Aconite Root Research Articles

Aconite-Induced Metamorphosis From Beauty to Ugliness in a Japanese Tale.

The authors present a narrative that details the cause and process of a woman's transformation from beauty to ugliness in a Japanese tale. In " Tokaido Yotsuya Kaidan ," the metamorphosis from a beauty to an ugly woman is analyzed. After taking medication to recover from childbirth, Oiwa's face became disfigured and grotesque. Oiwa: It seems to be good for my blood, but when I drink it, it causes fraying and breakdown, causing sudden pain. I feel a numbing dullness. When she looked at herself in the mirror, she was shocked. Oiwa: What's wrong with my face? I hate this, it's such a disgusting thing. Neighbor: It was a lie that the medicine you drank was a helpful medicine that protects the appearance of people's faces. Your face is that of a wicked woman (). Oiwa: Is it really me? Why does she have the face of an evil woman? Her hair falls out in a gruesome combing scene, driving her mad. The poison Oiwa took was aconite, which grows wild in Japan. Both aconite tincture and raw aconite roots contain high concentrations of Aconitum alkaloids, which can penetrate the stratum corneum following the diffusion gradient. As her hair fell out during a horrific combing session, she abandoned her maternal role and sought revenge, having lost what she considered a symbol of her femininity. In treating female patients with facial disfigurement, it is important to be mindful of their psychological state, akin to that of Oiwa, who became disfigured through no fault of her own.

Cardiotoxic effects of poisoning from aconite root in a middle-aged man in Bhutan: a case report

Cardiotoxic effects of poisoning from aconite root in a middle-aged man in Bhutan: a case report

Transdermal Delivery of Polymeric Nanoparticles Containing Aconite Root for the Treatment of Chemotherapy‐Induced Peripheral Neuropathy

Chemotherapy‐induced peripheral neuropathy (CIPN) poses challenges like pain and numbness, necessitating innovative treatments due to current limitations. Conventional approaches, relying on pain relief medications and dose adjustments, fall short in addressing neurotoxicity, resulting in inadequate pain relief and undesired effects. Aconite root (AR), a medicinal herb withcenturies of use against various diseases, contains a compound named Aconine, which alleviates pain by blocking specific neural channels. However, AR also contains Aconitine, a toxic substance hydrolyzed into nontoxic Aconine through heating. Herein, hyaluronate‐poly(lactic‐co‐glycolic acid) nanoparticles (HA‐PLGA/AR NPs) encapsulating Aconine are fabricated, enabling controlled release, protection, and transdermal delivery, enhancing therapeutic outcomes. High‐performance liquid chromatography identifies optimal Aconine content after 48 h of AR boiling, with minimal neural toxicity confirmed. Characterization via transmission electron microscopy, dynamic light scattering, and in vitro assays demonstrates superior drug release by HA‐PLGA/AR NPs, establishing effective transdermal Aconine delivery. In an in vitro CIPN model with paclitaxel (PTX)‐treated PC12 cells, HA‐PLGA/AR NPs stimulate enhanced neurite growth, validating their localized analgesic impact on CIPN and suggesting potential symptom alleviation. Taken together, HA‐PLGA/AR NPs offer a promising strategy for controlled transdermal Aconine delivery, potentially alleviating CIPN and addressing various neuropathies and diseases.

Quantitative Determination Method of Aconitum Monoester Alkaloids Using Relative Molar Sensitivity (RMS) for the Assay in the Japanese Pharmacopoeia

Recently, a novel quantitative method using relative molar sensitivity (RMS) was applied to quantify the ingredients of drugs and foods. An important development in this regard can be observed in the Japanese Pharmacopoeia (JP) 18, where the quantification of perillaldehyde, an unstable compound, in crude drug "Perilla Herb", was revised to incorporate the RMS method.In this study, the primary objective was to improve the tester safety and reduce the amount of reagents used in the JP test. To achieve this, the quantification of three toxic Aconitum monoester alkaloids (AMAs) was explored using the RMS method, employing a single reference compound for all three targets. These AMAs, namely benzoylmesaconine hydrochloride, benzoylhypaconine hydrochloride, and 14-anisoylaconine hydrochloride, which are the quantitative compounds of Kampo extracts containing Aconite Root (AR), were quantified using the reference compound benzoic acid (BA). Reliable RMS values were obtained using both 1H-quantitative NMR and HPLC/UV. Using the RMS of three AMAs relative to the BA, the AMA content (%) in commercial AMAs quantitative reagents were determined without analytical standards. Moreover, the quantitative values of AMAs using the RMS method and the calibration curve method using the three analytical standards were similar. Additionally, similar values were achieved for the three AMAs in the Kampo extracts containing AR using the RMS and the modified JP18 calibration curve methods. These results suggest that the RMS method is suitable for quantitative assays of the Kampo extracts containing AR and can serve as an alternative to the current method specified in the JP18.

Acute Traditional Chinese Medicine Fuzi Poisoning: A Case Report

Fuzi is lateral root of aconite crowfoot plants of aconite root of processed products, its medicinal sheen, sweet, hot, toxic, authority and by the kidney, spleen, for "back to Yang inverse first to save medicine", there are back to Yang Yang to save inverse, fire, cold analgesic effect, modern pharmacology study anti-inflammatory analgesic, cardiac, anti-aging and other functions, is the doctor of traditional Chinese medicine clinical commonly used drugs, often used in the treatment of cardiovascular diseases, diseases such as rheumatoid arthritis. According to different machining processing technology can be divided into salted aconite root, Heishun tablet, Baishun tablets, Light monkshood tablet, etc. Clinical use of Fuzi is often after processing and attenuation, but poisoning still occurs from time to time. A case of poisoning caused by taking Fuzi in our hospital is reported as follows.

Identification of antagonistic fungi and their antifungal activities against aconite root rot pathogens

ABSTRACT Root rot is one of the main diseases affecting Aconitum carmichaelii Debx. during cultivation, seriously limiting yields of this herb. Currently, there is no effective control measure for aconite root rot. The antifungal activities of antagonistic strains against aconite root rot pathogens (Fusarium proliferatum, Fusarium solani, and Fusarium oxysporum) were investigated in this study. Three antagonistic strains, JKT7, JKT28 and JKT39, were screened and identified as Trichoderma asperellum, Trichoderma hamatum and Trichoderma virens, respectively. Dual culture tests showed that the inhibition rates of the three Trichoderma strains on the pathogens were all approximately 70%. The volatile metabolites had inhibitory effects on the mycelial growth of pathogens, while the nonvolatile metabolites in the culture filtrates did not show significant inhibitory effects. The volatile components analyzed by GC‒MS were mainly ketones, esters, and alcohols. These results indicate that these strains of Trichoderma and their secondary metabolites have antimicrobial activities against the pathogens of aconite root rot. This study could provide a scientific basis for the biocontrol of aconite root rot.

Aconitum carmichaelii triggers neurotoxicity and Parkinson‐like symptoms through initiation of ROS‐mitochondrial apoptosis and the Nox5/DJ‐1 signaling pathway

AbstractBackground Aconitum carmichaelii, the mother root of Aconitum, has a long‐applied history for treating many diseases in China. Increased use of it has prompted significant concerns regarding its extensive cardiotoxicity and neurotoxicity. The molecular mechanisms underlying A. carmichaelii‐induced neurotoxicity are poorly understood.MethodsWe took advantage of the zebrafish model to investigate the neurotoxic mechanism of A. carmichaelii. In addition to the behavior and neuronal activity testing, gene expression of neuronal oxidative stress, and apoptosis levels were also analyzed.ResultsIn contrast to the excitatory effect of low‐dose A. carmichaelii decoction, hypoactivity of locomotor behavior, and neural activity, especially telencephalon, were detected in the 20 mg/mL group. High doses of A. carmichaelii induced excessive ROS by downregulating DJ‐1 and activating Nox5, and further triggered cell apoptosis through the bax/bcl2a‐caspase‐9 pathway in zebrafish larva. Mitochondrial protection‐related genes PinK1 and Parkin were upregulated to protect against mitochondrial dysfunction during cellular stress. The ROS scavenger‐NAC significantly alleviated neurotoxicity in the 20 mg/mL group.ConclusionThe study reveals the potential mechanism of A. carmichaelii‐induced neurotoxicity and provides new insights into a significant risk marker of A. carmichaelii poisoning.

Aconitum Alkaloid Songorine Exerts Potent Gamma-Aminobutyric Acid-A Receptor Agonist Action In Vivo and Effectively Decreases Anxiety without Adverse Sedative or Psychomotor Effects in the Rat.

Songorine (SON) is a diterpenoid alkaloid from Aconitum plants. Preparations of Aconitum roots have been employed in traditional oriental herbal medicine, however, their mechanisms of action are still unclear. Since GABA-receptors are possible brain targets of SON, we investigated which subtypes of GABA-receptors contribute to the effects of SON, and how SON affects anxiety-like trait behavior and psychomotor cognitive performance of rats. First, we investigated the effects of microiontophoretically applied SON alone and combined with GABA-receptor agents picrotoxin and saclofen on neuronal firing activity in various brain areas. Next, putative anxiolytic effects of SON (1.0–3.0 mg/kg) were tested against the GABA-receptor positive allosteric modulator reference compound diazepam (1.0–5.0 mg/kg) in the elevated zero maze (EOM). Furthermore, basic cognitive effects were assessed in a rodent version of the psychomotor vigilance task (PVT). Local application of SON predominantly inhibited the firing activity of neurons. This inhibitory effect of SON was successfully blocked by GABA(A)-receptor antagonist picrotoxin but not by GABA(B)-receptor antagonist saclofen. Similar to GABA(A)-receptor positive allosteric modulator diazepam, SON increased the time spent by animals in the open quadrants of the EOM without any signs of adverse psychomotor and cognitive effects observed in the PVT. We showed that, under in vivo conditions, SON acts as a potent GABA(A)-receptor agonist and effectively decreases anxiety without observable side effects. The present findings facilitate the deeper understanding of the mechanism of action and the widespread pharmacological use of diterpene alkaloids in various CNS indications.

An Analysis of Aconiti Ciliare Radix Patents

Objectives: The purpose of this study is to investigate and analyze Korean domestic patents on aconiti ciliare radixand to identify the trend of aconitum tuber technology.Methods: To analyze the patent, a combinations of words such as “aconitum” or “korean aconite root” were usedin search engine Kipris(www.kirpis.or.kr). The patents of aconiti ciliare radix were analyzed in three ways: year trendanalysis, internatonal patent classification (IPC) code analysis related to content classification, and patent registrationstatus analysis.Results: Among the patents found in the search results, 17 patents with significant contents were analyzed. Resultsshowed that, first, patents were steadily registered until 2018, but recently there has been no new patent registration.Second, there were many patents related to efficacy verification and decoction method, and the number of IPC codesrelated to them was also high. Third, there are five patents maintaining the registration status, and they are patentsrelated to the aconiti ciliare radix extraction method, toxicity removal, and combination method.Conclusions: In this study, the domestic patents of aconiti ciliare radix were analyzed. The analysis results of thisstudy are expected to be exploited as basic data for the development of Korean medicine analgesics with fewer sideeffects by suppressing tuber toxicity and the creation of new medical technologies.

Suppressive effects of processed aconite root on dexamethasone-induced muscle ring finger protein-1 expression and its active ingredients

Processed aconite root (PA), the tuberous root of Aconitum carmichaelii prepared by autoclaving, is a crude drug used in Japanese traditional Kampo medicine and traditional Chinese medicine for the symptoms of kidney deficiency, that is related to the muscle atrophy in modern medicine. The objective of the present study is to evaluate the effectiveness of PA on muscle atrophy and to find its active ingredients using dexamethasone-induced muscle ring finger protein-1 (MuRF1) mRNA expression in murine myoblast C2C12 cells. Dexamethasone-induced MuRF1 expression was significantly suppressed by methanol-soluble part of boiling water extract of PA in a concentration-dependent manner with its IC50 value of 1.5 mg/ml. By the activity-guided fractionations of PA extract using the partition between organic solvents and its aqueous solution, the activity of PA did not transfer into the fraction containing aconitine-type diterpenoid alkaloids but into BuOH layer. Then, we found higenamine and salsolinol as the active ingredients in PA. Higenamine and salsolinol significantly suppressed dexamethasone-induced MuRF1 expression, and their IC50 values were 0.49 and 50 µM, respectively. The contents of higenamine and salsolinol in the decoctions of commercially available fourteen PA products are 0.12 and 14 µg/ml as the average values, and varied with the coefficient of variation (CV) values of 97 and 63%, respectively. Higenamine also significantly suppressed dexamethasone-induced mRNA expressions of muscle atrophy F-box protein (MAFbx)/atrogin1, casitas B-lineage lymphoma-b (Cbl-b), troponin, branched-chain amino acid aminotransferase 2 (BCAT2), and Bcl-2 binding and pro-apoptotic protein3 (Bnip3). Although the quality control of PA is regulated by the contents of diterpene alkaloids, salsolinol and higenamine can be used as the marker compounds to certificate the pharmacological activities of PA.Graphical abstract

Analytical Pyrolysis for Valorization of Herbal Pharmaceutical Industry Wastes Excluding Necessity of Preparative Isolation of their Components

The work is devoted to the comprehensive comparative analysis of extraction cakes, obtained after isolation of pharmaceuticals from medical herbs (Aconítum leucostómum, Thermopsis alterniflora, Glycyrrhiza Glabra and Vinca erecta) to characterize their composition and structural features of components, that is necessary for following valorization and for evaluation of extraction efficiency. Application of analytical pyrolysis to analysis of the medical herbs’ residues allowed to avoid disadvantages, connected with preparative isolation of components and get integral information about phytomass constituents and their transformation during extraction. The results have shown that aconite and licorice roots extraction cakes can be considered as perspective raw material for the chemical and biological processing for obtaining of carbohydrates-based products, whereas the periwinkle grass waste is perspective source for obtaining of aromatic and phenolic products. The data of the analytical pyrolysis indicate the сompleteness of biologically active compounds extraction from licorice roots. Extraction cakes of aconite, thermopsis and periwinkle grasses contained different amounts of unextracted targeted pharmaceutical compounds, which can increase their value.

Clinical application of Aconitum carmichaelii Debx. (Fu Zi in Chinese) by traditional Chinese medicine physicians--A cross-sectional questionnaire survey in Beijing

To investigate clinical application of aconite root ( Aconitum carmichaelii Debx.; hereinafter “aconite”) by traditional Chinese medicine (TCM) physicians in TCM hospitals in Beijing and explore the specific use of aconite and the effect of different doses on decoction time. This was a cross-sectional study using two-stage sampling. Questionnaires were administered among TCM physicians from TCM hospitals in Beijing between September 2020 and August 2021. The questionnaire mainly included general demographics, clinical backgrounds of TCM physicians, and clinical application of aconite. The data analyses were performed using SPSS 20.0. A total of 387 questionnaires were collected, of which 385 were valid. Of the 385 participating TCM physicians, 331 (85.97%) used aconite in clinical practice. The top three medical diagnoses treated with aconite were heart failure, diarrhea without cause, and chronic gastritis. The TCM pattern treated most frequently with a high dose of aconite was spleen-kidney yang deficiency, and the TCM pattern treated most frequently with a low dose was spleen yang deficiency, while spleen-kidney yang deficiency was treated most frequently with a common dose of aconite. The top three common formulas were Sini decoction, Mahuang Xixin Fuzi decoction, and Zhenwu decoction. Hei Shun Pian was the most common herbal pieces of aconite. The highest frequency of the maximum dose of aconite was 15 g, that of the minimum dose was 3 g, and that of the common dose was 10 g. There was a certain correlation between decoction time and the dose of aconite. Most TCM physicians advised their patients to take medicine twice a day. In this study, we refined and quantified the use of aconite and enriched the exploration of the clinical application of aconite besides its provisions in the Pharmacopoeia of the People's Republic of China .

A systematic review of pharmacological activities, toxicological mechanisms and pharmacokinetic studies on Aconitum alkaloids.

The tubers and roots of Aconitum (Ranunculaceae) are widely used as heart medicine or analgesic agents for the treatment of coronary heart disease, chronic heart failure, rheumatoid arthritis and neuropathic pain since ancient times. As a type of natural products mainly extracted from Aconitum plants, Aconitum alkaloids have complex chemical structures and exert remarkable biological activity, which are mainly responsible for significant effects of Aconitum plants. The present review is to summarize the progress of the pharmacological, toxicological, and pharmacokinetic studies of Aconitum alkaloids, so as to provide evidence for better clinical application. Research data concerning pharmacological, toxicological and pharmacokinetic studies of Aconitum alkaloids were collected from different scientific databases (PubMed, CNKI, Google Scholar, Baidu Scholar, and Web of Science) using the phrase Aconitum alkaloids, as well as generic synonyms. Aconitum alkaloids are both bioactive compounds and toxic ingredients in Aconitum plants. They produce a wide range of pharmacological activities, including protecting the cardiovascular system, nervous system, and immune system and anti-cancer effects. Notably, Aconitum alkaloids also exert strong cardiac toxicity, neurotoxicity and liver toxicity, which are supported by clinical studies. Finally, pharmacokinetic studies indicated that cytochrome P450 proteins (CYPs) and efflux transporters (ETs) are closely related to the low bioavailability of Aconitum alkaloids and play an important role in their metabolism and detoxification in vivo.

Herbal textual research on Chinese medicine "Fuzi"(Aconiti Lateralis Radix Praeparata.)

To ensure the use of aconite roots as much as possible in accordance with the traditional medication principles, this paper examines the species, origin and processing of the ancient aconite, attempting to provide a basis for the research and development of drugs in the perspective of "Jingdian Mingfang" (Chinese Classical Formulas). The study found that a species discovered after the Tang Dynasty, Aconitum carmichaelii Debx., became the mainstream of this species category. Following the Song Dynasty, this species became the main source of authentic aconite, called "Chuanwu". This species is also currently the source of aconite roots. From this situation, the dry daughter roots of Aconitum carmichaelii Debx. should be considered in the research and development of "Jingdian Mingfang", and the cultivation products of Sichuan Jiangyou and Shanxi Hanzhong as well.

Low back pain with lumbar subcutaneous edema successfully treated using traditional Chinese medicine, including radix astragali

Abstract Introduction: Lumbar subcutaneous edema (LSE) is incidentally found in obese patients during the course of evaluating the cause of low back pain using magnetic resonance imaging (MRI). However, there is no established treatment for LSE, and the mechanism underlying its development is unknown. Patient concerns: A 77- year- old woman presented with chronic low back pain that had persisted for several years. Her BMI was 25.1 kg/m2, which indicates obesity in Japan. Diagnosis: MRI revealed LSE, which extended from the level of the L2 vertebral body to the sacrum. Interventions: We prescribed Maxing Yigan (MYG), a traditional Chinese medicine formula, to which we added powdered cinnamon bark and processed aconite root (hereafter referred to as modified MYG). Outcomes: This treatment was ineffective for six months. We then added Radix Astragali (RA) to the modified MYG. One month later, her low back pain was found to have markedly improved. MRI also confirmed that the LSE decreased remarkably. Conclusions: According to the clinical and MRI findings, modified MYG, including RA, was effective for the treatment of low back pain and LSE. The mechanism underlying the development of LSE could be lymphatic pooling due to perilymphatic inflammation associated with obesity. Modified MYG, including RA, might suppress perilymphatic inflammation and thereby improve lymphatic drainage. Further investigations are required to support this hypothesis.

Adverse Effects of Kampo Medicines.

This review summarizes the adverse effects of Kampo medicines. These adverse effects in terms of immunoallergic reactions include interstitial pneumonia, liver injury, allergic cystitis, and drug eruption. Many cases of interstitial pneumonia, liver injury, and allergic cystitis associated with Kampo formulas have been reported to be caused by formulas containing Scutellariae Radix (Scutellaria root, ogon). The known adverse effects linked to overdose of Kampo formulas include pseudoaldosteronism [caused by Glycyrrhizae Radix (licorice, kanzo)], sympathomimetic symptoms [caused by Ephedrae Herba (ephedra, mao)], aconite poisoning [caused by Aconiti Tuber (processed aconite root, bushi and uzu)], and diarrhea [caused by Rhei Rhizoma (rhubarb, daio)]. In recent years, mesenteric phlebosclerosis caused by the long-term administration of Gardeniae Fructus (gardenia fruit, sanshishi) has also been reported. It is necessary to consider these potential adverse effects when prescribing Kampo medicines in clinical practice.

Analysis on quality value transfer of substance benchmarks of Zhenwu Decoction

By preparing 15 batches of Zhenwu Decoction substance benchmarks,the characteristic map,index component content and paste-forming rate were determined to define the peak attribution,similarity range,paste-forming rate range,paeoniflorin and6-gingerol content range and transfer rate range. The similarity between the substance benchmark characteristic map and the control map R generated from the 15 batches of substance benchmarks was higher than 0. 970. There were 19 characteristic peaks in total. By further summarization of the characteristic peaks,it could be seen that tuckahoe had 3 characteristic peaks,white peony root had 10 characteristic peaks,atractylodes had 3 characteristic peaks,ginger had 1 characteristic peak,and Aconite root had 3 characteristic peaks; among them,white peony root and aconite root had 1 common peak. The contents and transfer rates of the 15 batches were0. 50%-0. 93 and 16. 11%-26. 20%; those for 6-gingerol were 0. 018 2%-0. 033 9% and 13. 16%-24. 10%,respectively. The pasteforming rate ranged from 10. 00% to 14. 85%. In this study,the transfer process of substance benchmark value of classic formula Zhenwu Decoction was analyzed based on the characteristic map,the paste-forming rate and the content of the index components; a scientific and stable substance benchmark quality evaluation method was preliminarily established to provide a basis for subsequent development of classic formula Zhenwu Decoction and quality control of relevant preparations.

Neuropharmacological Effects of Mesaconitine: Evidence from Molecular and Cellular Basis of Neural Circuit.

Mesaconitine (MA), a diester-diterpenoid alkaloid in aconite roots, is considered to be one of the most important bioactive ingredients. In this review, we summarized its neuropharmacological effects, including analgesic effects and antiepileptiform effects. Mesaconitine can act on the central noradrenergic system and the serotonin system; behaving like the norepinephrine reuptake inhibitors and tricyclic antidepressants that increase norepinephrine levels in stress-induced depression. Therefore, the possible perspectives for future studies on the depression of MA were also discussed as well. The pharmacological effect of MA on depression is worthy of further study.

Chinese herbal medicine Baoyuan Jiedu decoction inhibits the accumulation of myeloid derived suppressor cells in pre-metastatic niche of lung via TGF-β/CCL9 pathway

Baoyuan Jiedu (BYJD for short) decoction, a traditional Chinese medicine formula, is composed of Astragalus, Ginseng, Aconite root, Honeysuckle, Angelica, Licorice, which has the functions of nourishing qi and blood, enhancing immune function, improving quality of life and prolonging survival time of tumor patients. The present study aimed to investigate the effect and mechanism of BYJD decoction on reversing the pre-metastatic niche. We showed that BYJD decoction could prolong the survival time of 4T1 tumor-bearing mice. Moreover, we found that the BYJD decoction inhibited the formation of lung pre-metastatic niche and inhibited recruitment of myeloid derived suppressor cells (MDSCs) in the lung. Mechanistically, we showed that the proteins and genes expression of TGF-β, Smad2, Smad3, p-Smad2/3, Smad4, CCL9 in the TGF-β/CCL9 signaling pathway were suppressed by BYJD decoction. In line with the above findings, our results confirm that BYJD decoction inhibits the accumulation of MDSC in pre-metastatic niche of lung via TGF-β/CCL9 pathway.

Neoline, an active ingredient of the processed aconite root in Goshajinkigan formulation, targets Nav1.7 to ameliorate mechanical hyperalgesia in diabetic mice

Ethnopharmacological relevanceGoshajinkigan (GJG), a traditional Japanese Kampo formula, has been shown to exhibit several pharmacological actions, including antinociceptive effects. Processed aconite root (PA), which is considered to be an active ingredient of GJG, has also been demonstrated to have an ameliorative effect on pain, such as diabetic peripheral neuropathic pain. We recently identified neoline as the active ingredient of both GJG and PA that is responsible for its effects against oxaliplatin-induced neuropathic pain in mice. Aim of the studyIn the present study, we investigated whether GJG, PA, and neoline could inhibit Nav1.7 voltage-gated sodium channel (VGSC) current and whether neoline could ameliorate mechanical hyperalgesia in diabetic mice. Materials and methodsTo assess the electrophysiological properties of GJG extract formulation, powdered PA, and neoline on Nav1.7 VGSCs, whole-cell patch clamp recording was performed using human HEK293 cells expressing Nav1.7 VGSCs. In addition, the ameliorative effects of neoline on diabetic peripheral neuropathic pain were evaluated using the von Frey test in streptozotocin (STZ)-induced diabetic model mice. ResultsGJG extract formulation significantly inhibited Nav1.7 VGSC peak current. Powdered PA also inhibited Nav1.7 VGSC peak current. Like GJG and PA, neoline could inhibit Nav1.7 VGSC current. When diabetic mice were treated with neoline by intraperitoneal acute administration, the mechanical threshold was increased in diabetic mice, but not in non-diabetic mice, in a behavioral study. ConclusionThese results suggest that neoline might be a novel active ingredient of GJG and PA that is one of responsible ingredients for ameliorating mechanical hyperalgesia in diabetes via the inhibition of Nav1.7 VGSC current at least.