| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| 5g |
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Purity: ≥98%
Andrographolide, a naturally occuring labdane diterpenoid extracted from the stem and leaves of Andrographis paniculata, is an irreversible/covalent NF-κB inhibitor with potential anti-inflammatory activity. In endothelial cells, it creates a covalent bond with the cysteine residue on p50 to prevent NF-κB activation.
| Targets |
p50
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| ln Vitro |
Andrographolide (AP) reduces the expression of osteoclast-specific markers and inhibits RANKL-mediated osteoclast differentiation and bone resorption in vitro. Andrographolide reduces inflammation by preventing TNF-induced NF-B activation through covalent modification of reduced Cys62 of p50, without affecting I-B degradation or p50/p65 nuclear translocation. Without affecting p38 or JNK signaling, andrographolide also blocks the ERK/MAPK signaling pathway. RAW 264.7 cells' differentiation into osteoclasts is inhibited by andrographolide in a concentration-dependent manner. In both BMMs and RAW 264.7 cells, andrographolide inhibits osteoclast formation in a concentration-dependent manner without obviously having cytotoxic effects. Treatment with andrographolide significantly reduces the area of bone resorption. After 2.5 μM Andrographolide treatment, only about 30% of the bone resorption seen in the control group is accomplished. After receiving treatment with 10 μM Andrographolide, osteoclastic bone resorption is almost entirely inhibited[1].
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| ln Vivo |
Treatment with andrographolide (5 or 30 mg/kg) lessens the severity of bone loss brought on by LPS. In addition, andrographolide slightly improves BMD and cortex thickness in comparison to LPS treatment. The protective effects of andrographolide against bone loss caused by LPS are confirmed by histological analysis. Increased TRAP-positive osteoclast numbers and inflammatory bone erosion are caused by LPS injection[1].
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| Enzyme Assay |
In vitro osteoclastogenesis assays are preformed to examine the effects of Andrographolide on osteoclast differentiation. BMM cells, or bone marrow macrophages, are created. In a T-75 cm2 flask with complete cell culture media and 30 ng/mL M-CSF, cells taken from the femur and tibiae of a 6-week-old C57/BL6 mouse are incubated for proliferation. The cells are washed when the medium is changed to remove any stromal cells that may still be present. Cells are three times PBS-washed and then trypsinized for 30 minutes to harvest BMMs once they have reached 90% confluence. BMMs are cells that stick to the bottom of the dish. BMMs are plated in 96-well plates at a density of 8×103 cells per well in triplicate and incubated for 24 hours at 37 °C in a humidified incubator containing 5% CO2. Then, different concentrations of andrographolide (0, 2.5, 5, or 10 μM) are added to the cells along with M-CSF (30 ng/mL) and RANKL (50 ng/mL). Cells are fixed and stained to check for tartrate-resistant acid phosphatase (TRAP) activity after five days. Osteoclasts are multinucleated cells that are positive for TRAP and have five or more nuclei[1].
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| Cell Assay |
Effects of Andrographolide on cell proliferation are determined with a CCK-8. BMMs are plated in 96-well plates at a density of 3×103 cells per well in triplicate. After twenty-four hours, the cells are exposed to increasing doses of andrographolide (0, 2.5, 5, 10, or 20 μM) for two days. The plates are then incubated at 37°C for an additional 2 hours after the addition of 10 μL of CCK-8 to each well. The optical density (OD) is then determined using an ELX800 absorbance microplate reader at a wavelength of 450 nm (650 nm reference). Calculations are made to determine cell viability[1].
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| Animal Protocol |
Mice: Four groups of seven C57BL/6 mice each are created using 8-week-old mice. One day prior to the injection of LPS (5 g/g body weight), mice are administered i.p. injections of andrographolide (5 or 30 mg/kg body weight) or PBS as a control. Over the course of eight days, either andrographolide or PBS is intraperitoneally injected. On days one and four, LPS is administered intraperitoneally. All mice are euthanized 8 days after receiving the initial LPS injection, and their left femurs are all scanned using a high-resolution micro-CT with a 9-m resolution.
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| References |
| Molecular Formula |
C20H30O5
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| Molecular Weight |
350.45
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| Exact Mass |
350.21
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| Elemental Analysis |
C, 68.54; H, 8.63; O, 22.83
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| CAS # |
5508-58-7
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C[C@@]12CC[C@H]([C@@]([C@H]1CCC(=C)[C@H]2C/C=C/3\[C@@H](COC3=O)O)(C)CO)O
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| InChi Key |
BOJKULTULYSRAS-OTESTREVSA-N
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| InChi Code |
InChI=1S/C20H30O5/c1-12-4-7-16-19(2,9-8-17(23)20(16,3)11-21)14(12)6-5-13-15(22)10-25-18(13)24/h5,14-17,21-23H,1,4,6-11H2,2-3H3/b13-5+/t14-,15-,16+,17-,19+,20+/m1/s1
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| Chemical Name |
(3E,4S)-3-[2-[(1R,4aS,5R,6R,8aS)-6-hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylidene-3,4,4a,6,7,8-hexahydro-1H-naphthalen-1-yl]ethylidene]-4-hydroxyoxolan-2-one
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| Synonyms |
Andrographolide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8535 mL | 14.2674 mL | 28.5347 mL | |
| 5 mM | 0.5707 mL | 2.8535 mL | 5.7069 mL | |
| 10 mM | 0.2853 mL | 1.4267 mL | 2.8535 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04833946 | Recruiting | Other: Andrographis paniculata [150 mg] Other: Microcrystalline Cellulose (MCC) |
Knee Osteoarthritis (Knee OA) |
Vedic Lifesciences Pvt. Ltd. | March 13, 2021 | Not Applicable |
| NCT03455049 | Completed | Other: Andrographis Paniculata Ext |
Increased Insulin | Indonesia University | October 17, 2017 | Not Applicable |
| NCT04196075 | Completed | Drug: Andrographis Paniculata | Squamous Cell Carcinoma of Esophagus |
Chinese University of Hong Kong |
March 1, 2018 | Phase 3 |
| NCT01993472 | Terminated | Drug: Andrographolides Drug: Capecitabine |
Colorectal Neoplasms | Gu Yanhong | November 2013 | Phase 2 |
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