caspase 3/7 activities and, ultimately, cell death. Intriguingly, this agent therapeutically synergizes with roflumilast, a pan-PDE4 inhibitor that has been successfully repurposed for the treatment of aggressive B-cell malignancies in recent clinical tests. Our findings unveiled that A. continentalis extract and three of the plant's diterpenes exhibit anti-cancer activities. We also demonstrate the synergistic inhibitory effect of Continentalic acid on the survival of B-lymphoma cells when combined with roflumilast. Taken in conjunction, Continentalic acid may hold significant potential for the treatment of B-cell lymphoma.
Continentalic acid Rather Than Kaurenoic Acid Is Responsible for the Anti-Arthritic Activity of Manchurian Spikenard In Vitro and In Vivo
Int J Mol Sci 2019 Nov 4;20(21):5488.PMID:31690022DOI:10.3390/ijms20215488.
The aim of this study was to identify the active compound responsible for the pharmacological activities of Manchurian spikenard (Aralia continentalis Kitag.). Interleukin (IL)-1β-stimulated human chondrocytes and monoiodoacetate (MIA)-induced osteoarthritic rats were treated with the 50% ethanolic extract of spikenard or its major components, such as Continentalic acid (ent-pimara-8(14),15-diene-19-oic acid) and kaurenoic acid (ent-kaura-16-en-19-oic acid). The spikenard extract significantly inhibited IL-1β-stimulated production of IL-6, IL-8, metalloproteinase (MMP)-1, MMP-13, cyclooxygenase (COX)-2, inducible nitric oxide synthase (iNOS) and prostaglandin(PG)E2 in a dose-dependent manner but not MMP-3 production. The extract also inhibited the IL-1β-induced translocation of NF-κB/p65 into the nucleus and dose-dependent phosphorylation levels of extracellular signal-regulated kinase (ERK), Jun amino-terminal kinase (JNK) and p38 mitogen-activated protein (MAP) kinase. Continentalic acid exhibited significant anti-arthritic activity corresponding exactly to that of the extract containing an equivalent amount of Continentalic acid. On the other hand, kaurenoic acid exhibited a compatible activity at about a 10-times higher molar concentration than that of Continentalic acid. In vitro anti-arthritic activities of the spikenard extract and Continentalic acid were also confirmed in MIA-induced osteoarthritic rats. The 50% ethanolic extract of Manchurian spikenard exhibited promising anti-arthritic activities in the in vitro and in vivo osteoarthritis models, and Continentalic acid, not kaurenoic acid, was most probably responsible for those activities.
Continentalic acid from Aralia continentalis shows activity against methicillin-resistant Staphylococcus aureus
Phytother Res 2006 Jun;20(6):511-4.PMID:16619343DOI:10.1002/ptr.1894.
In a continuing search for compounds with antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), a chloroform extract of roots of Aralia continentalis was found to contain Continentalic acid (CA, C(20)H(30)O(2)), a diterpenic acid. This compound exhibited potent activity against standard methicillin-susceptible Staphylococcus aureus (MSSA) as well as clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA). It was determined that Continentalic acid had minimum inhibitory concentrations (MICs) of approximately 8-16 microg/mL against S. aureus, including the MSSA and MRSA standard strains. Therefore, the results obtained in this study suggest that Continentalic acid might have potential as an adjunct in the treatment of antibiotic-resistant bacteria.
Continentalic acid exhibited nephroprotective activity against the LPS and E. coli-induced kidney injury through inhibition of the oxidative stress and inflammation
Int Immunopharmacol 2020 Mar;80:106209.PMID:32004924DOI:10.1016/j.intimp.2020.106209.
The present study investigated the effect of the Continentalic acid (CNT) isolated from the Aralia Continentalis against the LPS and E. coli-induced nephrotoxicity. The LPS and E. coli administration markedly altered the behavioral parameters including spontaneous pain, tail suspension and survival rate. However, the treatment with CNT dose dependently improved the behavioral parameters. The CNT treatment significantly improved the renal functions test (RFTs) and hematological parameters following LPS and E. coli-induced kidney injury. Furthermore, the LPS and E. coli administration markedly compromised the anti-oxidant enzymes and enhanced the oxidative stress markers. However, the CNT treatment markedly enhanced the anti-oxidants enzymes such as GSH, GST, Catalase and SOD, while attenuated the oxidative stress markers such as MDA and POD. The MPO enzyme is widely used marker for the neutrophilic infiltration, the LPS and E. coli administration markedly increased the MPO activity. However, the CNT treatment markedly attenuated the MPO activity in both LPS and E. coli-induced kidney injury. Furthermore, the CNT treatment markedly attenuated the NO production compared to the LPS and E. coli-induced kidney injury group. Additionally, the CNT treatment improved the histological parameters markedly (H and E, PAS and Masson's trichome staining) and protect the kidney from the inflammatory insult of the LPS and E. coli evidently. The comet assay revealed marked DNA damage, however, the CNT treatment markedly prevented the LPS and E. coli-induced kidney damage. The CNT treatment markedly enhanced the expression of Nrf2, while attenuated the iNOS expression in both models of kidney injury.