alpha-Spinasterol

alpha-Spinasterol
Product Name alpha-Spinasterol
CAS No.: 481-18-5
Catalog No.: CFN98748
Molecular Formula: C29H48O
Molecular Weight: 412.7 g/mol
Purity: >=98%
Type of Compound: Steroids
Physical Desc.: Powder
Targets: TRPV | HMG-CoA reductase
Source: The roots of Bupleurum chinense DC.
Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Price: $218/10mg
Alpha-Spinasterol is a novel efficacious and safe antagonist of the TRPV1 receptor with anti-inflammatory and antinociceptive effects.Alpha-Spinasterol has a significant therapeutic potential to modulate the development and/or progression of diabetic nephropathy. It also can prevent TP-induced prostatic hyperplasia and may be beneficial in the management of benign prostatic hyperplasia.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

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The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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    Fitoterapia . 2017 Jun;119:12-19.
    A novel method for synthesis of α-spinasterol and its antibacterial activities in combination with ceftiofur[Pubmed: 28351722]
    Abstract In this study, we designed a novel method of the synthesis of α-spinasterol from commercially available stigmasterol and explored the combinational effect of the α-spinasterol with ceftiofur in vitro against S. pullorum cvcc533, S. pneumoniae CAU0070, E. coli, and S. aureus. α-Spinasterol was obtained by a key reaction of Bamford-Stevens reaction with a desirable yield for five steps. The combination of α-spinasterol and ceftiofur showed stronger synergetic effect against the four pathogenic strains compared with that of stigmasterol and ceftiofur alone. In time-kill analyses, at concentrations above the MICs, ceftiofur in combination with α-spinasterol exhibited time-dependency and concentration-dependency comparing to time dependency with ceftiofur alone. We conclude that the combination usage of α-spinasterol and ceftiofur is an effective and promising strategy against the four pathogenic bacterial strains in vitro. Keywords: Antibacterial activity; Ceftiofur; Stigmasterol; α-Spinasterol.
    Mol Med Rep. 2014 Jun;9(6):2362-6.
    α-Spinasterol from Melandrium firmum attenuates benign prostatic hyperplasia in a rat model.[Pubmed: 24682042]
    Spinasterol, a biologically active compound, exhibits a number of pharmacological activities, including antitumor, antiulcerogenic and anticarcinogenic activity, and originates from the aerial parts of Aster scaber Thunb (Asteraceae). The present study investigated whether alpha-Spinasterol isolated from Melandrium firmum Rohrbach could prevent benign prostatic hyperplasia (BPH) induced by testosterone propionate (TP) in rats.
    METHODS AND RESULTS:
    Male Wistar rats were randomly divided into four groups of eight rats following castration. A negative control group received subcutaneous injections of corn oil. Treatments were administered orally 1 h prior to TP injection. All the rats were sacrificed at the scheduled termination time and their prostates were removed, cleaned and weighed. The prostate size ratio (prostate weight/rat body weight) was then calculated. Additional histopathological examinations were conducted, and the levels of TP and dihydrotestosterone (DHT) in the serum and prostate were measured. TP significantly increased the prostate size ratio (P<0.01), and DHT and testosterone levels in the serum and prostate. The TP-induced increase was significantly inhibited in alpha-Spinasterol-treated rats when compared with the negative controls (P<0.05). In addition, histopathological examination demonstrated that α-spinasterol treatment suppressed TP-induced prostatic hyperplasia.
    CONCLUSIONS:
    It is concluded that alpha-Spinasterol can prevent TP-induced prostatic hyperplasia and may be beneficial in the management of BPH.
    J Ethnopharmacol. 2014;151(1):144-50.
    Anti-inflammatory action of hydroalcoholic extract, dichloromethane fraction and steroid α-spinasterol from Polygala sabulosa in LPS-induced peritonitis in mice.[Pubmed: 24161429]
    Polygala sabulosa A. W. Bennett is a small herb popularly known as "timutu-pinheirinho" that is widely distributed in southern Brazil and that is used to treat disorders of the bowel and kidney and as a topical anesthetic and expectorant in folk medicine. This study was designed to investigate the anti-inflammatory properties of the hydroalcoholic extract (HEPs), CH2Cl2 fraction and the steroid α-spinasterol obtained from the aerial parts of Polygala sabulosa in a model of acute inflammation induced by intraperitoneal injection of bacterial lipopolysaccharide in mice.
    METHODS AND RESULTS:
    The anti-inflammatory effect of HEPs (3-300 mg/kg, i.g.), CH2Cl2 fraction (0.003-30 mg/kg, i.g.) and steroid α-spinasterol (0.001-1mg/kg, i.p. or 1-10mg/kg, i.g.), were evaluated in mice subjected to the acute inflammation caused by intraperitoneal (i.p.) injection of lipopolysaccharide (LPS, 0.02 µg/kg). The anti-inflammatory activity of the HEPs, CH2Cl2 fraction and steroid were assessed by determining the total numbers of leukocytes and differential cell counts (neutrophils and mononuclear cells) and levels of pro-inflammatory (IL-1β, TNF-α, IL-6) or anti-inflammatory (IL-10) cytokines in peritoneal fluid. The administration of HEPs (3-300 mg/kg, i.g.) completely inhibited inflammatory cell infiltration (300 mg/kg, i.g.) and it reduced TNF-α (100-300 mg/kg) and IL-1β (100mg/kg) levels in LPS-injected mice. Furthermore, the administration of CH2Cl2 fraction (0.003-30 mg/kg, i.g.) or α-spinasterol (0.001-10mg/kg, by i.p. or i.g.) significantly reduces inflammatory cell infiltration in LPS-injected mice. Moreover, dexamethasone (0.5mg/kg, i.p., used as a positive control) inhibited inflammatory cell infiltration and reduced the levels of TNF-α, IL-1β and IL-6 in LPS-injected mice.
    CONCLUSIONS:
    Taken together, these results provide the first experimental evidence demonstrating that HEPs have significant anti-inflammatory effects on LPS-induced inflammation. These effects appear to be, at least in part, due to the presence of α-spinasterol. These findings support the widespread use of Polygala sabulosa in popular medicine and demonstrate that this plant has therapeutic potential for the development of phytomedicines with anti-inflammatory properties.
    Planta Med. 2004 Aug;70(8):736-9.
    alpha-Spinasterol isolated from the root of Phytolacca americana and its pharmacological property on diabetic nephropathy.[Pubmed: 15326549 ]

    METHODS AND RESULTS:
    Based on an inhibitory activity-guided fractionation for the high glucose-induced proliferation of glomerular mesangial cells (GMCs), chloroform extracts of the roots of Phytolacca americana were found to contain alpha-Spinasterol (C (29)H (48)O), a delta (7)-sterol. This phytosterol proved to be a potent inhibitor (IC (50) = 3.9 x 10 (-12) g/mL, 9.5 pmol/L) of glomerular mesangial cell proliferation caused by high-ambient glucose (5.6 mM vs. 25 mM), and its inhibitory potency was about 1,000 times higher than that of simvastatin, an HMG-CoA reductase inhibitor used as a positive control. alpha-Spinasterol also significantly reduced the increases of serum triglycerides, renal weight and urinary protein excretion in streptozotocin-induced diabetic mice, and these were comparable to the results observed in insulin-treated diabetic mice.
    CONCLUSIONS:
    Therefore, the results obtained in this study suggest that alpha-Spinasterol has a significant therapeutic potential to modulate the development and/or progression of diabetic nephropathy.
    Br J Pharmacol . 2017 Dec;174(23):4247-4262.
    α-Spinasterol: a COX inhibitor and a transient receptor potential vanilloid 1 antagonist presents an antinociceptive effect in clinically relevant models of pain in mice[Pubmed: 28849589]
    Abstract Background and purpose: Postoperative pain is one of the most common manifestations of acute pain and is an important problem faced by patients after surgery. Moreover, neuronal trauma or chemotherapeutic treatment often causes neuropathic pain, which induces disabling and distressing symptoms. At present, treatments of both painful conditions are inadequate. α-Spinasterol, which is well characterized as a transient receptor potential vanilloid 1 antagonist, has anti-inflammatory, antioxidant and antinociceptive effects. Therefore, we investigated its antinociceptive potential on postoperative and neuropathic pain, as well as its effect on COX-1 and COX-2 activities. Experimental approach: Nociceptive responses in a postoperative pain model (surgical incision-induced) or different neuropathic pain models (trauma or chemotherapy-induced) were investigated in mice. Key results: Oral administration of α-spinasterol reduced postoperative pain, when given as a pre- (0.5 h before incision) or post-treatment (0.5 h after incision), and reduced cell infiltration in the injured tissue. α-Spinasterol also reduced the mechanical allodynia induced by partial sciatic nerve ligation and the mechanical and cold allodynia induced by paclitaxel. Moreover, α-spinasterol inhibited COX-1 and COX-2 enzyme activities without altering the body temperature of animals. Importantly, α-spinasterol did not alter spontaneous or forced locomotor activity. Furthermore, it did not cause gastric damage or liver and kidney changes, nor did it alter cell viability in the cerebral cortex and spinal cord slices of mice. Conclusion and implications: α-Spinasterol is an effective and safe COX inhibitor with antinociceptive effects in postoperative and neuropathic pain models. Therefore, it is an interesting prototype for the development of novel analgesic drugs.
    J Pharmacol Exp Ther. 2012 Nov;343(2):258-69.
    Identification of the plant steroid α-spinasterol as a novel transient receptor potential vanilloid 1 antagonist with antinociceptive properties.[Pubmed: 22837009]
    The transient receptor potential vanilloid 1 (TRPV1) receptor is relevant to the perception of noxious information and has been studied as a therapeutic target for the development of new analgesics. The goal of this study was to perform in vivo and in vitro screens to identify novel, efficacious, and safe TRPV1 antagonists isolated from leaves of the medicinal plant Vernonia tweedieana Baker.
    METHODS AND RESULTS:
    All of the fractions and the hydroalcoholic extract produced antinociception in mice during the capsaicin test, but the dichloromethane fraction also had antioedematogenic effect. Among the compounds isolated from the dichloromethane fraction, only alpha-Spinasterol reduced the nociception and edema induced by capsaicin injection. Moreover, α-spinasterol demonstrated good oral absorption and high penetration into the brain and spinal cord of mice. alpha-Spinasterol was able to displace [3H]resiniferatoxin binding and diminish calcium influx mediated by capsaicin. Oral administration of the dichloromethane fraction and alpha-Spinasterol also produced antinociceptive effect in the noxious heat-induced nociception test; however, they did not change the mechanical threshold of naive mice. The treatment with α-spinasterol did not produce antinociceptive effect in mice systemically pretreated with resiniferatoxin. In addition, alpha-Spinasterol and the dichloromethane fraction reduced the edema, mechanical, and heat hyperalgesia elicited by complete Freund's adjuvant paw injection. The dichloromethane fraction and alpha-Spinasterol did not affect body temperature or locomotor activity.
    CONCLUSIONS:
    In conclusion, alpha-Spinasterol is a novel efficacious and safe antagonist of the TRPV1 receptor with antinociceptive effect.
    J Neural Transm (Vienna). 2015 Sep;122(9):1239-47.
    α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice.[Pubmed: 25764210]
    alpha-Spinasterol is a plant-derived compound which was reported to act as a selective antagonist for the transient receptor potential vanilloid 1 (TRPV1) receptor. Several studies revealed that the TRPV1 receptors might modulate seizure activity in animal models of seizures and epilepsy.
    METHODS AND RESULTS:
    The aim of the present study was to investigate the effect of alpha-Spinasterol on the seizure threshold in three acute models of seizures, i.e., in the intravenous (i.v.) pentylenetetrazole (PTZ) seizure test, in the maximal electroshock seizure threshold (MEST) test and in the model of psychomotor seizures induced by 6 Hz stimulation in mice. Our results revealed significant anticonvulsant effect of alpha-Spinasterol in all the used seizure tests. In the i.v. PTZ test, statistically significant elevation was noted in case of the threshold for myoclonic twitches (doses of 0.1-1 mg/kg) and generalized clonus seizures (doses of 0.5 and 1 mg/kg) but not for tonic seizures. The studied TRPV1 antagonist also increased the threshold for tonic hindlimb extension in the MEST (doses of 0.5 and 1 mg/kg) and 6 Hz psychomotor seizure (doses of 0.1 and 0.5 mg/kg) tests in mice. Furthermore, alpha-Spinasterol did not produce any significant impairment of motor coordination (assessed in the chimney test) and muscular strength (investigated in the grip-strength test) and it did not provoke significant changes in body temperature in mice.
    CONCLUSIONS:
    Based on the results of our study and the fact that alpha-Spinasterol is characterized by good blood-brain permeability, we postulate further investigation of this compound to precisely evaluate mechanism of its anticonvulsant action and opportunity of its usage in clinical practice.
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