Fourteen undescribed steroidal saponins from Solanum capsicoides leaves and their neuroprotective effects.

A total of 14 previously undescribed steroidal saponins named capsicsaponins A-N were isolated from the leaves of Solanum capsicoides, encompassing various types, including cholesterol derivatives and pseudospirostanol saponins. The structures of all compounds were determined through comprehensive analysis of spectroscopic data (1D NMR and 2D NMR), along with physicochemical analysis methods (acid hydrolysis, OR, and UV). Moreover, in the H2O2-induced pheochromocytoma cell line model, compounds 1-14 were screened for their neuroprotective effects on cells. The bioassay results demonstrated compounds 8-14 were able to revive cell viability compared to the positive control edaravone. The damage neuroprotection of the most active compound was further explored.

Five new sesquiterpenoids isolated from Dictamnus dasycarpus Turcz.

Five new sesquiterpenoids, dictamtrinorguaianols E and F (1-2), and dictameudesmnosides F, G, and H (3-5), along with seven known sesquiterpenoids (6-12) were isolated from Dictamnus dasycarpus Turcz. The structures of all new compounds were characterized by spectroscopic methods, including UV, IR, HR-ESI-MS, and 1D and 2D NMR. The In-vitro anti-proliferative activities of all the compounds against two human cancer cell lines (SW982 and A549) were evaluated by CCK-8 assay. Compounds 1 and 4 showed medium anti-proliferative activity against SW982 cells, with IC50 values of 3.49 ± 0.10 and 6.42 ± 1.23 µM, respectively. Additionally, compounds 2, 7, and 8 exhibited medium anti-proliferative activity against A549 cells, with IC50 values ranging from 0.80 ± 0.05 to 6.60 ± 0.46 µM.

Euchronin A-F isolated from the Arnebia euchroma (Royle) Johnst. and their anti-proliferative activities in vitro.

Six new naphthoquinones, euchronin A-F (1-6) and nine known naphthoquinones (7-15), were isolated from the roots of Arnebia euchroma (Royle) Johnst. The structures of the new compounds were confirmed by extensive spectroscopic analyses, including UV, IR, HR-ESI-MS, 1D and 2D NMR. In the present study, we estimated the anti-proliferative activities of these compounds with HaCaT cells. The results indicated that compounds 2 and 4 showed strong anti-proliferative activities at 25 µM, with relative viability at 38.83% and 68.44%, respectively.

Cytotoxicity sesquiterpenoids from the leaves of Datura stramonium L.

Four new sesquiterpenoids, dstramonins A-D (1-4), and one new natural product (5), together with three known compounds (6-8), were isolated from the leaves of Datura stramonium L. The structures of new compounds were elucidated by extensive spectroscopic analysis and comparison with the literature. The cytotoxicity of isolates against LN229 cells was assessed and compounds 2-4, and 7 displayed cytotoxic activity with IC50 values ranging from 8.03 to 13.83 µM.

Phenolic components from the fruits of Solanum xanthocarpum with anti-inflammatory activity.

Two new compounds (1 and 2), along with thirty-one known compounds (3-33) were isolated from the fruits of Solanum xanthocarpum. The structure of isolates was elucidated by analysis of spectroscopic data and the physicochemical methods. Meanwhile, the anti-inflammatory activity of isolates was determined using LPS-induced RAW 264.7 cells. The results of anti-inflammatory assays indicated that most isolated compounds (3, 4, 6, 8-14, 17-20, and 30) possessed significant nitric oxide (NO) production inhibition in lipopolysaccharide (LPS)-induced RAW 264.7 cells with IC50 values ranging from 14.33 to 48.55 µM.

Study on the mechanism of Coptis chinensis Franch. And its main active components in treating Alzheimer's disease based on SCFAs using Orbitrap Fusion Lumos Tribrid MS.

ETHNOPHARMACOLOGICAL RELEVANCE: Coptis chinensis Franch. (CCF), as an extensively used traditional Chinese medicine, has therapeutic effects on Alzheimer's disease (AD), but its mechanism of action has not yet been elucidated. AIM OF THE STUDY: This study aims to reveal the mechanism of action of CCF via the gut-brain axis, and provide a new strategy for the clinical treatment of AD. MATERIALS AND METHODS: APPswe/PS1ΔE9 mice were used as AD models, and were given CCF extract by intragastric administration. Barnes maze was used to test the therapeutic effect of CCF on the treatment of AD. To reveal the mechanism of action of CCF in the treatment of AD, Vanquish Flex UHPLC-orbitrap fusion lumos mass was chosen to detect endogenous differential metabolite; MetaboAnalyst 5.0 was applied to derive relevant metabolic pathways; similarly, to explore the effects of CCF on the gut-brain axis, Vanquish Flex UPLC-Orbitrap fusion lumos mass was utilized to detect the changes in the content of SCFAs in AD mice after CCF administration; the prototype components and metabolites in CCF were identified by UPLC/ESI/qTOF-MS, then their effects on Bifidobacterium breve were explored. RESULTS: CCF shortened the latency time of AD mice, improved the target quadrant ratio of AD mice, and made the maze roadmap simpler of AD mice; CCF regulated fifteen potential metabolites of AD mice, interestingly, ILA (indole-3-lactic acid) in SCFAs (short-chain fatty acids) was also included; CCF acted on histidine and phenylalanine metabolic pathways of AD mice; CCF increased the contents of acetic acid and ILA in AD mice; magnoflorine, jatrorrhizine, coptisine, groenlandicine, thalifendine, palmatine, berberine, epiberberine, hydroxylated jatrorrhizine, and 3-methoxydemethyleneberberine in CCF were detected in fecal samples of AD mice; magnoflorine, palmatrubine, 13-methylberberine, berberine, coptisine, and palmatine promoted the growth of Bifidobacterium breve. CONCLUSIONS: we have demonstrated that CCF acts on the gut-brain axis by regulating SCFAs to treat AD.

Phenylpropanoids from Solanum capsicoides and their anti-inflammatory activity.

Two new phenylpropanoids, 4-O-(1''-O-cis-caffeoyl)-ß-glucopyran osyl-1-allyl-3-methoxy-benzene (1), 4'-O-(1''-O-cis-caffeoyl)-ß-glucopyranosyl-hydroxymegastigm-4-en-3-one (2), together with nine known compounds were obtained from the leaves of Solanum capsicoides. Their structures were elucidated based on spectroscopic methods, and comparing spectral data with those in literature. Meanwhile, their anti-inflammatory activities were evaluated on (LPS)-induced RAW 246.7 cells, and 1, 9, and 10 showed better inhibitory effects with IC50 values of 17.19 ± 1.12, 18.15 ± 0.47, and 19.8 ± 0.95 µM, respectively.

Integrated Chinese herbal medicine with Western Medicine versus Western Medicine in the effectiveness of primary hypertension treatment: A systematic review and meta-analysis of randomized controlled trials.

ETHNOPHARMACOLOGICAL RELEVANCE: Integrated Chinese herbal medicine (CHM) and Western Medicine (WM) treatments have been used for primary hypertension (PHTN) patients in China. Currently, there are many randomized control trials (RCTs) published regarding the effect of CHM and WM on PHTN, which indicated that combining Chinese with WM was effective and safe for PHTN when compared with WM alone, but the quality of evidence was insufficient, and there is no clear information and summary are available for these RCTs assessing the effectiveness of CHM with WM versus WM in patients with PHTN. OBJECTIVES: This systematic study and meta-analysis aimed to evaluate the effectiveness and safety of CHM combined with WM in comparison with WM in reducing systolic and diastolic blood pressure for patients with PHTN. METHODS: The information of this study was searched from electronic databases (PubMed, COCHRANE, EMBASE, Ovid, CNKI, VIP, Wanfang, and CBM). The markedly effective and effective terms were according to Guiding Principles for Clinical Research of New Chinese Medicines. Two investigators independently reviewed each trial. The Cochrane risk of bias assessment tool was used for quality assessment, and RevMan 5.4 was used for meta-analysis. RESULTS: In this study, a total of 29 studies that included 2623 patients were recorded. The study results displayed that the clinical effectiveness in the treatment of hypertension patients from the integrated medicines was considerably higher than that with WM alone, clinical effective (RR 1.23, 95% CI [1.17, 1.30], P < 0.00001), and markedly effective (ME) in the patients (RR 1.66, 95% CI [1.52, 1.80], and P < 0.00001). Random effect in SBP (MD 7.91 mmHg,[6.00, 983], P < 0.00001) and DBP (MD 5.46 mmHg, [3.88, 6.43], P < 0.00001), a subgroup analysis was carried out based on the type of intervention, duration of treatment, and CHM formulas that showed significance. Furthermore, no severe side effects were reported, and no patients stopped treatment or withdrawal due to any severe adverse events. CONCLUSION: Compared to WM alone, the therapeutic effectiveness of CHM combined with WM is significantly improved in the treatment of hypertension. Additionally, CHM with WM may safely and efficiently lower systolic blood pressure (SBP) and diastolic blood pressure (DBP) in individuals with PHTN. However, rigorous randomized controlled trials with a large sample, high quality, long duration of treatment, and follow-up are recommended to strengthen this clinical evidence.

New steroids from the pericarps of Datura metel L.

Three new steroids (1-3) and 13 reported analogs (4-16) were extracted from Datura metel L. pericarps. Structure analysis of these extracted compounds was performed by 1 D-NMR and 2 D-NMR spectroscopy, and their spectra were compared with those of similar compounds previously described in the literature. The extracted steroids (1-3) and known compounds (4-16) were evaluated for anti-inflammatory activity against LPS-activated RAW 264.7 cells. Compounds 5, 7, 9, 12 and 15 showed potential anti-inflammatory activity with IC50 less than 35 µM, while compounds 3 and 11 showed weak anti-inflammatory activity with IC50 less than 100 µM.

Two new terpenoids with anti-inflammatory activity from the fruits of Arenga pinnata (Wurmb) Merr.

Two new terpenoids (1 and 2), arenterpenoid D (1) and pinnasesquiterpene A (2), along with 16 phenylpropanoids (3-18) and 8 known terpenoids (19-26) were isolated from 70% EtOH extract of the Arenga pinnata (Wurmb) Merr. fruits. Their structures were elucidated by spectroscopic methods including HR-ESI-MS, 1D, and 2D NMR. The absolute configuration of arenterpenoid D (1) was defined by X-ray crystallographic analysis. Furthermore, we evaluated the anti-inflammatory activity of all compounds, and outcomes showed that 2 and 21 exposed moderate suppressive effects against NO generation in lipopolysaccharide-stimulated RAW 264.7 cells.

Mantuoluosides A-H, new steroids isolated from the leaves of Datura stramonium L.

Eight new steroids, designated mantuoluosides A-H (1-8), were obtained from the enrichment of steroids of the Datura stramonium L. using HPD-BJQH macroporous resin. Their respective structures were elucidated based on spectroscopic methods and comparison data with literature. The anti-inflammatory activities of these compounds were evaluated on (LPS)-induced RAW264.7 cells with inhibition ratio. It was found that most isolates showed potential anti-inflammatory activity with varying degrees of inhibition rate in a concentration-dependent manner at non-cytotoxic concentrations.

Inositol Derivatives with Anti-Inflammatory Activity from Leaves of Solanum capsicoides Allioni

Eight new inositol derivatives, solsurinositols A-H (1-8), were isolated from the 70% EtOH extract of the leaves of Solanum capsicoides Allioni. Careful isolation by silica gel column chromatography followed by preparative high-performance liquid chromatography (HPLC) allowed us to obtain analytically pure compounds 1-8. They shared the same relative stereochemistry on the ring but have different acyl groups attached to various hydroxyl groups. This was the first time that inositol derivatives have been isolated from this plant. The chemical structures of compounds 1-8 were characterized by extensive 1D nuclear magnetic resonance (NMR) and 2D NMR and mass analyses. Meanwhile, the in vitro anti-inflammatory activity of all compounds was determined using lipopolysaccharide (LPS)-induced BV2 microglia, and among the isolates, compounds 5 (IC50 = 11.21 ± 0.14 µM) and 7 (IC50 = 14.5 ± 1.22 µM) were shown to have potential anti-inflammatory activity.

Schisandraceae triterpenoids: A review of phytochemistry, bioactivities and synthesis.

ETHNOPHARMACOLOGICAL RELEVANCE: Plants of the Schisandraceae family have a rich and medicinal history dating back to ancient times. Many of them are used as folk medicine in the treatment of chronic coughs, asthma, nocturnal emission, spontaneous sweating, night sweats, palpitation, insomnia and thirst. AIM OF THE REVIEW: The current review is carried out on triterpenoids from the Schisandraceae family, aiming to comprehensively summarize their phytochemistry, pharmacology and synthesis and provide new insights to the chemical and pharmacological study and rational utilization on medicinal plants of the Schisandarceae family. MATERIALS AND METHODS: The information was searched from the scientific literature published from June 2014 to November 2021 on the online databases (including PubMed, CNKI, Elsevier, SciFinder and Web of Science) and other bibliography (e.g. the Chinese Pharmacopoeia, 2020 edition, Chinese herbal books). The scientific literature related to phytochemistry, pharmacology, biological activites and synthesis of triterpenoids from the Schisandraceae family was gathered. RESULTS: From June 2014 to November 2021, there were approximately 211 novel triterpenoids isolated and identified from 18 species of the Schisandraceae family. These compounds exhibit tremendous diversity in their structures, and some of them possess promising pharmacological activities, including anti-viral, anti-tumor, anti-inflammatory, hepatoprotective, immunosuppressive activities and neuroprotective effects. In the attempt to synthesize active compounds, the total synthesis of 13 schinortriterpenoids belonging to five structural types was successfully completed. CONCLUSIONS: Studies of triterpenoids from the Schisandraceae family are well documented in this review (from June 2014 to November 2021), and it is also well acknowledged that they are valuable resources with medicinal efficacy. However, relevant pharmacological studies are limited to in vitro tests, and data from in vivo studies and toxicology are lacking or unavailable. Fortunately, there is growing interest in the synthesis of active compounds, which should serve as an approach for accessing active compounds to develop in vivo or toxicity studies, with a view of clarifying their in vitro and vivo mechanisms for more effective and safe natural drugs.

Datinolides E-I, five new withanolides with anti-inflammatory activity from the leaves of Datura inoxia Mill.

Five new withanolides, datinolides E-I (1-5), and three known withanolides (6-8) were separated from Datura inoxia Mill. leaves, and datinolide E (1) was the first withanolide with C-27 connected to a nitrogen-containing group. Their structures were clarified by comprehensive spectroscopic analysis and comparison with literature. The anti-inflammatory of isolated compounds against RAW264.7 cells was investigated by the CCK8 assay.

The Polysaccharides from the Aerial Parts of Bupleurum chinense DC Attenuate Epilepsy-Like Behavior through Oxidative Stress Signaling Pathways.

Bupleurum chinense DC. is a traditional Chinese medicine with a long medicinal history and is often used as the main ingredient in prescription drugs for epilepsy. The aerial parts of B. chinense DC. have similar efficacy and composition to B. chinense DC. Therefore, we speculated that the aerial parts of B. chinense DC. could be used in the treatment of epilepsy. Polysaccharides from the aerial parts of B. chinense DC. were selected to explore their therapeutic effects on epilepsy and their potential mechanism of action. The study is aimed at clarifying the antiepileptic effects of the polysaccharides from the aerial parts of B. chinense DC. and their potential underlying mechanisms. The chemical profile of the aerial parts of B. chinense DC. polysaccharides (ABP) was characterized by FT-IR spectrum and HPLC chromatogram. To determine the therapeutic effects of ABPs on epilepsy, we established a kainic acid- (KA-) induced rat model of epilepsy, and through H&E staining, Nissl staining, immunohistochemistry, biochemical analysis, ELISA, and Western blot analysis, we explored the mechanisms underlying the therapeutic effects of ABPs on epilepsy. The monosaccharide content of ABP included galacturonic acid (45.19%), galactose (36.63%), arabinose rhamnose (12.13%), and mannose (6.05%). Moreover, the average molecular weight of ABP was 1.38 × 103 kDa. ABP could improve hippocampal injuries and neuronal function in the KA-induced epilepsy rat model. ABP significantly inhibited oxidative stress in the hippocampus of KA-induced rats. More importantly, ABP could regulate TREM2 activation in the PI3K/Akt/GSK-3ß pathway to inhibit neuronal apoptosis, including increasing the expression of superoxide dismutase and lactate dehydrogenase and decreasing the expression of malondialdehyde. The current study defined the potential role of ABP in inhibiting the development of epilepsy, indicating that ABP could upregulate TREM2 to alleviate neuronal apoptosis, by activating the PI3K/Akt/GSK-3ß pathway and oxidative stress in epilepsy.

The Aerial Parts of Bupleurum Chinense DC. Aromatic Oil Attenuate Kainic Acid-Induced Epilepsy-Like Behavior and Its Potential Mechanisms.

The aerial parts of Bupleurum Chinense DC. aromatic oil (BAO) were a well-known Chinese herbal medicine plant extract used to treat epilepsy. This study aimed to explore the therapeutic effect of BAO on kainic acid- (KA-) induced epileptic rats and the possible mechanism of its antiepileptic effect. The composition and content of BAO were analyzed by GC-MS, and BAO was administered orally to alleviate the epileptic behavior induced by KA brain injection. The behavior of epileptic rats was determined by Racine grading criteria. And hematoxylin-eosin staining (HE), Nissl staining, immunohistochemistry, Elisa, Western blot, and other methods were used to study the antiepileptic mechanism of BAO, and the possible mechanism was verified by the epileptic cell model of hippocampal neurons induced by the low-Mg2+ extracellular fluid. BAO was mainly composed of terpenoids and aliphatic compounds. And BAO could improve KA-induced epilepsy-like behavior, neuroinflammation, and neurotransmitter abnormalities in the hippocampus. Furthermore, BAO could regulate the expression of GABA, NMDAR1, Notch1, and MAP2 to improve the symptoms of epilepsy. These results were also validated at the cellular level. These results indicated that BAO could alleviate the epilepsy-like behavior through the action of the Notch/NMDAR/GABA pathway.

Chemical Constituents of the Roots of Schisandra chinensis.

One new phenylpropanoid schineolignin D (1), one new sesquiterpene (-)-(7S,10S)-3,11,12,13-tetrahydroxycalamenene (2), one new quinic acid 4-(E)-O-coumaroylquinic acid ethyl ester (3), and seven known compounds 4-10 were separated from the roots of Schisandra chinensis. The chemical structures of all compounds were characterized by NMR spectroscopic experiments. All compounds were assessed for their neuroprotective effects on PC12 cell lines induced by H2 O2 . Compounds 1, 3-4, and 7 showed statistically significant neuroprotective activities with the negative control group at 12.5 µM.

Bioactive lipids from the fruits of Solanum xanthocarpum and their anti-inflammatory activities.

Bioactive lipids widely found in daily consumed plants and animals are essential or beneficial to health and some of them are important physiological regulators in the human body. In our current investigation, 18 bioactive lipids (1-18), including 8 sphingolipids (1-8), 7 oxylipins (9-15), 3 phenolic lipids (16-18) were isolated from the fruits of Solanum xanthocarpum. And compounds 1, 9, 15, 16, and 18 were new lipids. In this study, homologues (4-8, 16, and 17) and configuration isomers (2 and 3) of bioactive lipids were separated, and NMR combined with MS/MS2 was an effective method to identify these compounds. These findings provided the reference for the separation and structural identification of bioactive lipids. The anti-inflammatory activities of all isolated lipids were evaluated by their inhibition of the NO release of LPS-induced RAW 264.7 cells. Aglycone components of sphingolipids, oxylipids with free carboxylic acid groups, phenylpropionic acid-fatty acid glyceride polymer exhibited significant anti-inflammatory activities. Further analysis by molecular docking revealed the interactions of bioactive compounds with the iNOS protein.

Four new secoiridoids from the stem barks of Syringa reticulata (Bl.) Hara.

Four new secoiridoids, syrretoside A (1), syrretoside B (2), 5ß, 8ß-syrretaglucone C(3), 5ß, 8α-syrretaglucone C (4), together with eight known secoiridoids (5-12), were isolated from the stem barks of Syringa reticulata (Bl.) Hara. The structures of isolated compounds were established based on the physical and chemical means, NMR spectroscopy, high-resolution mass spectrometry (HR-ESI-MS), and circular dichroism spectrum (CD), as well as in comparison with the literature. The cytotoxicity of isolated compounds was investigated using CCK8 assay, which showed that these compounds had different degrees of inhibitory effect on two human tumor (MGC803, LN229) cell lines.