Aerial Parts Research Articles

Phytochemicals, UPLC-QTOF-MS/MS analysis, potential acaricidal activity and molecular modeling of Datura metel grown in North-Eastern India

The present investigation emphasized exploitation of Datura metel L. for potential acaricidal activity. Extraction method suggested higher extraction efficiency with the use of 50 % methanol over aqueous medium. UPLC-QTOF-ESI-MS analysis of the extracts resulted tentative identification of eighteen tropane alkaloids such as tigloidin, hyoscyamine N-oxide, scopolamine N-oxide, hyocyamine, hydroxyapoatropine, tropinone, scopine, hyoscine, atropine, valtropine, ditigloyloxytropane, ditigloyloxytropanol, apohyoscine, tigloyloxytropane, norhyoscine, meteloidine, cuscohygrine and tropine in the aerial parts (EAP) and roots (ER). Further, nine phenolic acids such as gallic, protocatechuic, chlorogenic, vanillic, p-coumaric, ferulic, quinic, syringic, and sinapic acids along with fourteen flavonoids such as luteolin-7-glucoside, catechin-3-O-rhamnoside, kempferol-3,7-O-diglucoside, naringenin-6-β-D-glucopyranoside, quercetin 3-O-glucosyl-xyloside, apigenin-7-O-glucoside, flavonol-3-glucoside, luteolin, epicatechin, chrysoeriol, diadzein, genistein, hesperidin and hydroxycoumarin were also identified. Highest acaricidal activity was observed for ER showing LC50 and LC90 of 112.5 and 317.3 μg/mL after 48 h of exposure, respectively. Molecular modeling analysis revealed favourable interaction of tigloidine with UDP transferase of T. urticae through attractive charge, pi-alkyl, alkyl and conventional H bonds. Though, ER was found to be phytotoxic with the highest root growth inhibition in terms of IC50 value of 131.2 and 184.9 μg/mL against Chenopodium album and Triticum aestivum, respectively. Being eco-benign natural products, Datura phytochemicals can serve as potential bio-acaricide, thereby, a smart delivery system could be developed comprising synergistic concoction of the alkaloid rich phytochemical fractions for efficient management of the notorious acarids.

ITRAQ-based proteomic analysis reveals the effect of ribosomal proteins on essential-oil accumulation in Houttuynia cordata Thunb.

Houttuynia cordata Thunb., also known as Yuxingcao in Chinese, occupies a pivotal role in Asian traditional medicine and cuisine. The aerial parts and underground stems of H. cordata exhibit remarkable chemical diversity, particularly in essential oil. Nevertheless, the mechanisms regulating essential oil biosynthesis in H. cordata remain unclear. In this study, we present a quantitative overview of the proteomes across four tissues (flower, stem, leaf, and underground stem) of H. cordata, achieved through the application of the isobaric tag for relative and absolute quantitation (iTRAQ). Our research findings indicate that certain crucial ribosomal proteins and their interactions may significantly impact the production of essential oils in H. cordata. These results offer novel insights into the roles of ribosomal proteins and their associations in essential oil biosynthesis across various organisms of H. cordata.

Ascorbic Acid Improves Tomato Salt Tolerance by Regulating Ion Homeostasis and Proline Synthesis.

In this study, processing tomato (Solanum lycopersicum L.) 'Ligeer 87-5' was hydroponically cultivated under 100 mM NaCl to simulate salt stress. To investigate the impacts on ion homeostasis, osmotic regulation, and redox status in tomato seedlings, different endogenous levels of ascorbic acid (AsA) were established through the foliar application of 0.5 mM AsA (NA treatment), 0.25 mM lycorine (LYC, an inhibitor of AsA synthesis; NL treatment), and a combination of LYC and AsA (NLA treatment). The results demonstrated that exogenous AsA significantly increased the activities and gene expressions of key enzymes (L-galactono-1,4-lactone dehydrogenase (GalLDH) and L-galactose dehydrogenase (GalDH)) involved in AsA synthesis in tomato seedling leaves under NaCl stress and NL treatment, thereby increasing cellular AsA content to maintain its redox status in a reduced state. Additionally, exogenous AsA regulated multiple ion transporters via the SOS pathway and increased the selective absorption of K+, Ca2+, and Mg2+ in the aerial parts, reconstructing ion homeostasis in cells, thereby alleviating ion imbalance caused by salt stress. Exogenous AsA also increased proline dehydrogenase (ProDH) activity and gene expression, while inhibiting the activity and transcription levels of Δ1-pyrroline-5-carboxylate synthetase (P5CS) and ornithine-δ-aminotransferase (OAT), thereby reducing excessive proline content in the leaves and alleviating osmotic stress. LYC exacerbated ion imbalance and osmotic stress caused by salt stress, which could be significantly reversed by AsA application. Therefore, exogenous AsA application increased endogenous AsA levels, reestablished ion homeostasis, maintained osmotic balance, effectively alleviated the inhibitory effect of salt stress on tomato seedling growth, and enhanced their salt tolerance.

Fusarioid keratitis and other superficial infections: A 10-years prospective study from Northeastern Brazil.

Fusarium and allied genera (fusarioid) species are common colonizers of roots and aerial plant parts, or act as phytopathogens in forestry and horticultural or grain crops. However, they can also cause a wide range of infections in humans, including onychomycosis, cutaneous and invasive infections. Fusarioid keratitis is characterized by an infection of the cornea with a suppurative and ulcerative appearance, which may cause damage to vision and permanent blindness. The aim of the present study was to investigate the prevalence of fusarioid species, biofilm formation and antifungal susceptibility profiling of clinical isolates recovered from patients with keratitis and dermatomycoses. The study was performed between March, 2012-December, 2022. Demographic, clinical and epidemiological data of patients were also collected. In the present study, most of the patients with keratitis were male (74%), had a median age of 42 years old, worked with plant material or debris and 26% of them reported eye trauma. Regarding dermatomycosis, most of patients were female and exhibited toenail lesions. Forty-seven isolates belonged to the genus Neocosmospora (78.33%), nine to the Fusarium fujikuroi (15%) and four to the Fusarium oxysporum (6.66%) species complexes. Several strains were moderate biofilm producers, specifically among Fusarium annulatum. Most strains showed increased MICs to amphotericin B and ketoconazole and low MICs to itraconazole. MICs ranged from 0.25 to 16 μg/mL for amphotericin B, 0.0625 to >16 μg/mL for ketoconazole and 0.125 to 8 for itraconazole. It is possible to conclude that fusarioid keratitis in Northeastern Brazil is an important and neglected disease, given the high number of cases, increased need for keratoplasty and poor outcome of the disease.

Evaluation of Eruca Sativa and Capsicum annuum alcoholic extracts as pesticide against aphid and whitefly pests

The aphid (Aphidoidea family) and the whitefly (Aleyrodidae family) are closely related, quickly breeding insects that, when infected, render plants susceptible to diseases since they suck the juices of these plants. They damage the aerial parts of plants and even their roots. Their control is of high concern to limit the damage and minimize the loss of the crops with the use of the safest pesticides. The present study was conducted to assess the perished effect of the Eruca sativa (local name: arugula) leaves and the Capsicum annuum (local name: hot pepper) fruits on aphids and on the eggs and nymphs of whitefly by spraying their alcoholic extracts on tested species. Three pesticide concentrations (0.5, 1 and 1.5%) of either extract were prepared and tested. Adhesives, propellants and other materials were added to the extracts to enhance their effectiveness. The results indicated that the pesticide prepared from these extracts has a concentration- and time-dependent impact on the growth of all tested species; the highest mortality rate was achieved at 1.5% concentrations. The time required for that highest effect was 72 hours for Eruca sativa leaf extract on aphids (100%); and on the eggs (89%) and nymphs (94.1%) of whiteflies. Meanwhile, the highest mortality rates achieved by 1.5% Capsicum annuum fruit extract were after 48 hours on aphids (100%), on the nymphs of whiteflies (100%), and 72 hours on whitefly eggs (96.4%). These effects may be related to the presence of many bioactive substances that were detected in the extracts of these two plants, including tannins, glycosides, phenols, resins, flavonoids, saponins, alkaloids, coumarin, steroids and terpenes.

Examining the Bioactive Elements of Urtica urens Hydroalcoholic Extract and Its Possible Antidepressant Effects in Mice

The majority of antidepressant medications reduce depression symptoms, but they also have a number of undesirable side effects. The hunt is on for medications that are both more effective and well-tolerated. In light of this, the current investigation set out to assess the hydroalcoholic extract of Urtica Urens L.'s aerial parts' (HAUU) antidepressant potential in mice. The Tail Suspension Test (TST) and the Forced Swimming Test (FST) on mice were used to assess it. For 14 days, the HAUU (250 and 500 mg/kg, po) was given orally to distinct groups of 20–25-weight Swiss albino mice in order to conduct TST and FST testing. The presence of alkaloids, glycosides, phenols, flavonoids, and tannins was discovered through phytochemical examination. The HAUU demonstrated a dose-dependent decrease in the amount of time that mice were immobile. Mice's immobility duration was considerably shortened in both the FST and TST when 500 mg/kg of HAUU was administered. The extract's effectiveness was discovered to be on par with fluoxetine (20 mg mg/kg, po). It was discovered that when given orally at a dose of 2000 mg/kg, it was toxicologically safe and did not cause any mouse deaths. The results of the current investigation indicate that the HAUU is toxicologically safe and has strong antidepressant activity, as demonstrated by the TST and FST tests. Keywords: Urtica Urens L, Depression, Tail suspension test, Forced swimming test, Fluoxetine

The chemical composition of the essential oil of Calendula suffruticosa subsp. fulgida (Raf.) Guadagno aerial parts growing wild in Sicily (Italy)

Calendula L. is a relatively small genus belonging to the Asteraceae family, distributed in Europe to Western Himalaya, Macaronesia, Mediterranean to Sahara and Arabian Peninsula. Some of its species are largely utilised in the ethnopharmacology of several countries and several documented biological properties have been determined. In the present study, the essential oil composition of Calendula suffruticosa subsp. fulgida (Raf.) Guadagno, collected in Sicily, a plant never previously investigated, has been carried out. The oil was shown to be quite rich in sesquiterpene hydrocarbons (44.5%) with δ-cadinene (15.9%) and viridiflorene (6.3%) as main metabolites. Also, monoterpene hydrocarbons (39.3%) were present in good amount being α-thujene (10.0%) and sabinene (6.9%) the principal metabolites of the class. The comparison with all the essential oils from Calendula taxa studied so far has been carried out.

Nematicidal and insecticidal activity of essential oils from Artemisia scoparia and Centratherum punctatum and their mixtures

The present study involves the phytochemical analysis and assessing potential synergies among essential oils (EOs) against pests. The EOs were obtained by hydrodistillation from the aerial part (ASAO) and the root part (ASRO) of Artimisia scoparia, and from the aerial part of Centratherum punctatum (CPAO). The EOs yield ranged from 0.5 to 0.1% (v/w). The GC-MS analysis revealed the presence of 35, 43, and 49 compounds, constituting 99.2%, 98.34%, and 99.93% in ASAO, ASRO, and CPAO, respectively. Capillene was identified as the dominant compound both in ASAO and ASRO, but in variable amounts. Caryophyllene oxide (36.4%) was identified as the major component of CPAO. Pure EOs were blended in binary and ternary mixtures at ratios to analyze their synergistic effect against pests. The nematicidal activity (percent mortality and egg hatchability against Meloidogyne incognita at different concentrations was evaluated and the ternary mixture (ASAO + ASRO + CPAO) was found to be most effective at 1 μL/mL with 55.67 ± 1.41% larval immobility at 96 h of exposure. The antifeedant activity of pure and blended EOs was examined against Spodoptera litura using the leaf-dip method. Individually ASAO was most effective with 66.91% feeding inhibition, however the ternary combination showed 58.03% feeding inhibition. Moreover, molecular docking of selected volatiles (≥4% area) from the tested samples was carried out to analyze the interactions with target protein; acetylcholinesterase (AChE) and glutathione S-transferases (GST-1) and the ligands interacted favourably with the target proteins. The blending of EOs resulted in synergistic effects, enhancing their efficacy. Data acquired highlighted that A. scoparia and C. punctatum essential oils could be natural alternatives for nematode control and pest control in agriculture.

Phytochemical Investigation of Polyphenols from the Aerial Parts of Tanacetum balsamita Used in Transylvanian Ethnobotany and Parallel Artificial Membrane Permeability Assay.

In this study, based on ethnobotanical data recorded in Transylvania, the polyphenolic compounds and the permeability of the aerial part's extract of Tanacetum balsamita were investigated. Ultrahigh-performance liquid chromatography-tandem mass spectrometry was applied for the analysis of the extracts. Parallel artificial membrane permeability assay (PAMPA) for the gastrointestinal tract and the blood-brain barrier was conducted. In the ethanolic and aqueous extracts of the species traditionally used for wound, furuncle, and liver disorders, 92 polyphenols were characterized (e.g., flavonoid, hydroxycinnamic acid, catechin, dihydroxybenzoyl, lignan derivatives, and a monoterpene) including 54 compounds identified for the first time in the plant. In the PAMPA tests, eight components were shown to be capable of passive diffusion across the studied membranes. These include apigenin and seven methoxylated flavonoid derivatives. Based on these results, methoxylated flavonoids might promote the pharmacological potential of T. balsamita to be applied in the enhancement of novel remedies.

Time domain modeling of lightning transients in grounding systems considering frequency dependence and soil ionization

This paper presents a new model for analyzing transient grounding system behavior during a direct lightning strike. The modeling that we propose allows us to consider a simple grounding conductor buried horizontally or vertically, a grounding grid, wind turbine grounding system and grounding circuits for wind farms while including the aerial parts (towers and blades). This modeling is developed directly in the time domain taking into account the frequency dependence of the impedance and admittance of the wired conductors and of the electrical parameters of the soil (ρ, ε) and also considering the ionization of the soil. This formalism is based on transmission line equations, rational approximation by vector fitting and the Finite Difference Time Domain numerical method. The proposed formalism is verified considering both simulations and experimental results from available published researches. The Ground Potential Rise GPR in the grounding circuits of wind farms are discussed during the first stroke and also during the subsequent stroke whose frequency range generates more propagation of electrical waves along conductors. This formalism makes it possible to contribute to all knowledge/research of grounding systems.

Ecotoxicity of Cadmium along the Soil-Cotton Plant-Cotton Bollworm System: Biotransfer, Trophic Accumulation, Plant Growth, Induction of Insect Detoxification Enzymes, and Immunocompetence.

Cadmium (Cd) is a hazardous element that may jeopardize environmental safety and human health through biotransfer and trophic accumulation. Here, we tested Cd toxicity on cotton plants, cotton bollworms, and their responses. Results demonstrated that Cd accumulated in plant roots, aerial parts, insect larvae, pupae, and frass in a dose-dependent pattern. The ∼9.35 mg kg-1 of Cd in plant aerial parts, ∼3.68 in larvae, ∼6.43 in pupae, and high transfer coefficient (∼5.59) indicate significant mobility. The ∼19.61 mg kg-1 of Cd in larvae frass suggests an effective detoxification strategy, while BAFcotton (∼1.14) and BAFworm (∼0.54) indicated low bioaccumulation. Cadmium exposure resulted in compromised plant growth and yield as well as alterations in photosynthetic pigment contents, antioxidant enzyme activities, and certain life history traits of cotton bollworms. Furthermore, carboxylesterase activity and encapsulation rates of insect larvae decreased with increasing Cd concentrations, whereas acetylcholinesterase, phenol oxidase, glutathione S-transferase, and multifunctional oxidase exhibited hormesis responses.

Biocontrol potential of epiphytic bacteria against Xanthomonas citri pathotypes A and A*

BackgroundCitrus canker caused by the bacterium Xanthomonas citri (Hasse 1915) is known as a dangerous disease that has serious economic impacts on citrus production in many tropical and subtropical countries. In Iran, Citrus canker disease has caused significant damage to various citrus fruits, particularly limes. Nowadays, employing antagonistic bacteria as an effective and environmentally friendly method for plant disease management has gained special importance.ResultsCitrus leaf samples were collected from different regions of Iran, and after isolating epiphytic bacteria, ex planta and in planta investigations concerning antagonistic activities of the isolates against Xanthomonas citri pathotypes A and A* were performed. A total of 94 epiphytic bacterial isolates were isolated from citrus aerial parts. Based on biochemical, physiological, morphological, and genotypic tests, it was determined that these bacteria belong to the Bacillus and Staphylococcus genera. The highest inhibition activity against the pathogenic bacterium was related to isolates D4 and D5. Using the molecular method and the resulting dendrogram, it was found that these isolates were most similar to Bacillus amyloliquefaciens. The present findings demonstrated that pathogenicity test on key lime leaves infected with X. citri pathotypes A and A*, along with the application of the biocontrol strain B. amyloliquefaciens, resulted in a significant reduction in the number of canker lesions.ConclusionThe results strongly suggested that the identified antagonistic bacterial isolates hold promising potential as biocontrol agents for managing citrus bacterial canker disease.

Immunosuppressive leucosesterterpane and penta-nor-leucosesterterpane sesterterpenoids from Leucosceptrum canum

Five undescribed leucosesterterpane sesterterpenoids, leucosceptrines A−E, two undescribed penta-nor-leucosesterterpane (C20) sesterterpenoids, nor-leucosceptrines A and B, and three known analogues, were obtained from the aerial parts of Leucosceptrum canum of Chinese origin. Leucosceptrines A−C are the first examples of leucosesterterpane-type sesterterpenoids with unclosed dihydropyran rings and reverse configurations at chiral centers C-4 and/or C-12. Nor-leucosceptrines A and B possesses an unusual penta-nor-leucosesterterpane skeleton. Their structures were unambiguously elucidated through comprehensive spectroscopic analyses and single-crystal X-ray diffraction. A plausible biogenetic pathway for these sesterterpenoids was proposed. The immunosuppressive effects of these isolates on the secretion of the cytokine IFN-γ by T cells stimulated with anti-CD3/CD28 monoclonal antibodies were observed with different potencies.

Isolation of two new cucurbitane-type triterpenoids from Kedrostis gijef

Two new cucurbitane-type triterpenoids (2,3), together with two known compounds (1,4), were isolated from the aerial parts of Kedrostis gijef. The structure of all compounds was elucidated based on NMR, HRESIMS analyses, and by comparison with the literature. Additionally, the cytotoxic activity against HeLa, Caco-2, and SH-SY5Y cell lines was determined using MTT colorimetric assay.

Diterpenoids from the Aerial Parts of Isodon serra with Selective Cytotoxic Activity.

Four new diterpenoids, isodosins A-D (1-4), together with nine known compounds (5-13) were isolated and identified from the aerial parts of Isodon serra (Maxim.) Hara. The structures of the new diterpenoids were elucidated based on the analysis of HR-ESI-MS data, 1D/2D-NMR-spectroscopic data, and electronic circular dichroism (ECD) calculations. Cytotoxicities of compounds 2, 3, 5, 6, and 9 against the HepG2 and H1975 cell lines were evaluated with the MTT assay. As a result, compounds 2, 3, and 6 revealed higher levels of cytotoxicity against HepG2 cells than against H1975 cells. Moreover, compund 6 demonstrated the most efficacy in inhibiting the proliferation of HepG2 cells, with an IC50 value of 41.13 ± 3.49 μM. This effect was achieved by inducing apoptosis in a dose-dependent manner. Furthermore, the relationships between the structures and activities of these compounds are briefly discussed.

Four new sesquiterpenoids from the aerial parts of Pogostemon cablin (Blanco.) Benth. and their hypoglycemic activity

Four previously undescribed sesquiterpenoids (1–4), including two natural guaiane-type sesquiterpenoids (1–2), a rearranged guaiane-type sesquiterpenoid (3), and a norsesquiterpenoid (4), were isolated from the ethanol extract of the aerial parts of Pogostemon cablin (Blanco.) Benth. Their chemical structures were determined based on extensive spectroscopic data analysis, including UV, IR, NMR, HRESIMS, and CD spectroscopy. Compound 1 exhibited a good hypoglycemic activity with glucose uptake of 124.3% and 131.2% in myotubes, respectively, at the concentrations of 20 and 40 μM and showed no cytotoxicity. These findings provide a material basis for further research on P. cablin.

Influence of extraction solvents on the chemical constituents and biological activities of Astragalus aduncusfrom Turkey flora: In vitro and in silico insights.

The n-hexane, ethyl acetate, ethanol, ethanol/water (70% ethanol), and water extracts of Astragalus aduncus aerial parts were investigated for their antioxidant potential, enzyme inhibition activity (anti-acetylcholinesterase [AChE], anti-butyrylcholinesterase [BChE],antityrosinase, antiamylase, and antiglucosidase) and antiproliferative effect (against colon adenocarcinoma cell line[HT-29], gastric cancer cell line[HGC-27], prostate carcinoma cell line[DU-145], breast adenocarcinoma cell line[MDA-MB-231],and cervix adenocarcinoma cell line [HeLa]). In addition, the phytochemical profile of the extracts was evaluated using validated spectrophotometric and high-pressure liquid chromatography-electrospray ionization/tandem mass spectroscopymethods. Generally, the 70% ethanol extract demonstrated the strongest antioxidant properties, and it was the richest source of total phenolic constituents. Our findings indicated that the ethyl acetate extract was the most potent BChE inhibitor (11.44 mg galantamine equivalents [GALAE]/g) followed by the ethanol extract (8.51 mg GALAE/g), while the ethanol extract was the most promising AChE inhibitor (3.42 mg GALAE/g) followed by the ethanol/water extract (3.17 mg GALAE/g).Excellent tyrosinase inhibitory activity (66.25 mg kojic acid equivalent/g) was observed in ethanol/water extracts of the aerial part of A. aduncus. Тhese results showed that the most cytotoxic effects were exhibited by the ethyl acetate extract against HGC-27 cells (IC50: 36.76 µg/mL), the ethanol extract against HT-29 cells (IC50: 30.79 µg/mL), and the water extract against DU-145 cells (IC50: 37.01 µg/mL). A strong correlation was observed between the highest total flavonoid content and the highest content of individual compounds in the ethanol extract, including rutin, hyperoside, isoquercitrin, delphinidin-3,5-diglucoside (delphinidin-3,5-O-diglucoside), and kaempferol-3-glucoside (kaempferol-3-O-glucoside). In the present study, the A. aduncus plant was considered a new source of antioxidants, enzyme inhibitors, and anticancer agents and could be used as a future health-benefit natural product.

Application of INAA technique for analysis of essential and toxic elements in two Algerian plants Cynodon dactylon L. and Phragmites australis

Abstract This study represents the investigation of major and trace elements in two indigenous plants, Cynodon dactylon (L.) and Phragmites australis, grown in the Ghardaia region of Southern Algeria. Using Instrumental Neutron Activation Analysis (INAA) technique, the research aimed to ascertain the content of essential and toxic elements in the aerial parts of these plants. Twenty eight elements as (Ag, As, Ba, Br, Ca, Ce, Co, Cr, Cs, Eu, Fe, Hf, Hg, K, La, Lu, Na, Nd, Rb, Sb, Sc, Se, Sm, Sr, Tb, Th, Yb and Zn) were analysis with INAA method. Given the scarcity of data regarding essential and toxic chemical elements in food within Algeria, the study focused on evaluating the content of these elements in two plant species commonly utilized by Bedouins in traditional medicine and as fodder, as well as by professionals for decontamination and water purification purposes. The concentrations of mineral elements observed in these plants were found to be in proximity to the minimum levels recommended by the Food and Agriculture Organization (FAO). The data obtained from this investigation are deemed applicable for Algerian food purposes, offering valuable insights into the elemental composition of these plants and their potential roles in traditional and practical applications.

Abietane Diterpenes from Medusantha martiusii and Their Anti-Neuroinflammatory Activity.

Seven new abietane diterpenoids, comprising medusanthol A-G (1-3, 5, 7-9) and two previously identified analogs (4 and 6), were isolated from the hexane extract of the aerial parts of Medusantha martiusii. The structures of the compounds were elucidated by HRESIMS, 1D/2D NMR spectroscopic data, IR spectroscopy, NMR calculations with DP4+ probability analysis, and ECD calculations. The anti-neuroinflammatory potential of compounds 1-7 was evaluated by determining their ability to inhibit the production of nitric oxide (NO) and the proinflammatory cytokine TNF-α in BV2 microglia stimulated with LPS and IFN-γ. Compounds 1-4 and 7 exhibited decreased NO levels at a concentration of 12.5 µM. Compound 1 demonstrated strong activity with an IC50 of 3.12 µM, and compound 2 had an IC50 of 15.53 µM; both compounds effectively reduced NO levels compared to the positive control quercetin (IC50 11.8 µM). Additionally, both compounds significantly decreased TNF-α levels, indicating their potential as promising anti-neuroinflammatory agents.

Identification and anti-inflammatory activity of flavonoids from Cardiospermum halicacabum in murine RAW 264.7 macrophage-A bioassay-guided approach

Cardiospermum halicacabum Linn. (CH), known as balloon vine, is used for food and medicinal purposes, including inflammation treatment. In Tamil cuisine, CH stems and leaves feature in curries, crepes, sauces, and soups. While CH's anti-inflammatory effects are documented, its therapeutic compounds are unclear. This study aims to isolate anti-inflammatory constituents from CH using a bioassay-guided approach. CH aerial part was extracted with three different solvents and evaluated for their anti-inflammatory activity. The active ethanol-water extract (CH-EW) was subjected to solvent-solvent partitioning to get five fractions. Among fractions, the methanol fraction (CH-EW-ML) showed potent anti-inflammatory as well as antioxidant activity along with high flavonoid content. Further fractionation of the active methanol fraction resulted in the isolation of two flavonoids, apigenin-7-O-β-D-glucuronide (AAG) and diosmetin-7-O-β-D-glucuronide (DMG). DMG was isolated from CH for the first time. The compounds were evaluated for their nitric oxide (NO) inhibition activity in the RAW 264.7 cell line. DMG showed the most potent activity (IC50 = 16.72 ± 1.01 μM). Further studies showed that DMG can inhibit the production of reactive oxygen species (ROS) and proinflammatory cytokines as well as upregulate the expression of anti-inflammatory cytokines. This study represents the first evidence that DMG can inhibit NO, ROS, TNF-α, and IL-6 while upregulating IL-10. Our findings suggest that incorporating CH infusion into the diet may alleviate inflammation, with DMG being a promising therapeutic component for its anti-inflammatory effects.