Objective Lupane-type triterpenoid aglycones from Acanthopanax gracilistylus leaves (AGS) are underexplored compared to roots. This study aimed to establish an efficient isolation method and evaluate their anti-inflammatory potential. Methods Methanol extracts of AGS leaves were separated using high-speed counter-current chromatography (HSCCC) coupled with preparative HPLC. Six compounds were purified and structurally confirmed by NMR spectroscopy. Anti-inflammatory activity was assessed in LPS-stimulated RAW264.7 macrophages via nitric oxide (NO) production, with cytotoxicity measured by MTT assay. Results one lupane-triterpenoid and five Lupane-triterpenoid aglycones were obtained at purities of 94–97%. Cpds 6 and 7 sig-nificantly inhibited NO production by 57–64% at 20 µg/mL without affecting cell viability, whereas Cpds 1 and 2 were inactive, and Cpds 4 and 5 displayed a moderate impact. Additionally, Cpd 4 had moderate cytotoxicity. The integrated HSCCC-prep-HPLC strategy provided high-purity compounds efficiently with minimal solvent use. Conclusion This study presents an effective approach for isolating bioactive lupane-triterpenoid aglycones from AGS leaves. Cpds 6 and 7 demonstrate promising anti-inflammatory activity, supporting further pharmacological exploration.
BACKGROUND:Schizophrenia is a complex neuropsychiatric disorder characterized by impairments in cognition, perception, and social behavior. Current antipsychotic medications primarily target dopaminergic signaling but often exhibit limited efficacy in treating negative and cognitive symptoms. Moreover, long-term antipsychotic therapy is frequently associated with clinically relevant adverse effects, including metabolic syndrome and extrapyramidal symptoms (EPS). Phosphodiesterase 10A (PDE10A) has emerged as a promising non-dopaminergic therapeutic target involved in regulating cyclic nucleotide signaling in the striatum. However, several synthetic PDE10A inhibitors have shown safety and tolerability limitations. This study therefore investigated the antipsychotic-like potential of the ethanol extract of Dracocephalum moldavica (EEDM) and its major flavone glycoside, tilianin, in an MK-801-induced schizophrenia-like mouse model and explored the underlying molecular mechanisms. METHODS:Tilianin content in EEDM was quantified using HPLC, and phytochemical constituents were comprehensively characterized by UHPLC-Q-TOF LC-MS/MS. The inhibitory effect of EEDM and tilianin on PDE10A activity was evaluated using in vitro enzyme assays, supported by molecular docking. Behavioral tests, including the open field test (OFT), acoustic startle response (ASR), novel object recognition, and social interaction test (SIT), were performed in MK-801-induced schizophrenia-like mice. Mechanistic insights were explored through network pharmacology analysis and further validated by analyzing the cAMP/PKA/CREB signaling in the prefrontal cortex using Western blot analysis. RESULTS:HPLC analysis identified tilianin as the major constituent of EEDM, while UHPLC-Q-TOF LC-MS/MS profiling revealed a diverse phytochemical profile comprising multiple flavonoids and phenolic compounds. Molecular docking predicted stable, high-affinity binding of tilianin to the PDE10A catalytic site (docking score: -11.857 kcal/mol), and this prediction was supported by an enzymatic assay showing PDE10A inhibition by both EEDM (IC50 = 346.6 μg/ml) and tilianin (IC50 = 11.25 μg/ml; 25.20 μM). Tilianin ameliorated MK-801-induced hyperlocomotion, rescued prepulse inhibition (PPI) deficits, and reversed impairments in cognitive and social functions. Network pharmacology identified PDE10A, CREB1, ESR1, and MAPK1 as key hubs modulating synaptic plasticity. Furthermore, tilianin restored the disrupted cAMP/PKA/CREB signaling in the prefrontal cortex. CONCLUSION:These findings suggest that tilianin may act as a network-informed modulator associated with PDE10A inhibition and downstream neuroplastic signaling, providing a potential mechanistic basis for addressing the limited efficacy of conventional antipsychotic strategies in schizophrenia.
Ethnopharmacological relevance: The cortex of Eleutherococcus henryi (EH, Araliaceae), also known as "Wu-Jia-Pi", is known for its effects such as dispelling wind and dampness, calming the mind and enhancing intelligence, removing heat and toxin, strengthening muscles and bones, and nourishing the liver and kidneys. Throughout Chinese history and tradition, it has been used for conditions like amnesia, mental fatigue, arthritis, hepatitis, and rheumatism. However, research evaluating its neuroprotective effects and pharmacological properties remains scarce. Aim of the study: The goal is to explore the anti-neuroinflammatory properties of EH in vitro and to discover precisely the bioactive natural products within the medicinal plant that are relevant to its traditional usage. Materials and methods: Utilizing chromatographic techniques, a phytochemical exploration was conducted. The phytochemical structures of the natural products were then elucidated through an analysis involving comprehensive spectra and a comparison with relevant data from published studies. Network pharmacology combined with molecular dynamics simulations (MDs) and docking were applied to forecast potential antineuroinflammatory targets of active compounds. In vitro, the anti-neuroinflammatory efficacy was evaluated via the suppression of inflammatory mediators activated by lipopolysaccharide (LPS) in BV2 microglia. Results: The methanol extract of E.henryi (EHME) restrained the NO release in LPS-activated BV2 microglia, demonstrating anti-neuroinflammatory activity. Subsequently, chemical composition analysis revealed the separation and elucidation of 31 secondary metabolites, comprising 7 new compounds (1-7) and 1 new natural product (8). Based on LPS-induced BV2 cell in vitro activity tests, compounds 4-17, 19, 20, 22, 23, 26, 29 and 31 were found to exhibit potential anti-neuroinflammatory activity, with compound 6 showing the highest efficacy. Furthermore, employing network pharmacology in conjunction with both molecular docking and MDs, potential anti-neuroinflammatory targets of compound 6 were predicted to include TLR4, Src, MAPK, and NF-kappa B. Finally, validation through in vitro experiments confirmed that the anti-neuroinflammatory mechanism of compound 6 is associated with the TLR4/Src/MAPK p38/NF-kappa B p65 signaling pathways. Conclusions: The study affirmed the traditional efficacy of E. henryi and unveiled novel lignans as potent agents against neuroinflammation.
The phytochemical investigation on the rhizomes of Dryopteris crassirhizoma (Dryopteridaceae) resulted in the discovery of one novel compound, drycrassirhizomamide A (1), and one new natural product, drycrassirhizomamide B (2), as well as four known isolates, (S)-(-)-N-benzoylphenylalaninol (3), blumenol A (4), 8-C-glucosylnoreugenin (5), and dryopteroside (6). Their chemical structures were identified by NMR and mass spectroscopy. Compounds 1-2 were determined to be 1,19-diethyl 10-oxo-2,9,11,18-tetraazanonadecanedioate and C,C'-diethyl N,N'-1,6-hexanediylbis[carbamate]. The anti-inflammatory activities of these compounds were evaluated with LPS-stimulated RAW264.7 macrophage and BV2 microglia. The results showed that compounds 1-3 and 6 have inhibitory effects of NO production with IC50 values of 13.41, 30.36, 25.51, and 11.35 μM in LPS-stimulated RAW264.7 cells. Also, compounds 1 and 4-6 have abilities to inhibit NO production with the IC50 values of 40.11, 30.94, 15.76, and 16.79 μM in BV2 cells, which demonstrated that they may possess the potential anti-inflammatory activity.
The plant Dipsacus asperoides C. Y. Cheng et T. M. A., has been traditionally utilized as a medicinal plant in China due to its roots known as “Dipsaci Radix”. It is suggested that Dipsaci Radix exhibits antihyperglycemic, hypolipidemic, and antioxidant properties, along with down-regulating effects on advanced glycation end-products (AGEs) formation. However, there are currently no reliable reports on the effective components derived from Dipsaci Radix for anti-diabetes. In this study, the methanol extract and its corresponding ethyl acetate (EA) fraction of Dipsaci Radix were investigated as potential natural sources of antidiabetic agents and antioxidants by in vivo methods. The existence of phenolic components in extract and fraction enhances their antioxidant and antidiabetic properties. This is evidenced by the fact that all isolated phenolic compounds exhibited such properties, with half of them (Compound 2, 4, 5, 8, 10) displaying multidirectional inhibitory effects. Quality evaluation of these active components using high performance liquid chromatography-ultraviolet (HPLC-UV) technology combined with grey relational analysis provides further information regarding the spectrum-effect relationship between active components and their activities. Among them, the presence of the active ingredient “5-O-caffeoylquinic acid” significantly contributes to the antidiabetic and antioxidant properties of Dipsaci Radix. This holds promising applications in traditional health products and cosmeceuticals.
Eleutherococcus trifoliatus (Araliaceae) is called Baile or Lecai in China. E. trifoliatus is a medicinal and edible plant widely used in folk traditions. As a TCM, the dried herb of this species can remove damp heat and detoxicity, cure rheumatism, remove blood stasis, relieve pain, and alleviate cough and asthma symptoms. Many chemical compounds have been reported including diterpenoids, triterpenoids, phenylpropanoids, flavonoids, lignans, caffeoyl quinic acids, steroids, essential oils, etc., in which flavonoids, saponins, and caffeoyl quinic acids are the most bioactive components. In vitro and in vivo pharmacological experiments demonstrated that E. trifoliatus has anti-inflammatory, hypoglycemic, anticancer, antioxidant, antibacterial, anti-hyperalgesic, anti-fatigue, analgesic, and hemostatic effects. Here we reviewed E. trifoliatus in phytochemistry, analysis methods, and pharmacology.
The plant Dipsacus asperoides C. Y. Cheng et T. M. A., has been traditionally utilized as a medicinal plant in China due to its roots known as “Dipsaci Radix”. It is suggested that Dipsaci Radix exhibits antihyperglycemic, hypolipidemic, and antioxidant properties, along with down-regulating effects on advanced glycation end-products (AGEs) formation. However, there are currently no reliable reports on the effective components derived from Dipsaci Radix for anti-diabetes. In this study, the methanol extract and its corresponding ethyl acetate (EA) fraction of Dipsaci Radix were investigated as potential natural sources of antidiabetic agents and antioxidants by in vivo methods. The existence of phenolic components in extract and fraction enhances their antioxidant and antidiabetic properties. This is evidenced by the fact that all isolated phenolic compounds exhibited such properties, with half of them (Compound 2, 4, 5, 8, 10) displaying multidirectional inhibitory effects. Quality evaluation of these active components using high performance liquid chromatography-ultraviolet (HPLC-UV) technology combined with grey relational analysis provides further information regarding the spectrum-effect relationship between active components and their activities. Among them, the presence of the active ingredient “5-O-caffeoylquinic acid” significantly contributes to the antidiabetic and antioxidant properties of Dipsaci Radix. This holds promising applications in traditional health products and cosmeceuticals.
This study aimed to provide scientific data on the anti-Alzheimer’s disease (AD) effects of phenolic compounds from Drynariae Rhizoma (DR) extract using a multi-component approach. Screening of DR extracts, fractions, and the ten phenolic compounds isolated from DR against the key AD-related enzymes acetylcholinesterase (AChE), butyrylcholinesterase (BChE), β-site amyloid precursor protein cleaving enzyme 1 (BACE1), and monoamine oxidase-B (MAO-B) confirmed their significant inhibitory activities. The DR extract was confirmed to have BACE1-inhibitory activity, and the ethyl acetate and butanol fractions were found to inhibit all AD-related enzymes, including BACE1, AChE, BChE, and MAO-B. Among the isolated phenolic compounds, compounds (2) caffeic acid 4-O-β-D-glucopyranoside, (6) kaempferol 3-O-rhamnoside 7-O-glucoside, (7) kaempferol 3-o-b-d-glucopyranoside-7-o-a-L-arabinofuranoside, (8) neoeriocitrin, (9) naringin, and (10) hesperidin significantly suppressed AD-related enzymes. Notably, compounds 2 and 8 reduced soluble Amyloid Precursor Protein β (sAPPβ) and β-secretase expression by over 45% at a concentration of 1.0 μM. In the thioflavin T assay, compounds 6 and 7 decreased Aβ aggregation by approximately 40% and 80%, respectively, and degraded preformed Aβ aggregates. This study provides robust evidence regarding the potential of DR as a natural therapeutic agent for AD, highlighting specific compounds that may contribute to its efficacy.
基于野外实地考察及文献梳理筛查,首次报道了中国五加科五加属一新记录种:太白大刺五加(Acanthopanax aspertus var.taibeiensis X.Q.Liu,H.Y.Choi,G.H.Lee et C.S.Yook),并提供详细形态特征图.该种形态上与刺五加[Acanthopanax senticosus(Rupr.Maxim.)Harms]和韩国特产植物大虾蛦五加(Acanthopanax aspertus var.koreanus Nakai)近似,但太白大刺五加叶柄末端轮生大刺,茎绿色且茎上无针状下向密生刺,3者容易区分.凭证标本保存于湖南中医药大学标本馆.
The traditional herb Eleutherococcus henryi Oliv. is commonly used to treat inflammatory conditions including rheumatism, arthritis, and hepatitis, as well as mental fatigue and amnesia, according to traditional Chinese medicine (TCM) theory. Savinin is a natural lignan obtained from the roots of E. henryi. The present study was undertaken to determine whether savinin can relieve LPS-induced neuroinflammation and if so, what the mechanism is. Groups of male C57BL/6 mice were administered savinin (5, 10, 20 mg/kg) and DEX (10 mg/kg) by gavage once daily for a continuous 7 days. On the 5th day of continuous pre-administration, LPS (2.5 mg/kg) was injected into the lateral ventricles of the mice for modeling 48 h. We found that treatment with savinin decreased the levels of neuroinflammatory cytokines and histopathological alterations dramatically. Consequently, it improved the LPS-induced neuroinflammatory response in mice. Furthermore, savinin inhibited the up-regulated expression of related proteins in the activated MAPK/NF-κB and NLRP3 inflammasome signaling pathways caused by LPS. Docking studies demonstrated the binding of savinin to three receptors (MAPK, NF-κB and NLRP3) using a well-fitting mode. These findings suggest that savinin may suppress neuroinflammation induced by LPS in vivo via modulating MAPK/NF-κB and NLRP3 signaling pathways.
Antibacterial resistance has become one of the most serious problems threating global health. To overcome this urgent problem, many scientists have paid great attention to developing new antibacterial drugs from natural products. Hence, for exploring new antibacterial drugs from Chinese medicine, a series of experiments were carried out for verifying and elucidating the antibacterial activity and mechanisms of madecassic acid (MA), which is an active triterpenoid compound isolated from the traditional Chinese medicine, Centella asiatica. The antibacterial activity was investigated through measuring the diameter of the inhibition zone, the minimum inhibitory concentration (MIC), the growth curve, and the effect on the bacterial biofilm, respectively. Meanwhile, the antibacterial mechanism was also discussed from the aspects of cell wall integrity variation, cell membrane permeability, and the activities of related enzymes in the respiratory metabolic pathway before and after the intervention by MA. The results showed that MA had an inhibitory effect on eight kinds of pathogenic bacteria, and the MIC values for Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Bacillus megaterium were 31.25, 62.5, 250, 125, 62.5, and 62.5 µg/mL, respectively. For instance, 31.25 µg/mL MA could inhibit the growth of Staphylococcus aureus within 28 h. The antibacterial mechanism experiments confirmed that MA could destroy the integrity of the cell membrane and cell wall of Staphylococcus aureus, causing the leakage of macromolecular substances, inhibiting the synthesis of soluble proteins, reducing the activities of succinate dehydrogenase and malate dehydrogenase, and interacting with DNA, leading to the relaxation and ring opening of supercoiled DNA. Besides, the activities of DNA topoisomerase I and II were both inhibited by MA, which led to the cell growth of Staphylococcus aureus being repressed. This study provides a theoretical basis and reference for the application of MA in the control and inhibition of food-borne Staphylococcus aureus.
五环三萜类化合物是一类重要的天然化合物,广泛存在于水果、蔬菜和药用植物中,种类繁多,且具有丰富的药理活性.研究发现,五环三萜类化合物及其衍生物具有显著的抗菌活性,这为新型广谱抗菌药物的研发提供思路.本文查阅2015年至2021年国内外相关文献,对天然药用植物中具有抗菌活性的五环三萜类物质的研究进展进行综述,以期为五环三萜类抗菌药物的开发和应用提供参考.
阿尔茨海默病(Alzheimer's disease,AD)是一种进行性神经退行性疾病,研究表明神经炎症与AD的发生和发展有着密切的联系.天然来源的活性成分和提取物具有多靶点、多途径、高效低毒、疗效持久等优点,在AD防治方面表现出巨大的潜力.通过对近5年天然产物及提取物在AD防治中的抗炎作用机制包括调控小胶质细胞活化、抑制核因子-κBκB(nuclear factor-κB,NF-κB)通路、抑制丝裂原活化蛋白激酶(mitogen activated protein kinases,MAPK)通路、抑制活性氧通路等进行综述,为天然产物及提取物对AD的临床防治及新药开发提供科学理论参考.
为探究中药白簕(Acanthopanx trifoliatus(L.)Merr.)能否作为高效、低毒的防治阿尔茨海默病的天然药物原料,选用大鼠肾上腺嗜铬细胞瘤株PC12作为神经细胞模型,建立Aβ25-35 诱导的PC12 细胞氧化损伤模型,测定白簕叶总多酚干预24 h后PC12 细胞存活率;通过AAPH诱导的PC12 细胞衰老模型和β-半乳糖苷酶活性染色法评估PC12 细胞衰老情况.结果表明:与仅损伤处理组相比,5~60 mg/L的白簕叶总多酚能够显著提高(p<0.05)经Aβ25-35 诱导的氧化损伤的PC12 细胞的存活率,且能够降低AAPH诱导的细胞衰老模型中的β-半乳糖苷酶活性,表明白簕叶总多酚对PC12 细胞具有显著的保护作用,能有效缓解PC12 细胞氧化损伤与衰老.该研究为寻找有效防治阿尔茨海默病的天然药物的鉴定与筛选提供理论依据.
Ethnopharmacological relevance: Eleutherococcus nodiflorus (Dunn) S.Y.Hu (Araliaceae), also called Eleutherococcus gracilistylus, Acanthopanax gracilistylus, and Xi-zhu-wu-jia (Wujiapi or Nan Wujiapi) in Chinese, is a widely used traditional Chinese herb with the effects of dispelling pathogenic wind and eliminating dampness, nourishing liver and kidney, diuresis and detumescence, promoting blood circulation for removing blood stasis, and strengthening the bones and tendons according to the theory of Traditional Chinese Medicine (TCM). It has been used as medicine for the treatment of paralysis, arthritis, rheumatism, lameness, body asthenia, fatigue, edema, beriberi, and liver diseases. Meanwhile, E. nodiflorus (EN, thereafter) has ginseng-like activities known as "ginseng-like herb".Aims of the review: This review aims to present comprehensive information for the research progress of EN, including taxonomic position, botany, traditional usages, phytochemistry, pharmaceutical analysis, pharma-cology and toxicology. Among them, phytochemical and pharmacological studies are mainly focused.Materials and methods: Relevant literature was acquired from scientific databases including Web of Science, PubMed, Google Scholar, Baidu Scholar, SciFinder and Chinese national knowledge infrastructure (CNKI). Monographs and Chinese pharmacopeia were also utilized as references.Results: In the past decade, a great number of phytochemical and pharmaceutical analyses, as well as pharma-cological studies on EN have been carried out. Several kinds of chemical compositions have been reported, including essential oil, sesquiterpenes, diterpenes, triterpenes, phenylpropanoids, lignans, caffeoyl quinic acids, flavonoids, steroids, fatty acids, ceramides as well as other compounds, among which, diterpenes and triterpenes were considered to be the most active components. The fingerprint chromatography, qualitative and quantitative analysis were used for the methods of quality control of EN. Considerable pharmacological experiments in vitro and in vivo have demonstrated that EN possessed hypoglycemic, anti-inflammatory, anticancer, anti-ageing, anti-fatigue, immunomodulatory, hepatoprotective, antioxidant, anti-AChE, anti-BuChE, anti-hyaluronidase, and antiobesity activities.Conclusions: As an important TCM, a large number of investigations have proved that EN and terpenoids isolated from EN have markedly therapeutic efficacy on diabetes, inflammation, and cancer disorders. These research findings provide modern scientific evidence for the traditional uses of EN. Moreover, more novel and active secondary metabolites from EN, as well as the in vivo and clinical in-depth tests are required in the future.
Introduction: Our study aimed to find out whether the leaves of Acanthopanax gracilistylus with the ethanol extract have the antidiabetic effects in streptozotocin (STZ) induced type 1 diabetic rats. Materials and methods: Type 1 diabetic rats were induced by intraperitoneal STZ injection with 75 mg/kg. The animals were divided randomly with six rats in each group. The study lasted 28 days with daily administration, and at the end of the experiment, the rats were euthanized, the plasma/serum was separated for the biochemical parameters. The pancreatic tissue was used for histopathological and immunohistochemical measurement of NF-kappa B. Results: Treatments of Acanthopanax gracilistylus (100 mg/kg) group led to a significant reduction in diabetic rats in blood glucose was assessed at 2 h by the oral glucose tolerance test (OGTT). The treatment also resulted in insulin level (from 0.33 ng/ml reduced to 0.59 ng/ml), lipid profile (triglyceride lever was reduced from 206.18 to 139.16 mg/dl, and total cholesterol level was reduced from 129.08 to 100.04 mg/dl. By inhibiting NF-kappa B, the release of pro-inflammatory cytokines in diabetic rats induced by STZ was inhibited. In pancreatic tissues, Simultaneous observation of histopathological damage. Conclusion: These findings support the beneficial effect of the leaves of Acanthopanax gracilistylus treatment in diabetic rats, and we attribute it to its anti-diabetic effects.
Acanthopanax trifoliatus (L.) Merr. have been used as folk medicine to treat various diseases traditionally and the young leaves and shoots of A. trifoliatus are popularly consumed as vegetables and herbal tea in southern China. In the study, we firstly tested the cytotoxicity and NO production of 18 fractions that extracted from the leaves, stems and roots of A. trifoliatus to select the bioactive fraction. The increasing evidence suggested that the dichloromethane extract prepared from stems of A. trifoliatus (ATSDC) have anti-inflammatory activity. Therefore, the study followed to investigate the effects of ATSDC on the inflammatory response and the molecular mechanisms underpinning this effect in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. The manuscript showed that ATSDC effectively inhibited NO production in LPS-stimulated cells and significantly reduced the production of pro-inflammatory cytokines IL-6, at a dose of 40 mu g/mL, whereas TNF-alpha production tended to decrease under ATSDC treatment. We also confirmed a dose-dependent and significant inhibition of iNOS and COX-2 protein expression. In conclusion, ATSDC exerted strong inhibitory effect on the expression of iNOS and COX-2 protein in LPS-induced RAW 264.7 macrophages and could be potentially used in treatment of inflammatory-related diseases in the future.
二萜类化合物结构类型众多,广泛地存在于昆虫、植物和微生物中,结构类型的多变性导致其具有丰富的药理活性.目前,由于抗生素的广泛应用,加重了细菌耐药问题,严重影响了抗菌药物的临床疗效.研究发现,二萜类化合物具有显著的抗菌活性,具有抗菌谱广、低毒、作用靶位多、抗菌活性较高等特点,且与抗生素联合使用能增强抗菌效果,其主要抑菌机制通过破坏细胞壁和细胞膜,影响其代谢途径,或与细胞表面的蛋白结合,阻止营养吸收,从而抑制生长导致细菌死亡.本文查阅分析了2016年至2021年文献,对具有抗菌活性的天然二萜类物质的结构类型、抗菌活性及作用机制进行综述,以期为二萜类抗菌药物的进一步研究奠定基础,为解决细菌耐药性问题提供理论依据.
目的:研究糙叶五加不同药用部位的脂溶性化学成分.方法:采用闪式提取法分别提取糙叶五加根皮和茎中的脂溶性成分,采用气相色谱-质谱联用技术结合质谱库检索系统对其脂溶性化学成分进行分离和鉴定,应用色谱峰面积归一化法计算各组分的相对百分含量.结果:从糙叶五加根皮和茎的脂溶性成分中共鉴定出68个化合物,其中根皮和茎中分别鉴定出47和24种脂溶性成分,分别占总峰面积的78.86%和91.87%.结论:闪式提取糙叶五加根皮和茎的脂溶性化学成分种类和含量均存在较大差异,本研究可为糙叶五加的质量评价和进一步的资源开发利用提供实验依据和理论参考.
Obesity and overweight have posed a severe threat to humanity, needing urgent efforts for the development of safe and effective therapeutic interventions. In this research work, we have developed two polyherbal formulations A and B basically consisting of Helianthus tuberosus root powder (also called inulin of synanthrin) along with other herbs for the treatment of obesity. Evaluation of the antioxidant activity of both formulations using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radical scavenging assays showed good antioxidant potentials. Both formulations A and B showed good antiobesity activity on a diet-induced obesity (DIO) model of mice by effectively lowering the body weight of mice compared to the high-fat diet (HFD) control mice, mainly by reducing the food efficiency ratio (FER). Furthermore, both formulations ameliorated lipoprotein misbalances induced by obesity and thus decreased the atherogenic index. Treatment with both formulations significantly decreased the liver and epididymal white adipose tissue (WAT) weight. This was supported by the improvement in steatosis of the liver and reduced hypertrophy in WAT on histological examination. In addition, formulations A and B have been seen as effective in controlling fasting blood glucose levels probably by alleviating HFD-induced insulin resistance. All of these results collectively suggest that formulations A and B serve as potentially safe and effective herbal interventions to control obesity and its comorbidities.