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| Other Sizes |
| Targets |
NF-kappaB (nuclear factor kappa-light-chain-enhancer of activated B cells). Manassantin B inhibits NF-kappaB activation by suppressing the transcriptional activity of the RelA/p65 subunit. It also has effects on NF-IL6 (C/EBPbeta), a transcription factor involved in inflammatory responses. In electrophoretic mobility shift assays (EMSA), manassantin B has an inhibitory effect on DNA binding by NF-IL6, but not by NF-kappaB. However, it inhibits the transactivation activity of both NF-IL6 and NF-kappaB. The compound also influences other signaling pathways, including JNK, BCL, ERK, STAT, p38 MAPK, and mitochondrial complex I (inhibition of mitochondrial complex I-mediated respiration).
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| ln Vitro |
In cell-free assays, manassantin B has been evaluated for its effects on transcription factor DNA binding using EMSA. Nuclear extracts from PMA-stimulated U937 cells are incubated with radiolabeled oligonucleotide probes containing NF-kappaB or NF-IL6 consensus binding sites. Manassantin B inhibits the DNA binding activity of NF-IL6 but does not block NF-kappaB DNA binding. However, in reporter gene assays, manassantin B inhibits the transactivation activity of both NF-kappaB and NF-IL6. For mitochondrial complex I inhibition, manassantin B inhibits complex I-mediated respiration in purified mitochondria at nanomolar concentrations, with no effect on complex II or complex IV activity.
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| ln Vivo |
In cultured cells, manassantin B exhibits cytotoxic activity against HT-29 human colon cancer cells with an IC50 of 12 uM. It suppresses expression of pro-inflammatory cytokines, including IL-1beta and IL-6, through inhibition of NF-IL6 and NF-kappaB transactivation. In PMA-stimulated U937 promonocytic cells, manassantin B inhibits NF-IL6 activity. The compound also possesses anti-EBV lytic replication activity, indicating potential antiviral effects. In 3T3-L1 preadipocytes, manassantin B inhibits adipogenesis, and in high-fat diet-fed mice, it reduces body weight gain and adipose tissue weight. Manassantin B also inhibits ACAT-1 and ACAT-2 (acyl-coenzyme A:cholesterol acyltransferase) activities, contributing to cholesterol-lowering effects.
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| Enzyme Assay |
Transcription factor activation is assessed by EMSA. U937 cells are stimulated with PMA (phorbol 12-myristate 13-acetate, 10 ng/mL) for 4 hours to activate NF-kappaB and NF-IL6. Nuclear extracts are prepared. For EMSA, double-stranded oligonucleotides containing NF-kappaB (5′-AGTTGAGGGGACTTTCCCAGGC-3′) or NF-IL6 (5′-TGCAGATTGCGCAATCTGCA-3′) consensus binding sites are labeled with [gamma-32P]-ATP using T4 polynucleotide kinase. Nuclear extracts (5-10 ug) are incubated with labeled probe in binding buffer for 20 minutes at room temperature, with or without manassantin B (1-50 uM). DNA-protein complexes are resolved by native PAGE and visualized by autoradiography. For transactivation assays, cells are transiently transfected with NF-kappaB- or NF-IL6-luciferase reporter constructs, treated with manassantin B (1-50 uM) plus PMA or TNF-alpha for 6-24 hours, and luciferase activity is measured.
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| Cell Assay |
Cell viability assays are performed using HT-29 human colon cancer cells. Cells are seeded in 96-well plates (5,000-10,000 cells/well) and cultured overnight. The next day, cells are treated with manassantin B at concentrations ranging from 0-50 uM for 48 hours. Cell viability is measured using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) or CellTiter-Glo assays. IC50 values are calculated from dose-response curves. For anti-adipogenesis assays, 3T3-L1 preadipocytes are differentiated into adipocytes using a differentiation cocktail (insulin, dexamethasone, IBMX) with or without manassantin B (1-20 uM) for 6-8 days. Lipid accumulation is measured by Oil Red O staining. For NF-kappaB luciferase reporter assays, HEK293 or HeLa cells are co-transfected with NF-kappaB-luciferase and Renilla luciferase plasmids. After 24 hours, cells are treated with manassantin B (0.1-50 uM) for 1 hour, then stimulated with TNF-alpha (10 ng/mL) for 6 hours. Luciferase activity is measured, and fold induction is calculated relative to unstimulated controls.
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| Animal Protocol |
Manassantin B has been evaluated in vivo for anti-obesity effects. In diet-induced obese C57BL/6N mice, manassantin B demonstrates preventive and therapeutic effects on obesity, accompanied by decreased adipocyte size. It also increases AMPK phosphorylation in subcutaneous white adipose tissue and brown adipose tissue. In high-fat diet-fed C57BL/6 mice, oral administration of manassantin B-containing fractions reduces body weight gain and adipose tissue weight, with improvements in serum lipid profiles. Cholesterol-lowering effects have been observed in high cholesterol-fed mice. Typical doses for in vivo studies range from 10-50 mg/kg administered orally or intraperitoneally. For acute inflammation models, manassantin B may be administered prior to LPS challenge to measure cytokine reduction.
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| ADME/Pharmacokinetics |
Dedicated pharmacokinetic studies for pure manassantin B have not been extensively reported. As a lignan (molecular weight 716.8, C41H48O11), manassantin B is relatively lipophilic and is soluble in methanol and DMSO but sparingly soluble in water. For in vivo studies, the compound is typically formulated in vehicles such as 0.5% carboxymethylcellulose (CMC), DMSO diluted in saline, or oil-based formulations for oral administration. Absorption, distribution, metabolism, and excretion (ADME) data are not publicly available. The compound's natural product origin suggests it may be subject to extensive phase II metabolism (glucuronidation, sulfation) and potential enterohepatic recirculation. Bioavailability is likely moderate.
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| Toxicity/Toxicokinetics |
Formal toxicology studies for manassantin B have not been reported in publicly available literature. Based on the compound's natural product origin from Saururus chinensis, which has a history of use in traditional medicine, it is likely to have acceptable acute safety at moderate doses. In animal studies, including anti-obesity and cholesterol-lowering experiments, no significant toxicity or body weight loss has been reported at efficacious doses (10-50 mg/kg). However, comprehensive acute, sub-chronic, and chronic toxicity studies have not been conducted. For research use, standard laboratory safety precautions should be followed. Manassantin B should be handled as a potential investigational agent and not for human consumption.
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| References | |
| Additional Infomation |
Manasantin B is a lignan isolated from the weeping lizard (Saururus cernuus) and the Chinese lizard (Saururus chinensis), and has been shown to have antitumor activity. It is both a metabolite and an antitumor drug. It is a dimethoxybenzene, belonging to the benzodioxane class of compounds, and is also a lignan, oxacyclopentane compound, and secondary alcohol. Manasantin B has been reported in both the Chinese lizard and the weeping lizard.
Manassantin B is a natural product lignan originally isolated from Saururus chinensis (Chinese lizard's tail) and also found in Saururus cernuus. It is also known as saucernetin B. The compound has a molecular weight of 716.8 and molecular formula C41H48O11. Manassantin B is the 1,2-dineolignan component, along with manassantin A and saucerneol B. The compound has been studied for its NF-kappaB inhibitory activity, which underlies its anti-inflammatory, anti-obesity, and anticancer properties. It also potently and specifically inhibits mitochondrial complex I (with no effect on complex II or IV), which may contribute to its cytotoxic effects. Manassantin B is not approved for human therapeutic use. The compound is used as a research tool for studying NF-kappaB and NF-IL6 signaling, obesity, and cancer biology. It is also referred to as MNSB in some literature. |
| Molecular Formula |
C41H48O11
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|---|---|
| Molecular Weight |
716.81322
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| Exact Mass |
716.32
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| CAS # |
88497-88-5
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| PubChem CID |
10439828
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| Appearance |
White to off-white solid powder
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| LogP |
7.536
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
52
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| Complexity |
1080
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@@H]1[C@@H](C)[C@@H](C2C=CC(O[C@H](C)[C@@H](C3C=CC4OCOC=4C=3)O)=C(OC)C=2)O[C@@H]1C1C=CC(O[C@H](C)[C@@H](C2C=CC(OC)=C(OC)C=2)O)=C(OC)C=1
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| InChi Key |
GSWZMFDCPMPHDL-FZBBBUCASA-N
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| InChi Code |
InChI=1S/C41H48O11/c1-22-23(2)41(29-12-16-33(36(20-29)47-8)51-25(4)39(43)27-10-14-31-37(18-27)49-21-48-31)52-40(22)28-11-15-32(35(19-28)46-7)50-24(3)38(42)26-9-13-30(44-5)34(17-26)45-6/h9-20,22-25,38-43H,21H2,1-8H3/t22-,23-,24-,25-,38+,39+,40+,41+/m1/s1
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| Chemical Name |
(1R,2R)-1-(1,3-benzodioxol-5-yl)-2-[4-[(2S,3R,4R,5S)-5-[4-[(1R,2R)-1-(3,4-dimethoxyphenyl)-1-hydroxypropan-2-yl]oxy-3-methoxyphenyl]-3,4-dimethyloxolan-2-yl]-2-methoxyphenoxy]propan-1-ol
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3951 mL | 6.9753 mL | 13.9507 mL | |
| 5 mM | 0.2790 mL | 1.3951 mL | 2.7901 mL | |
| 10 mM | 0.1395 mL | 0.6975 mL | 1.3951 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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