| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
HIV-1 protease
Rosamultin targets HIV-1 protease as an inhibitor. It also targets oxidative stress pathways through its antioxidant and anti-apoptotic effects. The compound's anti-inflammatory effects are mediated through modulation of inflammatory signaling pathways. Its antinociceptive properties suggest activity at pain pathways. The compound's hepatoprotective effects are mediated, at least in part, through enhanced activity of epoxide hydrolase. As a triterpenoid glycoside, rosamultin may also interact with cellular membranes and modulate various signaling pathways involved in inflammation and oxidative stress. |
|---|---|
| ln Vitro |
R is separated from Rosamultin. At a 100 μM concentration, rugosa roots inhibit HIV-1 protease by 53% [1].
Rosamultin showed an inhibitory effect of 52.9 ± 2.0% against HIV-1 protease at a concentration of 100 μM in a cell-free enzymatic assay. Among seven compounds isolated from R. rugosa (gallic acid, methyl gallate, quercetin, hyperoside, (+)-catechin, rosamultin, and kaji-ichigoside F1), rosamultin exhibited the most potent inhibitory activity (53%) against HIV-1 protease at 100 μM. In vitro, rosamultin isolated from the root of R. rugosa inhibits HIV-1 protease by 53% at a concentration of 100 μM. The compound has demonstrated antioxidant, anti-inflammatory, and antinociceptive properties in various cell-based assays. It has been shown to protect cells from H₂O₂-induced oxidative stress injury through its antioxidant and anti-apoptotic effects. The compound's effects on HIV-1 protease activity have been characterized using enzyme inhibition assays. Its ability to modulate inflammatory cytokine production and oxidative stress markers has been studied in relevant cell models. |
| ln Vivo |
In vivo, rosamultin has been studied for its hepatoprotective effects, protecting against bromobenzene-induced hepatotoxicity through enhanced activity of epoxide hydrolase. The compound's anti-inflammatory and antinociceptive properties have been evaluated in animal models. Its antioxidant effects have been demonstrated in models of oxidative stress. The compound's potential for treating oxidative stress injury has been investigated. Studies have examined its effects on liver function, inflammatory markers, and pain responses in rodent models.
|
| Enzyme Assay |
The HIV-1 protease inhibitory activity was measured using a recombinant HIV-1 protease prepared in-house. The substrate used was His-Lys-Ala-Arg-Val-Leu-(pNO2-Phe)-Glu-Ala-Nle-Ser-NH2. The enzyme stock solution was diluted for the assay. Test compounds were dissolved in dimethyl sulfoxide (10% in the reaction mixture). The reaction mixture (5 μL total volume) consisted of 1 μL of 50 mM sodium acetate buffer (pH 5.0), 1 μL of substrate solution, 1 μL of the test compound solution (or plant extract), and 2 μL of HIV-1 protease solution. The mixture was stirred, centrifuged, and incubated at 37°C for 1 hour in a microtube. A control reaction was performed under identical conditions without the test compound. The reaction was terminated by heating at 90°C for 1 minute. Then, 35 μL of sterile water was added, and a 5 μL aliquot was analyzed by HPLC. The hydrolysate and remaining substrate were quantitatively analyzed by reversed-phase HPLC on a C18 column (150 × 4.6 mm i.d.) with a linear gradient of acetonitrile from 20% to 40% in 0.1% trifluoroacetic acid at a flow rate of 1.0 mL/min, with detection at 280 nm. The retention times of the substrate and the pNO2-Phe-bearing hydrolysate were approximately 9 and 4 minutes, respectively. Inhibitory activity was calculated as: % inhibition = (A_control - A_sample) × 100 / A_control, where A is the relative peak area of the hydrolysate. Rosamultin was tested at 100 μM and showed 52.9% inhibition. [2]
In cell-free biochemical assays, rosamultin is evaluated for its inhibitory activity against HIV-1 protease. Enzyme activity assays using a substrate (His-Lys-Ala-Arg-Val-Leu-(pNO2-Phe)-Glu-Ala-Nle-Ser-NH2) are used to measure the compound's ability to inhibit protease activity. Rosamultin inhibits HIV-1 protease by 53% at 100 μM. Its antioxidant activity is assessed using standard biochemical assays. The compound's purity and molecular weight (650.84 g/mol) are characterized using analytical techniques. These assays confirm the compound's mechanism as an HIV-1 protease inhibitor and antioxidant. |
| Cell Assay |
Cellular assays for rosamultin involve evaluating its effects on HIV-1 protease activity, oxidative stress, and inflammation in relevant cell lines. The compound's ability to protect cells from H₂O₂-induced oxidative stress injury has been demonstrated. Its anti-inflammatory effects are assessed by measuring cytokine production and inflammatory marker expression. The compound's antinociceptive properties are evaluated in cellular models of pain signaling. Studies have examined its effects on cell viability, apoptosis, and oxidative stress markers in various cell types.
|
| Animal Protocol |
Animal models for rosamultin include models of hepatotoxicity, oxidative stress, inflammation, and pain. The compound has been studied for its hepatoprotective effects in bromobenzene-induced hepatotoxicity models. Its anti-inflammatory and antinociceptive effects have been evaluated in standard rodent models of inflammation and pain. The compound's antioxidant effects have been assessed in models of oxidative stress. Studies have examined its effects on liver enzyme levels, inflammatory markers, and pain responses.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for rosamultin are limited. The compound has a molecular weight of 650.84 g/mol with a molecular formula of C36H58O10. The CAS number is 88515-58-6. The compound is a 19α-hydroxy triterpene extracted from natural sources. It should be stored as a powder at -20°C for up to 3 years. Standard pharmacokinetic studies in preclinical species have characterized its absorption, distribution, metabolism, and excretion. As a natural product, its bioavailability and metabolic stability may be limited.
|
| Toxicity/Toxicokinetics |
The toxicity profile of rosamultin has not been extensively documented. As a natural product with demonstrated biological activities, standard safety precautions for handling laboratory chemicals apply. The compound is for research use only and not for human use. No significant toxicity has been reported in the available literature. However, as with all research compounds, appropriate handling procedures should be followed to minimize exposure.
|
| References | |
| Additional Infomation |
Rosamultin has reportedly been found in Rosa laevigata, Rubus ellipticus var. obcordatus, and other organisms for which data is available.
Rosamultin is an ursane-type triterpenoid isolated from the root of Rosa rugosa. The root of R. rugosa has been used as an antidiabetic in Korean folkloric medicine and has been reported to have hypolipidemic effects and DPPH radical-scavenging activity. Among naturally occurring ursane-type triterpenoids, ursolic acid and uvaol were previously reported to have HIV protease inhibitory activity; the malonyl hemiester of ursolic acid showed more potent activity. In this study, rosamultin showed the most potent inhibition (53%) among the tested compounds from R. rugosa at 100 μM. [2] Rosamultin is a 19α-hydroxyursane-type triterpenoid isolated from Rosa rugosa and Potentilla anserina L. It has antioxidant, anti-inflammatory, antinociceptive properties, and anti-HIV activity. The compound inhibits HIV-1 protease by 53% at a concentration of 100 μM. It has potential for treating H₂O₂-induced oxidative stress injury through its antioxidant and anti-apoptotic effects. Rosamultin may protect against bromobenzene-induced hepatotoxicity through enhanced activity of epoxide hydrolase. The compound has a molecular weight of 650.84 g/mol and a formula of C36H58O10. The CAS number is 88515-58-6. |
| Molecular Formula |
C36H58O10
|
|---|---|
| Molecular Weight |
650.8397
|
| Exact Mass |
650.403
|
| CAS # |
88515-58-6
|
| PubChem CID |
21122581
|
| Appearance |
White to off-white solid powder
|
| Density |
1.31g/cm3
|
| Boiling Point |
741.5ºC at 760 mmHg
|
| Flash Point |
223.6ºC
|
| Index of Refraction |
1.604
|
| LogP |
2.433
|
| Hydrogen Bond Donor Count |
7
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
46
|
| Complexity |
1250
|
| Defined Atom Stereocenter Count |
16
|
| SMILES |
C([C@]12CC[C@@H](C)[C@](O)(C)[C@H]1C1=CC[C@@H]3[C@]4(C[C@@H](O)[C@H](O)C(C)(C)[C@@H]4CC[C@@]3(C)[C@@]1(CC2)C)C)(=O)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1
|
| InChi Key |
MLKQAGPAYHTNQQ-BRDPIYJESA-N
|
| InChi Code |
InChI=1S/C36H58O10/c1-18-10-13-36(30(43)46-29-26(41)25(40)24(39)21(17-37)45-29)15-14-33(5)19(27(36)35(18,7)44)8-9-23-32(4)16-20(38)28(42)31(2,3)22(32)11-12-34(23,33)6/h8,18,20-29,37-42,44H,9-17H2,1-7H3/t18-,20-,21-,22+,23-,24-,25+,26-,27-,28+,29+,32+,33-,34-,35-,36+/m1/s1
|
| Chemical Name |
[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl] (1R,2R,4aS,6aR,6aS,6bR,8aR,10R,11R,12aR,14bS)-1,10,11-trihydroxy-1,2,6a,6b,9,9,12a-heptamethyl-2,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydropicene-4a-carboxylate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~153.65 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.84 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 (3.84 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 (3.84 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 | 1.5365 mL | 7.6824 mL | 15.3648 mL | |
| 5 mM | 0.3073 mL | 1.5365 mL | 3.0730 mL | |
| 10 mM | 0.1536 mL | 0.7682 mL | 1.5365 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.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
