Podocarpusflavone A
(Synonyms: 竹柏双黄酮 A；罗汉松双黄酮A) 目录号 : GC33143
A biflavone with diverse biological activities
Cas No.:22136-74-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Podocarpusflavone A is a biflavone that has been found in D. araucarioides and has diverse biological activities.1,2,3,4 It inhibits dengue virus NS5 RNA-dependent RNA polymerase (DENV-NS5 RdRp; IC50 = 0.75 ?M).3 Podocarpusflavone A also inhibits cathepsin B with an IC50 value of 1.68 ?M and inhibits STAT3 in a reporter assay in a concentration-dependent manner.1,2 It reduces the production of reactive oxygen species (ROS) and superoxide anions induced by phorbol 12-myristate 13-acetate in isolated human neutrophils when used at concentrations of 1 and 10 ?M, respectively.4 Podocarpusflavone A also inhibits aggregation of amyloid-β (1-40) peptide in a cell-free assay with an IC50 value of 4.9 μM.5 Podocarpusflavone A (20 ?M) decreases viability of A375, MALME-3M, SK-MEL-1, and SK-MEL-5 melanoma cells and reduces tumor growth in an A375 mouse xenograft model when administered at doses of 20 and 40 mg/kg.2
1.Zhang, Y., Tan, N.S., Huang, H., et al.Three bioactive biflavones isolated from Taxodium mucronatumYunnan Zhiwu Yanjiu27(1)107-110(2005) 2.Meng, H., Pang, Y., Liu, G., et al.Podocarpusflavone A inhibits cell growth of skin cutaneous melanoma by suppressing STAT3 signalingJ. Dermatol. Sci.100(3)201-208(2020) 3.Coulerie, P., Nour, M., Maciuk, A., et al.Structure-activity relationship study of biflavonoids on the Dengue virus polymerase DENV-NS5 RdRpPlanta Med.79(14)1313-1318(2013) 4.Arwa, P.S., Zeraik, M.L., Ximenes, V.F., et al.Redox-active biflavonoids from Garcinia brasiliensis as inhibitors of neutrophil oxidative burst and human erythrocyte membrane damageJ. Ethnopharmacol.174410-418(2015) 5.Sirimangkalakitti, N., Juliawaty, L.D., Hakim, E.H., et al.Naturally occurring biflavonoids with amyloid β aggregation inhibitory activity for development of anti-Alzheimer agentBioorg. Med. Chem. Lett.29(15)1994-1997(2019)
| Cas No. | 22136-74-9 | SDF | |
| 别名 | 竹柏双黄酮 A；罗汉松双黄酮A | ||
| Canonical SMILES | O=C1C=C(C2=CC=C(OC)C=C2)OC3=C(C4=CC(C5=CC(C6=C(O)C=C(O)C=C6O5)=O)=CC=C4O)C(O)=CC(O)=C13 | ||
| 分子式 | C31H20O10 | 分子量 | 552.48 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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 | 1.81 mL | 9.0501 mL | 18.1002 mL |
| 5 mM | 0.362 mL | 1.81 mL | 3.62 mL |
| 10 mM | 0.181 mL | 0.905 mL | 1.81 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。
Podocarpusflavone A inhibits cell growth of skin cutaneous melanoma by suppressing STAT3 signaling
J Dermatol Sci 2020 Dec;100(3):201-208.PMID:33127205DOI:10.1016/j.jdermsci.2020.10.008.
Background: JAK2/STAT3 pathway is involved in the development and progression of melanoma once DNA damage is caused by environment and genetic factors. Objective: Here, we aimed to identify novel inhibitor of JAK2/STAT3 pathway and reveal the underlying mechanisms. Methods: Eighty MedChemExpress compounds were screened by using STAT3-Luc reporter in A375 cells. Podocarpusflavone A (PCFA) was identified as an inhibitor of STAT3, which was further verified in four melanoma cell lines. The anti-melanoma effects and mechanism of PCFA were examined and explored in melanoma cells and mouse xenograft models by using Western blot and cell-counting kit-8 assay. Results: PCFA exhibited potent inhibitory effects on melanoma both in vitro and in vivo. PCFA inhibited the activation of STAT3 through suppressing the phosphorylation of JAK2, and then restrained cell cycle and induced apoptosis of melanoma cells. Conclusion: PCFA inhibits melanoma growth via the inhibition of JAK2/STAT3 pathway, which provides a promising therapeutic strategies of melanoma treatment.
Homology Modeling of Leishmanolysin (gp63) from Leishmania panamensis and Molecular Docking of Flavonoids
ACS Omega 2020 Jun 10;5(24):14741-14749.PMID:32596611DOI:10.1021/acsomega.0c01584.
Leishmaniasis is a chronic disease caused by protozoa of the distinct Leishmania genus transmitted by sandflies of the genus Phlebotomus (old world) and Lutzomyia (new world). Among the molecular factors that contribute to the virulence and pathogenesis of Leishmania are metalloproteases, e.g., glycoprotein 63 (gp63), also known as leishmanolysin or major surface protease (MSP). This protease is a zinc-dependent metalloprotease that is found on the surface of the parasite, abundant in Leishmania promastigote and amastigote. This study describes the prediction of three-dimensional (3D) structures of leishmanolysin (UniProt ID A0A088RJX7) of Leishmania panamensis employing a homology modeling approach. The 3D structure prediction was performed using the SWISS-MODEL web server. The tools PROCHECK, Molprobyty, and Verify3D were used to check the quality of the model, indicating that they are reliable. Best docking configurations were identified applying AutoDock Vina in PyRx 0.8 to obtain a potential antileishmanial activity. Biflavonoids such as lanaroflavone, Podocarpusflavone A, amentoflavone, and podocarpusflavone B showed good scores among these molecules. Lanaroflavone appears to be the most suitable compound from binding affinity calculations.
Biflavones from Chamaecyparis obtusa
Z Naturforsch C J Biosci 2005 Sep-Oct;60(9-10):679-85.PMID:16320608DOI:10.1515/znc-2005-9-1004.
From the leaves of Chamaecyparis obtusa several biflavones were isolated and identified, namely: sciadopitysin, ginkgetin, isoginkgetin, podocarpusflavone B, 7,7"-O-dimethylamentoflavone, bilobetin, Podocarpusflavone A, and 7-O-methylamentoflavone. The presence of amentoflavone and hinokiflavone was also confirmed. The composition of biflavones in other Chamaecyparis species--Ch. lawsoniana, Ch. thyoides--and cultivar varieties--Ch. pisifera "Squarrosa", Ch. pisifera "Boulevard"--was compared using the HPLC method. It was stated, that Podocarpusflavone A and 7-O-methylamentoflavone in addition to amentoflavone and hinokiflavone may be classified as chemotaxonomic markers of the genus Chamaecyparis.
Biflavonoids of Dacrydium balansae with potent inhibitory activity on dengue 2 NS5 polymerase
Planta Med 2012 May;78(7):672-7.PMID:22411725DOI:10.1055/s-0031-1298355.
In order to find new molecules for antiviral drug design, we screened 102 ethyl acetate extracts from New-Caledonian flora for antiviral activity against the dengue 2 virus RNA-dependant RNA polymerase (DV-NS5 RdRp). The leaf extract of Dacrydium balansae, which strongly inhibited the DV-NS5, was submitted to bioguided fractionation. Four biflavonoids ( 1- 4), three sterols ( 5- 7), and two stilbene derivatives ( 8- 9) were identified and evaluated for their antiviral potential on the DV-NS5 RdRp. Biflavonoids appeared to be potent inhibitors of DV-NS5 RdRp with IC (50)s between 0.26 and 3.12 µM. Inhibitory activity evaluations against the RNA polymerase from other Flaviviridae viruses allowed us to conclude that these compounds are specific inhibitors of the DV RNA polymerase. The strongest inhibitions were observed with hinokiflavone ( 4), but Podocarpusflavone A ( 2) is the strongest noncytotoxic inhibitor of the DV-NS5 and it also displayed polymerase inhibitory activity in a DV replicon. A preliminary structure-activity relationship study (SARs) revealed the necessity of the biflavonoid skeleton, the influence of number and position of methoxylations, and the importance of a free rotation of the linkage between the two apigenin monomers of the biflavonoids. To the best of our knowledge, Podocarpusflavone A ( 2) is the strongest noncytotoxic non-nucleotide molecule exhibiting a specific inhibitory activity against the RNA polymerase domain of DV-NS5 and thus is promising for chemotherapy development against dengue fever.
Bioactive compounds from Celaenodendron mexicanum
Planta Med 2000 Jun;66(5):463-8.PMID:10909269DOI:10.1055/s-2000-8598.
Bioactivity-directed fractionation of the CHCl3-MeOH extract of the leaves of Celaenodendron mexicanum by means of the brine shrimp lethality test and chromatographic techniques led to the isolation of three carboxylic acid triterpenes, the new tirucalla-type triterpene, 3 alpha-hydroxytirucalla-7,24Z-dien-26-oic acid, 3-oxotirucalla-7,24Z-dien-26-oic acid, and epi-oleanolic acid, and three biflavonoids amentoflavone, Podocarpusflavone A, and podocarpusflavone B. Four non-active compounds friedelin, maytensifolin B, 3 beta-hydroxyfriedelan-16-one, and celaenodendrolide were also obtained. epi-Oleanolic acid was the most active against brine shrimps with LC50 value of 23.3 microM. In addition, all isolates were tested for in vitro antiprotozoal and cytotoxic activities. 3-Oxotirucalla-7,24Z-dien-26-oic acid and epi-oleanolic acid showed the highest activity against Leishmania donovani promastigotes with IC50 values of 13.7 and 18.8 microM, respectively. Only 3-oxotirucalla-7,24Z-dien-26-oic acid showed activity against Trypanosoma brucei brucei bloodstream forms with IC50 value of 16.8 microM.