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| Targets |
Glaucocalyxin B targets cancer cells by inducing autophagy and inhibiting cell proliferation. Its mechanism involves the induction of autophagic cell death, a process distinct from apoptosis. It has been shown to decrease the growth of HL-60 leukemia cells. Its anti-inflammatory activity is likely mediated through the modulation of inflammatory signaling pathways, though the exact molecular targets are not fully detailed in the available sources. Its activity as an autophagy inducer makes it a unique tool for studying this cellular process.
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| ln Vitro |
The proliferation of HL-60 cells is dose-dependently inhibited by glaucocalyxin A (GlnA) and (GlnB), with IC50 values of roughly 6.15 and 5.86 µM, respectively, after 24 hours. Reactive oxygen species (ROS) buildup, DNA damage, G2/M phase cycle arrest, and HL-60 cell death can all be brought on by Gln A and B [1]. Through the induction of autophagy and death, GlnB suppresses the growth of human cervical cancer cells in vitro. This process may be facilitated by the Akt/phosphatidylinositol 4,5-bisphosphate 3-kinase pathway. The growth of cervical cancer cell lines HeLa and SiHa was dose-dependently reduced by GlnB therapy. Poly(ADP-ribose) polymerase 1 cleavage is enhanced and apoptotic cell populations are increased by GlnB. Additionally, GlnB promoted the cleavage of the light chain 3 II/I protein, indicating the induction of autophagy. Phosphatase and tensin homologs are expressed more when GlnB is administered, whereas phosphorylated protein kinase B is expressed less [2]. One of the five enantio-kaurinic acid diterpenoids, glaucocalyxin B (GLB), has the ability to significantly lower different levels of nitric oxide (NO), tumor necrosis factor (TNF)-α, interleukin (IL)-1β, cyclic Oxygenase (COX)-2, and inducible nitric oxide, which is produced in microglia by lipopolysaccharide-activated oxidase synthase (iNOS) [3].
In vitro, Glaucocalyxin B decreases the growth of HL-60 cells with an IC50 of approximately 5.86 μM at 24 hours. It acts as an autophagy inducer. These activities demonstrate its potent anticancer properties. Its anti-inflammatory activity has also been reported. Quantitative IC50 values for its effect on other cancer cell lines are not detailed in the publicly available sources. |
| ln Vivo |
In vivo activity data for Glaucocalyxin B is limited in publicly available literature. As a compound with potent anticancer activity in vitro, it is hypothesized to exhibit similar effects in animal models. However, specific in vivo efficacy studies, including pharmacokinetic and pharmacodynamic parameters, have not been detailed in the available sources. Further research is needed to fully characterize its in vivo activity and therapeutic potential.
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| Enzyme Assay |
For cell-free enzyme assays, the activity of Glaucocalyxin B as an autophagy inducer can be studied using in vitro assays that measure autophagosome formation or autophagic flux. However, these are typically cell-based assays. Its effect on specific enzymes, such as kinases, could be studied using standard kinase activity assays with purified enzymes.
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| Cell Assay |
For in vitro cellular assays, the anticancer activity of Glaucocalyxin B is typically assessed in cancer cell lines, such as HL-60 leukemia cells. Cells are seeded in multi-well plates and treated with varying concentrations of the compound for a defined period (e.g., 24-72 hours). Cell viability is measured using MTT, MTS, or SRB assays, and the IC50 value is calculated. Its effect on autophagy is assessed by measuring the expression of autophagy markers, such as LC3-II, by Western blot, or by visualizing autophagosomes using fluorescence microscopy.
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| Animal Protocol |
For in vivo studies, Glaucocalyxin B could be administered orally or intraperitoneally in rodent models of cancer. In a xenograft model, its anti-tumor efficacy would be assessed by measuring tumor volume over time. Its effect on autophagy in vivo could be assessed by examining tumor tissue for autophagic markers. Its anti-inflammatory effect could be assessed in models of inflammation.
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| ADME/Pharmacokinetics |
Glaucocalyxin B has a molecular formula of C20H26O4 and a molecular weight of 330.42 g/mol. Its CAS number is 80508-81-2. It is an ent-kaurane-type diterpenoid and is typically supplied as a powder. It is soluble in DMSO and ethanol. For in vitro studies, stock solutions are prepared in DMSO. For in vivo administration, it can be formulated in suitable vehicles. Storage is recommended at -20°C, protected from light. Its purity is typically >98% for research use.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural diterpenoid, its safety profile would need to be established through standard toxicological studies. In vitro cytotoxicity assays in various cell lines are typically performed alongside efficacy studies to confirm that the observed effects are not due to a general reduction in cell viability.
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| References |
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| Additional Infomation |
Reports indicate that Isodon japonicus and Isodon pharicus contain Glaucocalyxin B, and relevant data is available for reference.
Glaucocalyxin B is a research-grade compound and is not approved for any therapeutic use. It serves primarily as a valuable pharmacological tool for studying autophagy and cancer. Its mechanism of action involves the induction of autophagy and the inhibition of cancer cell proliferation. Its anticancer activity makes it a compound of interest for drug discovery. No clinical trials have been reported. |
| Molecular Formula |
C22H30O5
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| Molecular Weight |
374.4706
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| Exact Mass |
374.209
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| CAS # |
80508-81-2
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| PubChem CID |
14193399
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
509.1±50.0 °C at 760 mmHg
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| Melting Point |
190.5-191 ºC
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| Flash Point |
172.9±23.6 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.554
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| LogP |
1.37
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
752
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC(=O)O[C@@H]1[C@H]2CC[C@@H]3[C@]1([C@@H](C[C@H]4[C@]3(CCC(=O)C4(C)C)C)O)C(=O)C2=C
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| InChi Key |
LSUXOKVMORWDLT-KEXKRWMXSA-N
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| InChi Code |
InChI=1S/C22H30O5/c1-11-13-6-7-14-21(5)9-8-16(24)20(3,4)15(21)10-17(25)22(14,18(11)26)19(13)27-12(2)23/h13-15,17,19,25H,1,6-10H2,2-5H3/t13-,14-,15+,17+,19+,21-,22-/m0/s1
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| Chemical Name |
[(1R,2R,4S,9R,10S,13S,16R)-2-hydroxy-5,5,9-trimethyl-14-methylidene-6,15-dioxo-16-tetracyclo[11.2.1.01,10.04,9]hexadecanyl] acetate
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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 |
| 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) |
DMSO : ~100 mg/mL (~267.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.34 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 12.5 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: ≥ 1.25 mg/mL (3.34 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 12.5 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: ≥ 1.25 mg/mL (3.34 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 | 2.6704 mL | 13.3522 mL | 26.7044 mL | |
| 5 mM | 0.5341 mL | 2.6704 mL | 5.3409 mL | |
| 10 mM | 0.2670 mL | 1.3352 mL | 2.6704 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.
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