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Veratramine
Computational and Mathematical Methods in Medicine · 2022 · IF 2.809

Pharmacokinetics of Veratramine and Jervine from Alcohol Extracts of Radix Veratri

Song Wang,Jiali Cui,Gaoqiong Zhao,Hongbin Liu,Jingkun Wang

Background. Chinese Materia Medica and Jiangsu New Medical College record that Radix Veratri root is Liliaceae Veratrum taliense Loses. f. and the root of Veratrum stenophyllum Diels. According to traditional Chinese medicine (TCM) example, Radix Veratri is a Liliaceae plant Veratrum taliense. Another literature pointed out that the aliases of Veratrum taliense and Veratrum angustifolia are both Radix Veratri, and their effects are basically the same. The main active ingredient of Veratrum is veratramine, of which veratramine and Jervine are higher in content, reaching 24.60% and 21.28% of the total alkaloids, respectively. Veratrum alkaloids are both toxic and effective ingredients. In addition to its good clinical efficacy, attention should also be paid to its pharmacokinetic characteristics in vivo. It is particularly important to study the pharmacokinetic characteristics of veratramine and Jervine in vivo. Objective. The goal of this study was to develop a simple and effective method for measuring veratramine and Jervine in rat plasma at the same time. This method was used to study the pharmacokinetic characteristics of veratramine and Jervine in the alcohol extract of Radix Veratri in rats, to provide a reasonable basis for the clinical use of Radix Veratri. Methods. Eighteen SD rats were randomly assigned into three groups, half male and half female, and were given 0.04 g/kg, 0.08g/kg, and 0.16 g/kg Radix Veratri alcohol extract, respectively. Blood samples were collected at different time points and were analyzed by LC-MS/MS after protein precipitation. Bullatine was set as the internal standard; the plasma samples were extracted with ethyl acetate. After the sample was processed, acetonitrile-10 mM ammonium acetate, whose pH was adjusted to 8.8 with ammonia water, was taken as the mobile phase. Veratramine quantitative ion pair was , Jervine quantitative ion pair was , and Bullatine B (IS) quantitative ion pair was . In the positive ion mode, the multireaction monitoring (MRM) mode was used to determine the blood concentration of veratramine and Jervine. DAS 3.3.0 was used to calculate the relevant pharmacokinetic parameters. Results. Veratramine had a good linear relationship in the concentration range of 0.0745~18.2 ng/mL, and that of Jervine was 1.11~108 ng/mL. The correlation coefficient of three consecutive batches of the standard curve was greater than 0.995. Veratramine’s lower quantification limit was 0.745 ng/mL, Jervine’s was 1.11 ng/mL, and precision and accuracy were both less than 15%. The accuracy of veratramine was between 88.96% and 101.85%, and the accuracy of Jervine was between 92.96% and 104.50%. This method was adopted for the pharmacokinetic study of alcohol extracts of Radix Veratri. The results showed that only of veratramine female rats did not show linear kinetic characteristics in the dose range of Radix Veratri alcohol extract from 0.04 g/kg to 0.16 g/kg. For and of veratramine and Jervine, it could not determine whether the Radix Veratri alcohol extract showed linear kinetic characteristics within the dosage range of 0.04 g/kg~0.16 g/kg. Veratramine and Jervine showed obvious gender differences in the absorption and elimination stages. The absorption rate of veratramine and Jervine by male mice was about 10 times higher than that of female mice, and the elimination rate of male mice is about 20 times lower than that of female mice. It was suggested that the clinical application of the steroidal alkaloids veratramine and Jervine in Radix Veratri required rational use of drugs based on gender. Conclusion. An LC-MS/MS analysis method suitable for the pharmacokinetic study of veratramine and Jervine in Radix Veratri in SD rats was established to provide a basis for in vivo pharmacokinetic studies. The pharmacokinetic characteristics of veratramine and Jervine in the alcohol extract of Radix Veratri were significantly different in female and male rats. During the clinical use of Radix Veratri, it should pay close attention to the obvious gender differences that may occur after the medication.

CAS / MDL: 631-61-8 9041-08-1
研究领域: 中药学 · 药理学 · 分析化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ETHNOPHARMACOLOGY · 2019 · IF 3.414

Seven new veratramine-type alkaloids with potent analgesic effect from Veratrum taliense

Qiong Li,Yun-Li Zhao,Cheng-Bo Long,Pei-Feng Zhu,Ya-Ping Liu,Xiao-Dong Luo

Ethnopharmacological relevance Veratrum taliense is traditionally used TCMs in Yunnan province of China for pain and inflammation. Previous research and clinical applications have shown that V. taliense had significant analgesic activity. Jevine-type alkaloids were shown to be one of the anti-inflammatory and analgesic agents from V. taliense . However, other types of compounds from V. taliense related to its traditional use remains unknown. Aim of the study To identify veratramine-type steroidal alkaloids with analgesic effects from the roots and rhizomes of V. taliense . Materials and methods Compounds were isolated from the roots and rhizomes of V. taliense by chromatographic separation. Their structures were elucidated based on UV, IR, NMR and MS spectra data. Analgesic activity was assessed with acetic acid-induced writhing in mice model. Results Seven new veratramine-type alkaloids were isolated from the roots and rhizomes of V. taliense . They all exhibited significant analgesic activity, of which alkaloids 1 and 4 were more potent antalgic than the well-known analgesic drug, pethidine . Conclusions The veratramine-type alkaloids from V. taliense may serve as new leads for the discovery of analgesic drugs.

研究领域: 民族药理学 · 天然产物化学 · 植物化学 · 疼痛研究 · 药用植物
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MOLECULAR AND CELLULAR BIOCHEMISTRY · 2026 · IF 4.7

Targeting the Wnt/β-catenin pathway: veratramine mitigates MNNG-induced gastric precancerous lesions

Zhang Pan,Sun Xuelin,Liu Longteng,Zhang Yatong,Bo Jiaqi,Huang Wenli,Na Yifan,Zhang Jingyi,Qin Xiaoyun,Luo Qingfeng

Gastric precancerous lesions (GPLs) are a pivotal stage in the gastritis-gastric cancer sequence, and the absence of effective treatments presents a clinical challenge. Veratramine is a natural anti-inflammatory and analgesic steroid alkaloid; however, its effects on GPLs and the mechanisms have remained unexplored. This study investigated the effects of veratramine on GPLs using 1-Methyl-3-nitro-1-nitrosoguanidine (MNNG)-induced GES-1 cells and rat models, utilizing RNA-seq to elucidate the underlying mechanisms. In vitro, veratramine inhibited malignant cells (MC) proliferation, induced apoptosis, and triggered G0/G1 cell cycle arrest. It also suppressed epithelial-mesenchymal transition (EMT), migration, and invasion by upregulating E‑cadherin and downregulating Slug and vimentin. Transcriptomic and molecular docking analyses highlighted the Wnt/β-catenin pathway as a key target, regulated via DDX60, MUC1, APOL1, and MSH5. Veratramine reduced Wnt10B, β-catenin, and cyclin D1 expression and blocked β‑catenin nuclear translocation; these effects were reversed by the Wnt activator BML-284. In vivo, treatment with veratramine ameliorated the GPLs-induced pathological changes in rats. It restored body weight and preserved gastric mucosal integrity, as evidenced by intact glandular and cellular morphology, reduced hyperplasia, and attenuated intestinal metaplasia. These improvements were associated with a modulation of key molecular markers, specifically a decrease in the expression of N-cadherin, Wnt10B, and β-catenin, alongside an increase in E-cadherin expression in gastric tissues. These results collectively indicate that veratramine exerts its therapeutic effects against GPLs primarily by suppressing the Wnt/β-catenin signaling pathway. Taken together, our findings suggest that veratramine is a promising candidate small-molecule drug for the treatment of GPLs.

CAS / MDL: 1330-20-7 28718-90-3
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ACS Applied Nano Materials · 2025 · IF 5.5

Designing Veratramine Nanopesticide with Strong Adhesion Performance and Plant Uptake for Efficient Control toward Multiple Target Pests

Jingyi Chen,Yuankang Guo,Yajie He,Meizhen Yin,Xiangge Du,Jixing Xia,Jie Shen,Min Dong,Shuo Yan

Botanical pesticides are promising alternatives for sustainable pest management due to their environmental compatibility, biodegradability, and multitarget mechanisms that help delay pest resistance. Unfortunately, most botanical pesticides face challenges such as limited water solubility and poor foliar adhesion, thereby limiting their large-scale field application. Herein, the star polycation (SPc) nanocarrier and X-100 surfactant were introduced to successfully develop an efficient nanodelivery platform for veratramine (VAM). The SPc could spontaneously assemble with VAM via a hydrogen bond and van der Waals force, and the integration of Triton X-100 stabilized the nanoscale size (84 nm) to prepare a VAM nanopesticide. Interestingly, this optimized system reduced the contact angle and increased the retention of VAM on plant leaves while remarkably facilitating its systemic transport through roots and leaves. Compared to commercial VAM, the VAM nanopesticide showed stronger contact and stomach toxicity against multiple pest species such as aphids, thrips, and mites, which exhibited fast-acting properties in the field with high control efficacy even at 7 d after the spraying. Subsequently, the RNA-seq and biological experiments demonstrated that the application of VAM nanopesticide influenced various pathways in aphids, inducing starch and sucrose metabolism, protein digestion and absorption, etc., with inhibitory effects on the biosynthesis of trehalose and protein. Importantly, the application of the VAM nanopesticide did not adversely influence the predatory lady beetles or cowpea seedlings, confirming its safety in actual applications. Overall, our work addressed the formulation instability and environmental loss of VAM while ensuring its ecological safety, which offered a scalable nanoplatform to optimize botanical pesticides for enhanced efficacy and minimized ecological risks.

CAS / MDL: 60-70-8
研究领域: 农学 · 纳米技术 · 昆虫学 · 植物保护 · 环境毒理学 · 生物信息学
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