Discovery of Potential Anti-Microbial Molecules and Spectrum Correlation Effect of Ardisia crenata Sims via High-Performance Liquid Chromatography Fingerprints and Molecular Docking.

Ardisia crenata Sims, an important ethnic medicine, is recorded in the Chinese Pharmacopoeia for treating laryngeal diseases and upper respiratory tract infections. This study aimed to evaluate the antimicrobial effect of extracts and potential antimicrobial compounds of A. crenata Sims. It was found that the roots of A. crenata Sims have a potential inhibitory effect on Candida albicans and Aspergillus flavus, with MICs of 1.56 mg/mL and 0.39 mg/mL, and the leaves of A. crenata Sims have a potential inhibitory effect on Pseudomonas aeruginosa and Staphylococcus aureus, with MICs of 3.12 mg/mL and 6.77 mg/mL, respectively. Meanwhile, five compounds including one catechin and four bergenins were obtained from roots. These components were identified on the fingerprint spectrum, representing chromatographic peaks 16, 21, 22, 23, and 25, respectively. Among these, 11-ß-d-glucopyranosyl-bergenin and (-)-gallocatechin showed potential inhibition for Staphylococcus aureus and Pseudomonas aeruginosa with MIC of 0.26 and 0.33 mg/mL, respectively. The roots, stems, and leaves of A. crenata Sims are very similar in chemical composition, with large differences in content. Principal component analysis (PCA) and Hierarchical cluster analysis (HCA) showed that 16 batches of A. crenata Sims could be divided into four main production areas: Guizhou, Jiangsu, Guangxi, and Jiangxi. Furthermore, molecular docking results showed that 11-ß-d-glucopyranosyl-bergenin had a better affinity for Casein lytic proteinase P (ClpP), and (-)-gallocatechin possessed a strong affinity for LasA hydrolysis protease and LasB elastase. These findings suggest catechin and bergenins from A. crenata Sims can be used as antimicrobial activity molecules.

Comparative chloroplast genomes study of five officinal Ardisia Species: Unraveling interspecific diversity and evolutionary insights in Ardisia.

Ardisia S.W. (Primulaceae), naturally distributed in tropical and subtropical regions, has edible and medicinal values and is prevalent in clinical and daily use in China. More genetic information for distinct species delineation is needed to support the development and utilization of the genus Ardisia. We sequenced, annotated, and compared the chloroplast genomes of five Ardisia species: A. brunnescens, A. pusilla, A. squamulosa, A. crenata, and A. brevicaulis in this study. We found a typical quadripartite structure in all five chloroplast genomes, with lengths ranging from 155,045 to 156,943 bp. Except for A. pusilla, which lacked the ycf15 gene, the other four Ardisia species contained 114 unique genes, including 79 protein-coding genes, 30 tRNAs, and four rRNAs. In addition, the rps19 pseudogene gene was present only in A. brunnescens. Five highly variable DNA barcodes were identified for five Ardisia species, including trnT-GGU-psbD, trnT-UGU-trnL-UAA, rps4-trnT-UGU, rpl32-trnL-UAG, and rpoB-trnC-GAA. The RNA editiing sites of protein-coding genes in the five Ardisia plastome were characterized and compared, and 274 (A. crenata)-288 (A. brevicaulis) were found. The results of the phylogenetic analysis were consistent with the morphological classification. Sequence alignment and phylogenetic analysis showed that ycf15 genes were highly divergent in Primulaceae. Reconstructions of ancestral character states indicated that leaf margin morphology is critical for classifying the genus Ardisia, with a rodent-like character being the most primitive. These results provide valuable information on the taxonomy and evolution of Ardisia plants.

Ethnobotanical study of Zhuang medicinal herbs of Ardisia: variety systematization, traditional uses, phytochemistry, pharmacology, clinical application, and toxicity.

OBJECTIVES: This study aimed to systematize the Zhuang medicinal herbs of Ardisia (ZMHA) in China, to clarify the traditional use in Zhuang medicine and the dynamics of international research on phytochemistry, pharmacology, clinical application, and toxicity. KEY FINDINGS: There are 25 species of ZMHA, approximately 938 compounds from the different part, including triterpenoids, phenolics, volatile oils, etc. Pharmacological activity studies have also shown that this genus has anti-tumour, anti-inflammatory, anti-oxidant, anti-bacterial, anti-microbial, etc., and significant effects on respiratory, digestive, urinary, and musculoskeletal system diseases without toxic side effects. SUMMARY: The Ardisia has a medicinal history of nearly a thousand years, mainly for treating diseases of the injuries, musculoskeletal, and symptomatic system in Zhuang medicine. Some plants, such as A. crenata, A. gigantifolia, and A. japonica, are also commonly used in folk Zhuang medicine formulas, to treat musculoskeletal, injury, respiratory, and urinate systems disease. These diseases are related to inflammation. These could provide a new direction for future new drug development research. Therefore, species identification and resource investigation should be strengthened, and conducted in vitro mechanism, in vivo pharmacology, clinical efficacy, and toxicology studies and establish a perfect quality standard system.

Discovery of the Active Compounds of the Ethyl Acetate Extract Site of Ardisia japonica (Thunb.) Blume for the Treatment of Acute Lung Injury.

The objective of this study was to identify and evaluate the pharmacodynamic constituents of Ardisiae Japonicae Herba (AJH) for the treatment of acute lung injury (ALI). To fully analyze the chemical contents of various extraction solvents (petroleum ether site (PE), ethyl acetate site (EA), n-butanol site (NB), and water site (WS)) of AJH, the UPLC-Orbitrap Fusion-MS technique was employed. Subsequently, the anti-inflammatory properties of the four extracted components of AJH were assessed using the lipopolysaccharide (LPS)-induced MH-S cellular inflammation model. The parts that exhibited anti-inflammatory activity were identified. Additionally, a technique was developed to measure the levels of specific chemical constituents in the anti-inflammatory components of AJH. The correlation between the "anti-inflammatory activity" and the constituents was analyzed, enabling the identification of a group of pharmacodynamic components with anti-inflammatory properties. ALI model rats were created using the tracheal drip LPS technique. The pharmacodynamic indices were evaluated for the anti-inflammatory active portions of AJH. The research revealed that the PE, EA, NB, and WS extracts of AJH included 215, 289, 128, and 69 unique chemical components, respectively. Additionally, 528 chemical components were discovered after removing duplicate values from the data. The EA exhibited significant anti-inflammatory activity in the cellular assay. A further analysis was conducted to determine the correlation between anti-inflammatory activity and components. Seventeen components, such as caryophyllene oxide, bergenin, and gallic acid, were identified as potential pharmacodynamic components with anti-inflammatory activity. The pharmacodynamic findings demonstrated that the intermediate and high doses of the EA extract from AJH exhibited a more pronounced effect in enhancing lung function, blood counts, and lung histology in a way that depended on the dosage. To summarize, when considering the findings from the previous study on the chemical properties of AJH, it was determined that the EA contained a group of 13 constituents that primarily contributed to its pharmacodynamic effects against ALI. The constituents include bergenin, quercetin, epigallocatechingallate, and others.

Anti-inflammatory activity of a new lactone isolated from the leaves of Ardisia crenata Sims.

One new lactone (1) named Ardisicreolide C, together with three saponin compounds, Ardisiacrispin B (2), Ardisicrenoside A (3), Ardisiacrispin A (4) were isolated and identified from the leaves of Ardisia crenata Sims. The structures of 1-4 were elucidated by 1D, 2D-NMR and HR-MS spectra and together with the published data. In view of structures with lactone moieties showed good anti-inflammatory activity, the anti-inflammatory effects of Ardisicreolide C on LPS-induced RAW264.7 cells were evaluated by enzyme linked immunosorbent assay (ELISA) method. As a result, Ardisicreolide C could reduce release of nitric oxide (NO), tumour necrosis factor α (TNF-α), interleukin 1ß (IL-1ß), interleukin 4 (IL-4) and interleukin 10 (IL-10) of the cell supernatant to exert anti-inflammatory activity. This indicates that the leaves as non-medicinal parts of Ardisia crenata Sims contain compounds with good anti-inflammatory activity, which provides a new direction for the discovery of anti-inflammatory drugs.

Influence of time-temperature in the antioxidant activity, anthocyanin and polyphenols profile, and color of Ardisia compressa K. extracts, with the addition of sucrose or citric acid.

The objective of this study was to analyze and optimize the influence of heating time and citric acid (CA) or sucrose addition of Ardisia compressa K. extracts on phenolic compounds (TPC), monomeric anthocyanins (MAA), antioxidant activity (TAC), color density (CD), and hue tint (HT), using a full factorial design. Extractions were performed: temperature (25, 50, or 70 °C), time (15, 30, 60, or 90 min), CA (0.0 or 0.02 g), and sucrose (0.0 or 5.0 g). HPLC-DAD-ESI-MS was conducted in extracts without additives and with the addition of CA (0.02 g) or sucrose (5.0 g), at 25, 50, or 70 °C for 15 min. CA-added extracts showed maximum TPC, MAA, TAC (DDPH and ABTS assays), and CD values, with the lowest HT values. Malvidin 3-O-galactoside and myricetin-O-hexoside were the predominant anthocyanin and non-anthocyanin polyphenols. Time, temperature, and solute influenced the optimized extraction of TPC, MAA, anthocyanins, TAC, CD, and HT.

Investigating the Underlying Mechanisms of Ardisia japonica Extract's Anti-Blood-Stasis Effect via Metabolomics and Network Pharmacology.

OBJECTIVE: Our study aims to assess Ardisia japonica (AJ)'s anti-blood-stasis effect and its underlying action mechanisms. METHODS: The primary components of AJ were determined using liquid chromatography-mass spectrometry (LC-MS). The blood stasis model was used to investigate the anti-blood-stasis effect of AJ extract. The underlying mechanisms of AJ against blood stasis were investigated via network pharmacology, molecular docking, and plasma non-targeted metabolomics. RESULTS: In total, 94 compounds were identified from an aqueous extract of AJ, including terpenoids, phenylpropanoids, alkaloids, and fatty acyl compounds. In rats with blood stasis, AJ reduced the area of stasis, decreased the inflammatory reaction in the liver and lungs of rats, lowered the plasma viscosity, increased the index of erythrocyte deformability, and decreased the index of erythrocyte aggregation, suggesting that AJ has an anti-blood-stasis effect. Different metabolites were identified via plasma untargeted metabolomics, and it was found that AJ exerts its anti-blood-stasis effect by reducing inflammatory responses through the cysteine and methionine metabolism, linolenic acid metabolism, and sphingolipid metabolism. For the effect of AJ on blood stasis syndrome, the main active ingredients predicted via network pharmacology include sinensetin, galanin, isorhamnetin, kaempferol, wogonin, quercetin, and bergenin, and their targets were TP53, HSP90AA1, VEGFA, AKT1, EGFR, and PIK3CA that were mainly enriched in the PI3K/AKT and MAPK signaling pathways, which modulate the inflammatory response. Molecular docking was also performed, and the binding energies of these seven compounds to six proteins were less than -5, indicating that the chemical components bind to the target proteins. CONCLUSIONS: This study suggests AJ effectively prevents blood stasis by reducing inflammation.

Biosorption of Pb(II) Using Natural and Treated Ardisia compressa K. Leaves: Simulation Framework Extended through the Application of Artificial Neural Network and Genetic Algorithm.

This study explored the effects of solution pH, biosorbent dose, contact time, and temperature on the Pb(II) biosorption process of natural and chemically treated leaves of A. compressa K. (Raw-AC and AC-OH, respectively). The results show that the surface characteristics of Raw-AC changed following alkali treatment. FT-IR analysis showed the presence of various functional groups on the surface of the biosorbent, which were binding sites for the Pb(II) biosorption. The nonlinear pseudo-second-order kinetic model was found to be the best fitted to the experimental kinetic data. Adsorption equilibrium data at pH = 2-6, biosorbents dose from 5 to 20 mg/L, and temperature from 300.15 to 333.15 K were adjusted to the Langmuir, Freundlich, and Dubinin-Radushkevich (D-R) isotherm models. The results show that the adsorption capacity was enhanced with the increase in the solution pH and diminished with the increase in the temperature and biosorbent dose. It was also found that AC-OH is more effective than Raw-AC in removing Pb(II) from aqueous solutions. This was also confirmed using artificial neural networks and genetic algorithms, where it was demonstrated that the improvement was around 57.7%. The nonlinear Langmuir isotherm model was the best fitted, and the maximum adsorption capacities of Raw-AC and AC-OH were 96 mg/g and 170 mg/g, respectively. The removal efficiency of Pb(II) was maintained approximately after three adsorption and desorption cycles using 0.5 M HCl as an eluent. This research delved into the impact of solution pH, biosorbent characteristics, and operational parameters on Pb(II) biosorption, offering valuable insights for engineering education by illustrating the practical application of fundamental chemical and kinetic principles to enhance the design and optimization of sustainable water treatment systems.

Anti-cancer activity of green synthesized silver nanoparticles using Ardisia gigantifolia leaf extract against gastric cancer cells.

Using extracts from herbs for silver nanoparticle synthesis is attracting attention for its anticancer activity. Ardisia gigantifolia is a herb used in traditional Chinese medicine for treating stomach ailments, and some compounds isolated from this plant exhibit the inhibitory activity against different cancer cells. However, the synthesis of silver nanoparticle using extract of Ardisia gigantiflia leaves and their anti-cancer activity was not reported. In this report, the green synthesized silver nanoparticles using Ardisia gigantiflia extract (Arg-AgNPs) has average diameter of 6 nm with functional groups including O-H, C-H, and CO founded on the surface of these nanoparticles. The viability assays results revealed Arg-AgNPs reduced gastric cancer cell proliferation in a dose-dependent manner, with IC50 values of 1.37 and 0.65 µg/mL for AGS cells and 1.03 and 0.96 µg/mL for MKN45 cells. Arg-AgNPs caused cell cycle arrest at the G0/G1 phase and suppressed cell migration. Additionally, Arg-AgNPs significantly increased the percentage of senescent cells and promoted overproduction of reactive oxygen species (ROS) compared to the control. Thus, this study indicates that Arg-AgNPs can be considered as a promising candidate against human gastric cancer cells.

Terpenoids with Cytotoxic Activity from Roots of Ardisia crispa.

Three new terpenoids, ardisiacrispins G-I (1, 4 and 8), and eight known compounds, cyclamiretin A (2), psychotrianoside G (3), 3-hydroxy-ß-damascone (5), megastigmane (6), corchoionol C (7), zingiberoside B (9), angelicoidenol (10), trans-linalool-3,6-oxide-ß-D-glucopyranoside (11) were isolated from the roots of Ardisia crispa. The chemical structures of all isolated compounds were elucidated by extensive spectroscopic analyses, such as HR-ESI-MS, 1D and 2D NMR spectra. Ardisiacrispin G (1) represents the oleanolic-type scaffold featuring a rare 15,16- epoxy system. All compounds were evaluated for the cytotoxicity against two cancer cell lines (U87 MG and HepG2) in vitro. Compounds 1, 8 and 9 exhibited moderate cytotoxic activity with IC50 values ranging from 7.6±1.1 to 28.8±3.2 µM.

The carbon and nitrogen metabolisms of Ardisia quinquegona were altered in different degrees by canopy and understory nitrogen addition in a subtropical forest.

Although effects of atmospheric nitrogen (N) deposition on forest plants have been widely investigated, N interception and absorption effects by forest canopy should not be neglected. Moreover, how N deposition change the molecular biological process of understory dominant plants, which was easily influenced by canopy interception so as to further change physiological performance, remains poorly understood. To assess the effects of N deposition on forest plants, we investigated the effects of understory (UAN) and canopy N addition (CAN) on the transcriptome and physiological properties of Ardisia quinquegona, a dominant subtropical understory plant species in an evergreen broad-leaved forest in China. We identified a total of 7394 differentially expressed genes (DEGs). Three of these genes were found to be co-upregulated in CAN as compared to control (CK) after 3 and 6 h of N addition treatment, while 133 and 3 genes were respectively found to be co-upregulated and co-downregulated in UAN as compared to CK. In addition, highly expressed genes including GP1 (a gene involved in cell wall biosynthesis) and STP9 (sugar transport protein 9) were detected in CAN, which led to elevated photosynthetic capacity and accumulation of protein and amino acid as well as decrease in glucose, sucrose, and starch contents. On the other hand, genes associated with transport, carbon and N metabolism, redox response, protein phosphorylation, cell integrity, and epigenetic regulation mechanism were affected by UAN, resulting in enhanced photosynthetic capacity and carbohydrates and accumulation of protein and amino acid. In conclusion, our results showed that the CAN compared to UAN treatment had less effects on gene regulation and carbon and N metabolism. Canopy interception of N should be considered through CAN treatment to simulate N deposition in nature.

Anti-colorectal cancer of Ardisia gigantifolia Stapf. and targets prediction via network pharmacology and molecular docking study.

BACKGROUND: Ardisia gigantifolia Stapf. (AGS), a Chinese folk medicine widely grows in the south of China and several studies reported that AGS could inhibit the proliferation of breast cancer, liver cancer, and bladder cancer cell lines. However, little is known about its anti-colorectal cancer (CRC) efficiency. METHODS: In the present study, a combination of MTT assay, network pharmacological analysis, bioinformatics, molecular docking, and molecular dynamics simulation study was used to investigate the active ingredients, and targets of AGS against CRC, as well as the potential mechanism. RESULTS: MTT assay showed that three kinds of fractions from AGS, including the n-butanol extract (NBAGS), ethyl acetate fraction (EAAGS), and petroleum ether fraction (PEAGS) significantly inhibited the proliferation of CRC cells, with the IC50 values of 197.24, 264.85, 15.45 µg/mL on HCT116 cells, and 523.6, 323.59, 150.31 µg/mL on SW620 cells, respectively. Eleven active ingredients, including, 11-O-galloylbergenin, 11-O-protocatechuoylbergenin, 11-O-syringylbergenin, ardisiacrispin B, bergenin, epicatechin-3-gallate, gallic acid, quercetin, stigmasterol, stigmasterol-3-o-ß-D-glucopyranoside were identified. A total of 173 targets related to the bioactive components and 21,572 targets related to CRC were picked out through database searching. Based on the crossover targets of AGS and CRC, a protein-protein interaction network was built up by the String database, from which it was concluded that the core targets would be SRC, MAPK1, ESR1, HSP90AA1, MAPK8. Besides, GO analysis showed that the numbers of biological process, cellular component, and molecular function of AGS against CRC were 1079, 44, and 132, respectively, and KEGG pathway enrichment indicated that 96 signaling pathways in all would probably be involved in AGS against CRC, among which MAPK signaling pathway, lipid, and atherosclerosis, proteoglycans in cancer, prostate cancer, adherens junction would probably be the major pathways. The docking study verified that AGS had multiple ingredients and multiple targets against CRC. Molecular dynamics (MD) simulation analysis showed that the binding would be stable via forming hydrogen bonds. CONCLUSION: Our study showed that AGS had good anti-CRC potency with the characteristics of multi-ingredients, -targets, and -signaling pathways.

Ardisia gigantifolia stapf (Primulaceae): A review of ethnobotany, phytochemistry, pharmacology, clinical application, and toxicity.

ETHNOPHARMACOLOGICAL RELEVANCE: Ardisia gigantifolia Stapf, known as Zou-ma-tai (in Chinese), is a traditional folk medicine, which was commonly used by Dong, Jing, Li, Maonan, Miao, Mulam, Yao, and Zhuang people. The main use of A. gigantifolia is the treatment of rheumatoid arthritis, gouty arthritis, fractures, osteoproliferation, traumatic injuries, gynecological, and neurological diseases. Current studies have shown that the plant has various bioactive components, especially gigantifolinol, which has anti-tumor, anti-inflammatory, anti-tuberculosis, and neuroprotective activities. However, to date, few reviews have been made to summarize A. gigantifolia's related studies. AIMS OF THE REVIEW: This review aimed to summarize the traditional use, phytochemistry, pharmacology, clinical applications, and toxicity of A. gigantifolia, which expect to provide theoretical support for future utilization and highlight the further investigation of this vital plant. MATERIALS AND METHODS: The information related to A. gigantifolia were collated by surveying the traditional medicine books, ethnomedicinal publications, and searching academic resource databases including Web of Science, SciFinder, Springer Link, Pub Med, Science Direct, CNKI, and CQVIP database. RESULTS: A. gigantifolia has been used as a traditional folk medicine for more than 400 years in China. Different parts of the plant, including the aerial part, root, rhizome, and leaf, are mainly used as herbal medicine to treat rheumatoid arthritis, traumatic injuries, gynecological, etc. Currently, 165 compounds have been identified from the plant, including triterpenes, phenolics, coumarins, quinones, volatile oil, and sterols, 137 of which were identified from the rhizome parts. Pharmacological research showed that A. gigantifolia has various bioactivities, such as anti-tumor, anti-inflammatory, anti-oxidant, anti-thrombus, anti-tuberculosis, cough expectorant, and neuroprotective activities. Clinical studies have shown that the plant has no toxic side effects. In vivo administration at the maximum dose was not lethal, indicating the plant's safety. CONCLUSION: To date, most bioactive compounds are identified from the rhizomes of A. gigantifolia, which pharmacological activity and clinical observational studies have validated the plant's traditional use as a treatment for rheumatoid arthritis. It would be helpful to verify the mechanism of some components in vivo, such as gigantifolinol. Moreover, the plant's triterpenoid saponins demonstrated valid anti-tumor effects, especially the AG4 and AG36 compounds, which were shown to have anti-breast cancer effects both in vitro and in vivo. Further research on these components, including molecular mechanisms and in vivo metabolic regulation, needs to be confirmed.

A new oleanane-type triterpene from Ardisia lindleyana D.Dietr and its cytotoxic activity.

A new oleanane-type triterpene, ardisiapunine A (1), together with eight known compounds were isolated from the roots of Ardisia lindleyana D.Dietr. Their chemical structures were determined by means of spectroscopic methods including HR-ESI-MS and (1 D, 2 D) NMR data. The absolute configuration of compound 1 was established by a single-crystal X-ray diffraction experiment. The new compound is an unusual oleanane-type triterpene bearing an acetal and a C-13-C-18 double bond. The cytotoxicity of all isolated compounds were evaluated using four human cancer cell lines, including A549, HepG2, HeLa and U87. The new compound 1 and compound 2 were weakly active but the known compound 6 exhibited a high cytotoxicity compared to cisplatin.

Neuro-emotions based on electroencephalograph response to different color Ardisia mamillata Hance plants in elderly people with and without cognitive impairment.

Background: Given the aging population, the quality of mental health of elderly people deserves special attention. The aims of this study were (1) to assess the difference of neuro-emotion based on EEG from the cognitively impaired elderly (CNE) and the cognitively normal elderly (CIE) participants viewing different color Ardisia mamillata Hance and (2) to determine which color Ardisia mamillata Hance has greater benefits for boosting their neuro-emotions. Methods: The cognitive function of the participants was judged by using the revised Chinese version of the Mini-Mental State Examination (MMSE) scale combined with the daily cognitive performance of the participants, and the participants were divided into the cognitive normal elderly (CNE) and the cognitive impairment elderly (CIE). A total of 10 CNE volunteers and 10 CIE volunteers were recruited as participants for this study. For this study, two varieties of Ardisia mamillata Hance, green tiger tongue (GTT) with green leaves and red tiger tongue (RTT) with reddish brown leaves, were observed as plant materials. In total, six emotional indexes, including stress, engagement, interest, excitement, focus, and relaxation, were then measured by electroencephalography (EEG). Results: RTT had the most positive effect on EEG neuro-emotion in the CNE group, with significant reductions in stress, engagement, and focus in the RTT test, while the combination of GTT+RTT had a positive effect on EEG neuro-emotions in the CIE group, with significant reductions in engagement and focus in the GTT+RTT test. No statistically significant differences were found for the interest, excitement, and relaxation index in the CNE and CIE participants in all tests. Conclusion: Significant reductions were observed in stress, engagement, and focus values of the CIE participants in the RTT test, which indicated that the CNE participants were more relaxed. RTT is a reddish brown and warm color plant, so the CNE individuals should always have the warm color plants indoors or outdoors, which could help boost their neuro-emotions. Significant reductions were observed in engagement and focus values of the CIE participants in the GTT+RTT test, which indicated that the CIE participants were more relaxed. The combination of GTT+RTT test shows the combination cold and warm color plants; therefore, the CIE individuals should always have a combination of cool and warm color plants indoors or outdoors, which could help boost their EEG neuro-emotions.

Two New Phenolic Glycosides with Lactone Structural Units from Leaves of Ardisia crenata Sims with Antibacterial and Anti-Inflammatory Activities.

Two new lactones, named Ardisicreolides A-B (1-2), together with four known flavonoids, Quercetin (3), Myricetrin (4), Quercitrin (5), Tamarixetin 3-O-rhamnoside (6), were isolated from the ethyl acetate portion of 70% ethanol extracts of dried leaves from Ardisia crenata Sims. These compounds were identified from Ardisia crenata Sims for the first time. The structures of 1-6 were elucidated according to 1D and 2D-NMR methods and together with the published literature. All of the isolated compounds were evaluated for in vitro anti-microbial effect against Escherichia coli, Pseudomonas aeuroginosa, Enterococcus faecalis, Proteus vulgaris, Staphylococcus aureus, and Bacillus subtilis. In addition, compounds 1-2 were assessed for anti-inflammatory activity by acting on LPS-induced RAW 264.7 macrophage cells in vitro. The results showed that only compound 2 exhibited moderate antibacterial activity on Bacillus subtilis. Moreover, compounds 1 and 2 were found to significantly inhibit the production of nitric oxide (NO) and reduce the release of tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß), interleukin-4 (IL-4), and interleukin-10 (IL-10) in LPS-induced RAW 264.7 macrophage cells. The present data suggest that lactones from the leaves of A. crenata Sims might be used as a potential source of natural anti-inflammatory agents.

Electroencephalography-Based Neuroemotional Responses in Cognitively Normal and Cognitively Impaired Elderly by Watching the Ardisia mamillata Hance with Fruits and without Fruits.

BACKGROUND: The purpose of this study is to explore the difference between the indexes of neuro-emotion between the cognitively normal elderly (CNE) and cognitively impaired elderly (CIE) while viewing the Ardisia mamillata Hance with red fruit (F) and without red fruit (NF) to determine which kind of the Ardisia mamillata Hance would be more beneficial to the participants' neuro-emotions. METHODS: Nine CNE individuals and nine CIE individuals, ranging in age from 80-90 years old, participated in this study and signed the informed consent form before beginning the experiment. Six mood indicators (engagement, excitement, focus, interest, relaxation, and stress) were measured by an EEG headset during the participants' viewing of the NF, F, and NF + F. RESULTS: For the CNE group, their engagement, excitement, and focus values were the lowest, while their interest value was the highest when they view the NF + F; therefore, we obtain the results that the combination of NF + F was the most beneficial to their EEG emotions. For the CIE group, the combination of NF + F increased their interest score, but decreased their focus score, which indicated that the NF + F was the most beneficial to their neuro-emotions. CONCLUSIONS: This study concluded that the combination of plants with and without fruits was most beneficial to the neural emotions of both groups of elderly people. Especially for the CIE, plants with larger and warmer colors, such as yellow, red, and orange fruits, should be considered for installation indoors or outdoors, as this would be better for their emotional well-being.

Integrated transcriptome and metabolome analyses revealed regulatory mechanisms of flavonoid biosynthesis in Radix Ardisia.

Background: Radix Ardisia (Jab Bik Lik Jib) is a common Miao medicine and is widely distributed in the Guizhou region of southern China. The botanical origin of Radix Ardisia includes the dry root and rhizome of Ardisia Crenata Sims (ACS) or Ardisia Crispa (Thunb.) A.DC. (AC), which are closely related species morphologically. However, the secondary metabolites in their roots are different from one another, especially the flavonoids, and these differences have not been thoroughly explored at the molecular level. This project preliminarily identified regulatory molecular mechanisms in the biosynthetic pathways of the flavonoids between ACS and AC using a multi-omics association analysis. Methods: In this study, we determined the total levels of saponin, flavonoid, and phenolic in Radix Ardisia from different origins. Integrated transcriptome and metabolome analyses were used to identify the differentially expressed genes (DEGs) and differentially expressed metabolites (DEM). We also performed conjoint analyses on DEGs and DEMs to ascertain the degree pathways, and explore the regulation of flavonoid biosynthesis. Results: The total flavonoid and phenolic levels in ACS were significantly higher than in AC (P < 0.05). There were 17,685 DEGs between ACS vs. AC, 8,854 were upregulated and 8,831 were downregulated. Based on this, we continued to study the gene changes in the flavonoid biosynthesis pathway, and 100 DEGs involving flavonoid biosynthesis were differentially expressed in ACS and AC. We validated the accuracy of the RNA-seq data using qRT-PCR. Metabolomic analyses showed that 11 metabolites were involved in flavonoid biosynthesis including: Naringenin, Luteolin, Catechin, and Quercetin. A conjoint analysis of the genome-wide connection network revealed the differences in the types and levels of flavonoid compounds between ACS and AC. The correlation analysis showed that Naringenin, Luteolin, Catechin, and Quercetin were more likely to be key compounds in the flavonoid biosynthesis pathway also including 4CL, AOMT, CHS, CHI, DFR, F3'5'H, FLS, and LAR. Conclusions: This study provides useful information for revealing the regulation of flavonoid biosynthesis and the regulatory relationship between metabolites and genes in the flavonoid biosynthesis pathway in Radix Ardisia from different origins.

The ethnomedicinal and functional uses, phytochemical and pharmacology of compounds from Ardisia species: An updated review.

Medicinal plants are considered to be a critical source of novel compounds and pharmacophores. The genus Ardisia, consisting of approximately 500 species, is the largest genus in the Myrsinaceae family. Ardisia species are widely distributed throughout tropical and subtropical regions of the world and have been used for the treatment of cancer, hypertension, irregular menstruation, gonorrhea, diarrhea and postnatal syndromes, among others. Phytochemical studies of Ardisia species have resulted in the isolation and identification of 111 compounds, including triterpenoid saponins, quinones, phenols, coumarins, cyclic depsipepetide and flavonoids. Crude extracts and isolates from Ardisia have been reported to have in vitro and in vivo efficacies, including but not limited to anticancer, antiinflammatory, antimicrobial, antioxidant, antithrombotic and antidiabetic, antitubercular compounds. This review focuses on the medical and functional uses, phytochemical profile and pharmacological efficacies of Ardisia species over the past 15 years. This review will provide information indicating that Ardisia species represent an invaluable source of potential therapeutic compounds.

Cytotoxic 13,28 Epoxy Bridged Oleanane-Type Triterpenoid Saponins from the Roots of Ardisia crispa.

Ardisiacrispin D-F (1-3), three new 13,28 epoxy bridged oleanane-type triterpenoid saponins, together with four known analogues (4-7) were isolated from the roots of Ardisia crispa. The structures of 1-7 were elucidated based on 1D and 2D-NMR experiments and by comparing their spectroscopic data with values from the published literatures. Ardisiacrispin D-F (1-3) are first examples that the monosaccharide directly linked to aglycone C-3 of triterpenoid saponins in genus Ardisia are non-arabinopyranose. In the present paper, all compounds are evaluated for the cytotoxicity against three cancer cell lines (HeLa, HepG2 and U87 MG) in vitro. The results show that compounds 1, 4 and 6 exhibited significant cytotoxicity against Hela and U87 MG cells with IC50 values in the range of 2.2 ± 0.6 to 9.5 ± 1.8 µM. The present investigation suggests that roots of A. crispa could be a potential source of natural anti-tumor agents and their triterpenoid saponins might be responsible for cytotoxicity.