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Hecogenin Acetate Sale

(Synonyms: 龙舌兰皂苷乙酯) 目录号 : GC43808

A steroid sapogenin

Hecogenin Acetate Chemical Structure

Cas No.:915-35-5

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1g
¥839.00
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产品描述

Hecogenin acetate is a steroid sapogenin and an acetylated form of hecogenin that has anthelmintic and antinociceptive properties. It reduces the percentage of mobile larvae in goat fecal cultures containing Haemonchus, Oesophagostomum, and Trichostrongylus nematodes (EC50 = 0.49 mg/ml). Hecogenin acetate (5, 10, or 20 mg/kg, i.p.) inhibits development of mechanical hyperalgesia induced by carrageenan, TNF-α, dopamine , and prostaglandin E2 in mice. It also increases latency to tail withdrawal in the tail flick test and has no effect on motor performance in the rotarod test in mice when administered at a dose of 40 mg/kg.

Chemical Properties

Cas No. 915-35-5 SDF
别名 龙舌兰皂苷乙酯
Canonical SMILES O=C1[C@@]2(C)[C@](C[C@@]3([H])[C@]2([H])[C@H](C)[C@]4(OC[C@H](C)CC4)O3)([H])[C@]5([H])CC[C@@]6([H])C[C@@H](OC(C)=O)CC[C@]6(C)[C@@]5([H])C1
分子式 C29H44O5 分子量 472.7
溶解度 DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH 7.2)(1:2): 0.3 mg/mL 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.1155 mL 10.5775 mL 21.1551 mL
5 mM 0.4231 mL 2.1155 mL 4.231 mL
10 mM 0.2116 mL 1.0578 mL 2.1155 mL
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Research Update

Hecogenin Acetate inhibits reactive oxygen species production and induces cell cycle arrest and senescence in the A549 human lung cancer cell line

Anticancer Agents Med Chem 2014;14(8):1128-35.PMID:25115457DOI:10.2174/1871520614666140408151751.

Cellular and molecular mechanisms related to lung cancer have been extensively studied in recent years, but the availability of effective treatments is still scarce. Hecogenin Acetate, a natural saponin presenting a wide spectrum of reported pharmacological activities, has been previously evaluated for its anticancer/antiproliferative activity in some in vivo and in vitro models. Here, we investigated the effects of Hecogenin Acetate in a human lung cancer cell line. A549 non-small lung cancer cells were exposed to different concentrations of Hecogenin Acetate and reactive species production, ERK1/2 activation, matrix metalloproteinase expression, cell cycle arrest and cell senescence parameters were evaluated. Hecogenin Acetate significantly inhibited increase in intracellular reactive species production induced by H2O2. In addition, Hecogenin Acetate blocked ERK1/2 phosphorylation and inhibited the increase in MMP-2 caused by H2O2. Treatment with Hecogenin Acetate induced G0/G1-phase arrest at two concentrations (75 and 100 µM, 74% and 84.3% respectively), and increased the staining of senescence-associated β -galactosidase positive cells. These data indicate that Hecogenin Acetate is able to exert anti-cancer effects by modulating reactive species production, inducing cell cycle arrest and senescence and also modulating ERK1/2 phosphorylation and MMP-2 production.

Antiulcerogenic and healing activity of Hecogenin Acetate in rodents

Naunyn Schmiedebergs Arch Pharmacol 2023 Apr;396(4):759-769.PMID:36474020DOI:10.1007/s00210-022-02341-0.

Peptic ulcers are lesions in the gastric and duodenal mucosa generated by an imbalance between protective factors (gastroduodenal mucus secretion, bicarbonate production, adequate blood flow) and harmful factors (excess pepsin or hydrochloric acid). Some drugs used in peptic ulcer therapy are associated with adverse effects. The aim of this study was to evaluate the antiulcerogenic and healing activity of Hecogenin Acetate (HA) in acute and chronic models of gastric lesions in rodents. The antiulcerogenic activity of HA was evaluated in models of gastric lesions induced by absolute ethanol and in acidified ethanol with HA (5, 10, and 20 mg/kg). For the model of gastric lesions induced by ischemia and reperfusion, rats were pre-treated with HA (5, 10, 20 mg/kg). After that, they were submitted to 30 min of ischemia, followed by 1 h of reperfusion. To evaluate the healing activity was induced gastric ulcer using acetic acid (80%) in rats. After 24 h, they were treated for 7 consecutive days with HA (10 and 20 mg/kg). They were evaluated the possible signs of toxicity, measurement of the lesions, collagen deposition, and histological analysis. HA significantly reduced the area of the lesion in models of gastric lesions induced by absolute and acidified ethanol, ischemia-induced gastric lesions and reperfusion, and regarding healing. In the collagen deposition, the presence and increase of collagen demonstrate the healing effect. The AH has antiulcerogenic and healing potential demonstrated by the decrease in gastric injury and presence of collagen fibers, respectively.

Amorphous solid dispersions of Hecogenin Acetate using different polymers for enhancement of solubility and improvement of anti-hyperalgesic effect in neuropathic pain model in mice

Biomed Pharmacother 2018 Jan;97:870-879.PMID:29136763DOI:10.1016/j.biopha.2017.10.161.

Hecogenin Acetate (HA) is an acetylated sapogenin that has shown potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors. However, HA exhibits poor aqueous solubility, which may limit its application. This study aims to develop amorphous solid dispersions (ASD) using five hydrophilic polymers, to characterize them and to evaluate their antihyperalgesic activity. Physicochemical characterization was performed by X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and Fourier Transformed Infrared (FTIR) spectroscopy. In order to evaluate the hyperalgesia of the ASD, sciatic nerve crush injury (NCI) was induced in mice followed by administration of the ASD, where three parameters were evaluated: mechanical and thermal hyperalgesia as well as grip strength. XRD and SEM showed that ASD of HA with HPMC obtained by kneading (KND) presented an amorphous profile, unlike the others polymers, indicating interaction between HA and HPMC. FTIR analysis evidenced the strong interaction between HA and HPMC. Although the results of mechanical hyperalgesia were slightly improved on the groups treated with ASD of HA with HPMC, the thermal hyperalgesia showed that the incorporation of HA into HPMC matrix significantly improved its antinociceptive activity.

Evaluation of the antibacterial activity of Hecogenin Acetate and its inhibitory potential of NorA and MepA efflux pumps from Staphylococcus aureus

Microb Pathog 2023 Jan;174:105925.PMID:36462578DOI:10.1016/j.micpath.2022.105925.

Antimicrobial drugs are of great importance in the control of bacterial infections. Its indiscriminate use contributes to the consolidation of bacterial resistance. Its applicability is due to its secondary metabolites, such as saponins, which are compounds with relevant antibacterial action. Hecogenin Acetate is a saponin present in plants of the agave genus with analgesic, antioxidant, antinociceptive, cardioactive, anticancer, antifungal and antimicrobial activity. The present work aimed to identify the antibacterial activity of Hecogenin Acetate against strains of E. coli, P. aeruginosa and S. aureus and to investigate the NorA and MepA efflux pump inhibitory activity of S. aureus strains. The Minimum Inhibitory Concentration was evaluated by broth microdilution. The Antibiotic Activity Modifier effect and the assessment of efflux pump inhibition were evaluated by microdilution with sub-inhibitory concentrations. Hecogenin Acetate showed minimal inhibitory concentration without significant relevance. In the evaluation of the potentiating activity of the antibiotic action, a greater antagonistic behavior is noticed. In the analyzes performed with the efflux pump, it was noticed that the Hecogenin Acetate does not interfere in the efflux pump mechanism of the analyzed bacteria.

Role of peripheral and central sensitization in the anti-hyperalgesic effect of Hecogenin Acetate, an acetylated sapogenin, complexed with β-cyclodextrin: Involvement of NFκB and p38 MAPK pathways

Neuropharmacology 2021 Mar 15;186:108395.PMID:33516738DOI:10.1016/j.neuropharm.2020.108395.

Neuropathic pain develops due to injury to the somatosensory system, affecting the patient's quality of life. In view of the ineffectiveness of the current pharmacotherapy, substances obtained from natural products (NPs) are a promising alternative. One NP that has been discussed in the literature is Hecogenin Acetate (HA), a steroidal sapogenin with anti-inflammatory and antinociceptive activity. However, HA has low water solubility, which affects its bioavailability. Thus, the objective of this study was to evaluate the anti-hyperalgesic activity of pure and complexed Hecogenin Acetate (HA/βCD) in an animal model of chronic neuropathic and inflammatory pain. The inclusion complex was prepared at a molar ratio of 1:2 (HA:βCD) by the lyophilization method. For the induction of chronic inflammatory pain, the mice received an intraplantar injection of CFA (complete Freund's adjuvant), and were evaluated for mechanical hyperalgesia and for the levels of myeloperoxidase (MPO) in the skin of the paw after eight days of treatment. HA and HA/βCD reduced mechanical hyperalgesia in relation to the vehicle group until the fourth and fifth hours, respectively, in the acute evaluation, with a superior effect of the complexed form over the pure form in the second and third hour after treatment (p < 0.001). In the chronic evaluation, HA and HA/βCD reduced hyperalgesia in relation to the vehicle in the eight days of treatment (p < 0.001). Both pure (p < 0.01) and complexed (p < 0.001) forms reduced myeloperoxidase activity in the skin of the animals' paw. Groups of animals subjected to the same pharmacological protocol were submitted to the partial sciatic nerve ligation (PSNL) model and evaluated for mechanical and thermal hyperalgesia, and cold allodynia. HA and HA/βCD reduced mechanical hyperalgesia until the fourth and sixth hours, respectively, and both reduced hyperalgesia in relation to the vehicle in the chronic evaluation (p < 0.001). HA and HA/βCD also reduced thermal hyperalgesia and cold allodynia (p < 0.05 and p < 0.001, respectively). The analysis of the spinal cord of these animals showed a decrease in the levels of the pro-inflammatory cytokines TNF-α, IL-1β and IL-6 and a reduction in the phosphorylation of NFκB and p38MAPK, as well as a decrease in microglioses compared to the vehicle group. In addition, HA/βCD reduced the nociception induced by intraplantar injection of agonist TRPA1 (p < 0.01) and TRPM8 (p < 0.05). Treatment for eight days with HA and HA/βCD showed no signs of gastric or liver damage. HA and HA/βCD were, therefore, shown to have antinociceptive effects in chronic pain models. Based on our exploration of the mechanisms of the action of HA, these effects are likely to be related to inhibited leukocyte migration, interaction with the TRPA1 and TRPM8 receptors, reduced pro-inflammatory cytokines levels, microglial expression and suppression of NF-κB p65 and p38 MAPK pathway signaling. Therefore, HA/βCD has great potential for use in the treatment of chronic pain.