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Yes‐associated protein 1 (YAP1) and its paralogue PDZ‐binding motif (TAZ) play pivotal roles in cell proliferation, migration, and invasion, and abnormal activation of these TEAD transcriptional coactivators is found in diverse cancers in humans and mice. Targeting YAP1/TAZ signaling is thus a promising therapeutic avenue but, to date, few selective YAP1/TAZ inhibitors have been effective against cancer cells either in vitro or in vivo. We screened chemical libraries for potent YAP1/TAZ inhibitors using a highly sensitive luciferase reporter system to monitor YAP1/TAZ‐TEAD transcriptional activity in cells. Among 29 049 low‐molecular‐weight compounds screened, we obtained nine hits, and the four of these that were the most effective shared a core structure with the natural product alantolactone (ALT). We also tested 16 other structural derivatives of ALT and found that natural ALT was the most efficient at increasing ROS‐induced LATS kinase activities and thus YAP1/TAZ phosphorylation. Phosphorylated YAP1/TAZ proteins were subject to nuclear exclusion and proteosomic degradation such that the growth of ALT‐treated tumor cells was inhibited both in vitro and in vivo. Our data show for the first time that ALT can be used to target the ROS‐YAP pathway driving tumor cell growth and so could be a potent anticancer drug., YAP1 and its paralogue TAZ play pivotal roles in cell proliferation, migration, and invasion, and abnormal activation of these TEAD transcriptional coactivators is found in diverse cancers in humans and mice. We screened chemical libraries for potent YAP1/TAZ inhibitors using a highly sensitive luciferase reporter system to monitor YAP1/TAZ‐TEAD transcriptional activity in cells. We found that alantolactone primarily targets the ROS‐YAP pathway driving tumor cell growth and so could be a potent anticancer drug.

C-17-sesquiterpenoids are a group of natural products that have been recently discovered. These compounds have the peculiarity of lacking the alpha,beta-methylene butyrolactone system, which is known to be quite relevant for many of the biological activities reported for sesquiterpene lactones. Unfortunately, the biological interest of C-17-sesquiterpenoids has not been studied in-depth, mainly due to the poor isolation yields in which they can be obtained from natural sources. Therefore, in order to allow a deeper study of these novel molecules, we have worked out a synthetic pathway that provides C-17-sesquiterpenoids in enough quantities from easily accessible sesquiterpene lactones to enable a more thorough investigation of their bioactivities. With this synthesis method, we have successfully synthesized, for the first time, three natural C-17-sesquiterpenoids, pertyolides A, B, and C, with good overall yields. Furthermore, we have also evaluated their phytotoxicity against etiolated wheat coleoptiles and corroborated that pertyolides B and C present strong phytotoxic activity., This research was supported by the Ministerio de Economia, Industria y Competitividad (MINEICO), Spain, AGL2017-88083-R.

Reactive oxygen species are implicated in multiple pathological conditions including erectile dysfunction. This study evaluated the in vitro and in vivo antioxidant potential of the methanolic extracts of Inula glomerata and Salacia kraussii. The plant materials were pulverized and extracted with methanol. The phytochemical analysis, ability of the crude extracts to scavenge free radicals (ABTS, DPPH, NO.) in vitro as well as the total phenolic and flavonoid contents was investigated. In vivo, antioxidant potentials of the crude extracts (50/250 mg/kg body weight) were determined in an erectile dysfunction rat model. The phytochemical analysis revealed that both plants contain flavonoids, tannins, terpenoids, and alkaloids. The crude extracts at varying degree of efficiency, scavenged ABTS and DPPH radicals. The crude extracts at low concentrations (50 mg/kg b.w) significantly (p

Context Traditionally, Inula racemosa Hook. f. (Asteraceae) has been reported to be effective in cancer treatment which motivated the authors to explore the plant for novel anticancer compounds. Objective To isolate and characterize new cytotoxic phytoconstituents from I. racemosa roots. Materials and methods The column chromatography of I. racemosa ethyl acetate extract furnished a novel sesquiterpene lactone whose structure was established by NMR (1D/2D), ES-MS and its cytotoxic properties were assessed on HeLa, MDAMB-231, and A549 cell lines using MTT and LDH (lactate dehydrogenase) assays. Further, morphological changes were analyzed by flow cytometry, mitochondrial membrane potential, AO-EtBr dual staining, and comet assay. Molecular docking and simulation were performed using Glide and Desmond softwares, respectively, to validate the mechanism of action. Results The isolated compound was identified as racemolactone I (compound 1). Amongst the cell lines tested, considerable changes were observed in HeLa cells. Compound 1 (IC50 = 0.9 µg/mL) significantly decreased cell viability (82%) concomitantly with high LDH release (76%) at 15 µg/mL. Diverse morphological alterations along with significant increase (9.23%) in apoptotic cells and decrease in viable cells were observed. AO-EtBr dual staining also confirmed the presence of 20% apoptotic cells. A gradual decrease in mitochondrial membrane potential was observed. HeLa cells showed significantly increased comet tail length (48.4 µm), indicating broken DNA strands. In silico studies exhibited that compound 1 binds to the active site of Polo-like kinase-1 and forms a stable complex. Conclusions Racemolactone I was identified as potential anticancer agent, which can further be confirmed by in vivo investigations.

Impact of various ultrasound pretreatment and microwave drying parameters on the qualitative and antioxidant characteristics of Inula viscosa (L.) was investigated in this study. The leaves of Inula viscosa (L.) were sonicated for 10, 20, and 30 min in an ultrasonic bath (37 kHz, 150 Watts). Microwave drying was done at three distinct times (1, 3, and 5 min) and with three different microwave power levels (100, 180, and 300 Watts). Microwave dried samples were tested for color characteristics (L*, a*, b*), chlorophyll, carotenoid, total phenol, and antioxidant content. All dried samples were prepared by infusing them in hot water as tea, and the sensorial properties of teas including odor, color, aroma, and overall acceptability were evaluated by panelists. For 10, 20, and 30 min of ultrasound pretreatment, the L* values of leaves varied from 37.70 to 49.76, 34.97 to 46.25, and 27.88 to 43.34, respectively. The total carotenoid concentration ranged from 0.12 to 0.32 mg/g DW, while the total chlorophyll content was from 0.44 to 0.94 mg/g DW. The antioxidant activity of Inula viscosa (L.) leaves that were dried at 300 Watts for 5 min did not change significantly as a result of ultrasound pretreatment. There was a significant positive correlation between aroma and TPC, as well as between color and overall acceptability. The darkest-colored teas were deemed preferable by the panelists.

Flowers of

Recent studies have shown that Nur77 and AMPKα play an important role in regulating adipogenesis and isoalantolactone (ISO) dual-targeting AMPKα and Nur77 inhibits adipogenesis. In this study, we hypothesized that

Inulin is a natural polysaccharide abundant in plants. In the latest decades, in Mongolia, have been cultivated some plants which used in traditional medicine. Inulin polysaccharides were isolated from the roots of the Helianthus tuberosus L. and Inula helenium L. by ultrasound-assisted, microwave extraction, and conventional extraction methods. This polysaccharide is light yellow, tasteless, powder. The polysaccharide structure was confirmed by infrared spectroscopy (FT-IR). The poly fructose content of the Helianthus tuberosus L. ranged from 69 to 84%; in comparison, Inula helenium L ranged from 13 to 51%. The IR-FT spectra revealed typical inulin structure - 820, 876, and 937 cm-1 with terminated α-D-glucose residue. Булцуут цэцэг (Helianthus tuberosus l.) Өндөр зоосон цэцэг (Inula helenium l.) -ийн үндэснээс инулин гарган авах боломж Инулин нь ургамалд элбэг байдаг байгалийн полисахарид бөгөөд манай оронд инулинаар баялаг зарим төрлийн ургамлыг амжилттай нутагшуулан тарималжуулж байгаа билээ. Манай оронд нутагшсан Булцуут цэцэг (Helianthus tuberosus L.) болон Өндөр зоосон цэцэг (Inula helenium L.) ургамлын үндэснээс инулин полисахаридыг хэт авиа (ХА), богино долгион (БД) болон уламжлалт хандлах аргын тусламжтайгаар ялган авлаа. Энэ полисахарид нь ямар нэгэн амтгүй, цайвар шаргал өнгөтэй, нунтаг хэлбэртэй. Уг полисахаридын бүтцийг нил улаан туяаны спектроскопийн (FT-IR) аргаар баталгаажуулсан ба инулины агууламжийг нийт фруктозод шилжүүлэн тооцов. Булцуут цэцгийн полифруктаны агууламж 69-84%, Өндөр зоосон цэцгийнх 13-51% хооронд хэлбэлзэж байсан бөгөөд богино долгионы тусламжтай ялган авсан инулины полифруктаны агууламж хамгийн өндөр байв. НУТ-ны спектрийн шингээлтээр инулины бүтцийн гол зурвасууд нь 820, 876 саяны хэсэгт болон фураноз хэлбэртэй b-D-фруктоз, харин 937 см-1 саяны хэсэгт пираноз хэлбэртэй a-D-глюкозын үлдэгдэл байгааг харуулж байна. Түлхүүр үг: булцуут цэцэг, инулин, НУТ спектроскоп, өндөр зоосон цэцэг, полифруктан

Context Alantolactone, the bioactive component in Inula helenium L. (Asteraceae), exhibits multiple biological effects. Objective We aimed to determine the anti-inflammatory effect of alantolactone in a collagen-induced arthritis (CIA) mouse model and its immunomodulatory effects on Th17 differentiation. Materials and methods A CIA mouse model was established with DBA/1 mice randomly divided into four groups (n = 6): healthy, vehicle and two alantolactone-treated groups (25 or 50 mg/kg), followed by oral administration of alantolactone to mice for 21 consecutive days after arthritis onset. The severity of CIA was evaluated by an arthritic scoring system and histopathological examination. Levels of cytokines and anti-CII antibodies as well as percentages of splenic Th17 and Th17 differentiation with or without alantolactone treatments (0.62, 1.2 or 2.5 μM) were detected with ELISA and flow cytometry, respectively. Western blot analysis was used to evaluate intracellular signalling in alantolactone-treated spleen cells. Results In CIA mice, alantolactone at 50 mg/kg attenuated RA symptoms, including high arthritis scores, infiltrating inflammatory cells, synovial hyperplasia, bone erosion and levels of the proinflammatory cytokines TNF-α, IL-6 and IL-17A, but not IL-10 in paw tissues. Alantolactone also reduced the number of splenic Th17 cells and the capability of naïve CD4+ T cells to differentiate into the Th17 subset by downregulating STAT3/RORγt signalling by as early as 24 h of treatment. Discussion and conclusions Alantolactone possesses an anti-inflammatory effect that suppresses murine CIA by inhibiting Th17 cell differentiation, suggesting alantolactone is an adjunctive therapeutic candidate to treat rheumatoid arthritis.

Phytochemical study of the chloroform extract of the aerial parts of Inula germanica L., I. ensifolia L., I. conyza (Griess.) DC. and I. salicina L. led to the identification of 33 terpenoids. ?- and ?-amyrin, lupeol, taraxasterol, ?-taraxasterol and their 3-O-acetates and 3-O-palmitates were identified by GC/MS. In addition, the structures of 3-O-palmitates of mainaladiol, arnidiol, faradiol and 16-hydroxylupeol were confirmed by NMR. ent-Kaur-16-en-19- -oic acid and its 15?-(3-methylpentanoyloxy) and 15?-(3-methylbutanoyloxy) derivatives were isolated from I. conyza. Ten closely related sesquiterpene lactones (germacranolides and melampolides) were found in I. germanica and their structural identification was performed by spectral analyses. I. ensifolia and I. salicina were free of sesquiterpene lactones and diterpenoids. All triterpenoids and diterpenoids, grazielia acid, desacetylovatifolin and 8-(2-methylbutanoyloxy)- 1(10),4,11(13)-germacrutrien-6,12-olide-14-oic acid are described for the first time in the studied species. The principal component analysis was used to find a relationship between th? investigated up to now Inula species, growing in Bulgaria.

The aim of the research is to determine the total antioxidant activity of in vitro collection of antihepatotoxic action consisting of roots and rhizomes of Inula helenium L., grass Centaurium erythraea Rafn., flowers Tanacetum vulgare L., fruits Rosa sp., fruits of Crataegus sp. аnd its separate components by the method of colonometric titration and determination of antioxidant activity of dry extract (conditional name "Pentafite") obtained from this collection under conditions of experimental tetrachloride of carbon hepatitis in white rats. A method of chemiluminescent lipid analysis was used to evaluate the free radical oxidation of lipids in liver in test animals. It has been found that collection of antihepatotoxic action and plants included in it have antioxidant activity in vitro, at the same time synergistic effect on manifestation of total antioxidant activity of collection is revealed. Pharmacotherapy of experimental hepatitis in experimental rats by administration of Pentafite at a dose of 300 mg/kg has been found to significantly reduce the chemiluminometric values of lipids, which characterize the intensity of free radical reactions. "Pentafite" has a pronounced inhibitory effect on hyperlipoperoxidation in animal liver in case of toxic damage to it. The established antioxidant activity of collecting antihepatotoxic action and Pentafite extract may be important for their use in the treatment and prevention of hepatobiliary diseases.

This study aimed to investigate the antioxidant, antimicrobial, and cytotoxic potential of ethanolic extracts obtained from

In a globalized world, plant invasions are common challenges for native ecosystems. Although a considerable number of invasive plants form arbuscular mycorrhizae, interactions between arbuscular mycorrhizal (AM) fungi and invasive and native plants are not well understood. In this study, we conducted a greenhouse experiment examining how AM fungi affect interactions of co-occurring plant species in the family Asteracea, invasive Echinops sphaerocephalus and native forb of central Europe Inula conyzae. The effects of initial soil disturbance, including the effect of intact or disturbed arbuscular mycorrhizal networks (CMNs), were examined. AM fungi supported the success of invasive E. sphaerocephalus in competition with native I. conyzae, regardless of the initial disturbance of CMNs. The presence of invasive E. sphaerocephalus decreased mycorrhizal colonization in I. conyzae, with a concomitant loss in mycorrhizal benefits. Our results confirm AM fungi represent one important mechanism of plant invasion for E. sphaerocephalus in semi-natural European grasslands.

The chemical composition and the biological activities of aromatic plants may be influenced by seasonal changes. Therefore, the essential oil of Inula graveolens (IGEO), collected at Chebba salt marsh, was studied in terms of yields, compositions and biological activities, throughout four different seasons, namely spring, summer, autumn and winter (April, July, October and January, respectively). GC/MS analysis identified 30 compounds. Mostly quantitative rather than qualitative, variation was observed in the oil composition of each sample. It had been revealed a predominant presence of bornyl acetate and borneol, as well as significant differences of several compound amounts in function of the seasonal change. Biological activities were also related to the harvest season; hence, IGEO from spring gave the best antioxidant activity results and IGEO from autumn seemed to be the most potent against pathogenic microorganisms, while oils from summer and winter were the strongest inhibitors of acetylcholinesterase and tyrosinase.A matrix linking IGEO major compounds to biological was composed to identify relationships between concentrations of the volatile molecules and the biological activities of the samples. Furthermore, the seasonal variation of these main volatile constituents was also investigated through principal compound analysis (PCA). The obtained results revealed that each biological activity depends on the seasonal fluctuation of the amounts of certain chemical compounds. Keywords: Inula graveolens, Essential oil, Seasonal variations, Chemical composition, Biological activities, PCA

The genus Inula belongs to family Asteraceae and it is medicinally important because it possesses cytotoxic, anticancer, hepatoprotective, antibacterial and anti-inflammatory properties. The aim of this research was to explore antioxidant and anti-urease activities of fifteen Inula taxa in Turkey. Ethanol extracts of Inula taxa were obtained by Soxhlet extraction. Antioxidant activity was determined through total antioxidant activity, total phenolic content and copper reducing antioxidant capacity (CUPRAC) analyses. The highest total phenolic content and total antioxidant capacity were found in I. orientalis (158.54?0.002 ?g GAE/mL) and I. macrocephala (189.16?0.002 ?g AAE/mL). CUPRAC activity increases with the increasing concentration of the extracts and the standard. Moreover, all the tested plants exhibited better anti-urease activity than standard thiourea except for I. anatolica and I. thapsoides subsp. thapsoides. Results obtained from this study demonstrate that Inula species might be utilized as a probable natural source in the pharmaceutical and food industries but further and more specific studies are needed to determine active antioxidative and anti-urease compounds in the extracts.

The investigation of natural and safe antioxidants from natural origin is highly encouraged since it was revealed that synthetic antioxidants have restricted use in foods due to their toxicological effects and suspected carcinogenic potential. Purification of most active phenolics from the halophyte Inula crithmoїdes was the objective fixed for this work. The separation of the flower phenolics was carried using centrifugal partition chromatography (CPC) and yielded 24 fractions. A bio-guided selection of the most active fractions was done based on their antioxidant activities. Fractions 2, 7, 11 and 19 were the most active ones, even more potent than positive controls BHT, BHA and ascorbic acid. The semi-preparative High Performance Liquid Chromatography (HPLC) purification of the antioxidant molecules from these active fractions and their identification by Nuclear Magnetic Resonance spectroscopy (NMR) revealed that the most potent phenolics of I. crithmoїdes are the chlorogenic acid and its two derivatives 3-p-coumaroyl-5-caffeoyl quinic acid and 1,5-di-O-caffeoylquinic acid, in addition to the quercetin and its derivative quercimeritrin. All identified compounds are powerful antioxidants, as they have many biological properties allowing their use in agro-food, pharmaceutical or cosmetic industries. Keywords: Inula crithmoїdes, CPC, Antioxidant activities, Phenolics, HPLC, MNR

The protective and mutagen-modifying activity of the complex of biologically active substances(BAS) in the extract from the underground part of the plant Inula britannica in the cells of the visceral organs of laboratory mice was studied. Alkaline variation of the comet assay was used to determine genotoxic/antigenotoxic activity. The frequency of single-stranded DNA breaks in the cells of the brain andbone marrow, lungs, heart, kidneys, liver, stomach, spleen was assessed by the following parameters: %of DNA in tail, Olive tail moment, damage index. It was found that extracts of BAS in concentrations of100.0 mg/l and 150.0 mg/l did not show genotoxic activity, the frequency of single-strand breaks in allstudied organs did not statistically significantly exceed the spontaneous level in intact animals. Whenexposed to asymmetric dimethylhydrazine (UDMH), the cells of the studied organs showed a statisticallysignificant increase in the number of single-stranded DNA breaks compared to intact laboratory mice.When combined with UDMH as a positive control, extract of Inula britannica significantly reduces thegenotoxic effect of xenobiotics. The frequency of DNA breaks in animals that simultaneously receivedUDMH and Inula britannica extract was statistically significantly lower compared with mice that received only UDMH. All this suggests the presence of antimutagenic and antigenotoxic activity in theextract of Inula britannica.Key words: Inula britannica, biologically active substances, mutagen, antimutagen, genotoxicity,DNA comet assay.

In this study the possibility of using liquidInula viscosa(Dittrichia viscosa L.) to improve the growth and quality ofOscularia deltoidesandCorpuscolaria lehmaniiplants and protection againstAphis neriiwas evaluated. The 3 experimental groups in cultivation were: i) group without the use ofInula viscosaliquid macerate (CTRL), irrigated with water and previously fertilised substrate; ii) group treated with 1% ofInula viscosaliquid obtained from flowers (leaf spraying and soil irrigation), previously fertilized substrate (INU1); iii) group treated with 1% ofInula viscosaliquid obtained from leaves and stems (leaf spraying and soil irrigation), previously fertilized substrate (INU2). The test showed a significant increase in the agronomic parameters analyzed in plants treated with liquidInula viscosa. In fact, all plants treated with Inula showed a significant increase in plant height, leaves number, vegetative and roots weight, branches and flowers number and flowering time in bothCorpuscolaria lehmaniiandOscularia deltoides. An evaluation was also made of the number of individuals ofAphis neriipresent on the plants ofCorpuscolaria lehmaniiandOscularia deltoidesto assess whether the macerate of Inula can be used for the control of these insects. The GC-MS analysis of active fractions strongly suggested costic acid as the compound responsible for contact toxicity againstAphis nerii. Probably in the plant treated withInula viscosathere is an induction of the defense mechanisms that lead to greater resistance to biotic and abiotic stresses. The application of Inula macerate also improves the plant's defences against attacks by fungal pathogens and insects. Very interesting aspects, especially in view of a possible reduction of fertilizers and synthetic plant protection products.

With antimicrobial resistance rising globally, the exploration of alternative sources of candidate molecules is critical to safeguard effective chemotherapeutics worldwide. Plant natural products are accessible, structurally diverse compounds with antimicrobial potential. The pharmacological applications of plants in medicine can be guided by the attestation of traditional use, as demonstrated in this study. In Irish ethnomedical literature

Acute lung injury (ALI) is a severe respiratory disease characterized by diffuse lung interstitial and respiratory distress and pulmonary edema with a mortality rate of 35%-40%. Inula japonica Thunb., known as "Xuan Fu Hua" in Chinese, is a traditional Chinese medicine Inulae Flos to use for relieving cough, eliminating expectorant, and preventing bacterial infections in the clinic, and possesses an anti-pulmonary fibrosis effect. However, the effect and action mechanism of I. japonica on ALI is still unclear.This study aimed to investigate the protective effect and underlying mechanism of total flavonoids of I. japonica (TFIJ) in the treatment of ALI.A mouse ALI model was established through administration of LPS by the intratracheal instillation. Protective effects of TFIJ in the inflammation and oxidative stress were studied in LPS-induced ALI mice based on inflammatory and oxidative stress factors, including MDA, MPO, SOD, and TNF-α. Lipid metabolomics, bioinformatics, Western blot, quantitative real-time PCR, and immunohistochemistry were performed to reveal the potential mechanism of TFIJ in the treatment of ALI.TFIJ significantly alleviated the interstitial infiltration of inflammatory cells and the collapse of the alveoli in LPS-induced ALI mice. Lipid metabolomics demonstrated that TFIJ could significantly affect the CYP2J/sEH-mediated arachidonic acid metabolism, such as 11,12-EET, 14,15-EET, 8,9-DHET, 11,12-DHET, and 14,15-DHET, revealing that sEH was the potential target of TFIJ, which was further supported by the recombinant sEH-mediated the substrate hydrolysis in vitro (ICThese results demonstrated that TFIJ could suppress the sEH activity to stabilize the level of EETs, allowing the alleviation of the pathological course of lung injury in LPS-treated mice, which suggested that TFIJ could serve as the potential agents in the treatment of ALI.

Acute lung injury (ALI) is a life-threatening lung disease and characterized by pulmonary edema and atelectasis. Inula japonica Thunb. is a commonly used traditional Chinese medicine for the treatment of lung diseases. However, the potential effect and mechanism of total terpenoids of I. japonica (TTIJ) on ALI remain obscure.This study focused on the protective effect of TTIJ on lipopolysaccharide (LPS)-induced ALI in mice and its potential mechanism.A mouse model of ALI was established by intratracheal instillation of LPS to investigate the protective effect of TTIJ. RNA-seq and bioinformatics were then performed to reveal the underlying mechanism. Finally, western blot and real-time qPCR were used to verify the effects of TTIJ on the inflammation and oxidative stress.TTIJ notably attenuated LPS-induced histopathological changes of lung. The RNA-seq result suggested that the protective effect of TTIJ on LPS-induced ALI were associated with the Toll-like receptor 4 (TLR4) and nuclear factor-erythroid 2-related factor 2 (Nrf2) signaling pathways. Pretreatment with TTIJ significantly reduced the inflammation and oxidative stress via regulating levels of pro-inflammatory and anti-oxidative cytokines, such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), superoxide dismutase (SOD), and glutathione (GSH), in LPS-induced ALI mice. TTIJ treatment could suppress the cyclooxygenase-2 (COX-2) expression level and the phosphorylation of p65, p38, ERK, and JNK through the inactivation of the MAPK/NF-κB signaling pathway in a TLR4-independent manner. Meanwhile, TTIJ treatment upregulated expression levels of proteins involved in the Nrf2 signaling pathway, such as heme oxygenase-1 (HO-1), NAD(P)H: quinoneoxidoreductase-1 (NQO-1), glutamate-cysteine ligase catalytic subunit (GCLC), and glutamate-cysteine ligase modifier subunit (GCLM), via activating the Nrf2 receptor, which was confirmed by the luciferase assay.TTIJ could activate the Nrf2 receptor to alleviate the inflammatory response and oxidative stress in LPS-induced ALI mice, which suggested that TTIJ could serve as the potential agent in the treatment of ALI.

Duhaldea pterocaula (Franch.) Anderb, also known as Inula pterocaula Franch (I. pterocaula), is a folk medicine of the Yi nationality in China. The Inula plants display various biological activities, including anti-nociceptive and anti-inflammatory properties. I. pterocaula has been traditionally used for the treatment of bronchitis, vasculitis, and dizziness. However, very few studies have been reported on the pharmacology of I. pterocaula. The present study aims to characterize the anti-nociceptive and anti-inflammatory properties of I. pterocaula and explore the underlying mechanism. I. pterocaula was extracted by 95% ethanol and further portioned with petroleum ether, ethyl acetate (EA) and n-butanol, sequentially, to obtain corresponding factions with different polarities. The EA fraction (IPEA) was found to be one of the most effective fractions. It demonstrated potent analgesic effects in both acute and inflammatory pain mouse models, and caused no anti-nociceptive tolerance. Furthermore, IPEA improved the tolerance of mice to morphine. IPEA also showed potent anti-inflammatory effects on LPS-induced septic mice. BIC, a GABAAR antagonist, reversed the effects of IPEA in pain and inflammation models. Collectively, GABAARs play a key role in the pharmacological effects of IPEA. I. pterocaula may be useful as a complementary or alternative therapeutic agent for the treatment of pain and inflammation.

Given the undesirable side effects of commercially used mouth rinses that include chemically synthesized antimicrobial compounds such as chlorhexidine, it is essential to discover novel antimicrobial substances based on plant extracts. The aim of this study was to examine the antimicrobial effect of Inula viscosa extract on the initial microbial adhesion in the oral cavity. Individual test splints were manufactured for the participants, on which disinfected bovine enamel samples were attached. After the initial microbial adhesion, the biofilm-covered oral samples were removed and treated with different concentrations (10, 20, and 30 mg/mL) of an I. viscosa extract for 10 min. Positive and negative controls were also sampled. Regarding the microbiological parameters, the colony-forming units (CFU) and vitality testing (live/dead staining) were examined in combination with fluorescence microscopy. An I. viscosa extract with a concentration of 30 mg/mL killed the bacteria of the initial adhesion at a rate of 99.99% (log10 CFU value of 1.837 ± 1.54). Compared to the negative control, no killing effects were determined after treatment with I. viscosa extract at concentrations of 10 mg/mL (log10 CFU value 3.776 ± 0.831, median 3.776) and 20 mg/mL (log10 CFU value 3.725 ± 0.300, median 3.711). The live/dead staining revealed a significant reduction (p &lt, 0.0001) of vital adherent bacteria after treatment with 10 mg/mL of I. viscosa extract. After treatment with an I. viscosa extract with a concentration of 30 mg/mL, no vital bacteria could be detected. For the first time, significant antimicrobial effects on the initial microbial adhesion in in situ oral biofilms were reported for an I. viscosa extract.

Oxidative stress is linked to several invasive diseases which causes significant clinical and economic impact, therefore, there is a need to develop new antioxidants. The natural products could play an important role in overcoming the current need. In the present work, the antioxidant bioassay-guided fractionation of the ethanolic extract of Inula viscosa leaves (Asteraceae) was performed using DPPH and ABTS assays affording three known compounds, which were successfully characterized as ilicic acid (1), taxifolin (2) and quercetin (3) based on 1D, 2D NMR. Compounds 2 and 3 were identified as the most active, displaying similar or higher potency against ABTS (value 41.27 for quercetin and 142.58 for taxifolin) and similar activity against DPPH (value 41.27 for quercetin and 142.58 for taxifolin) than the well-known reference, ascorbic acid (value 65.36 for quercetin and 58.43 for taxifolin) but less potency than the standard gallic acid. The discussion of SAR of the antioxidant potential revealed that the type of natural product is crucial for the activity and the substitution pattern on the flavonoid skeleton modulate the antioxidant profile. Our findings show that I. viscosa leaves may be a natural source of antioxidants and once again the role of flavonoids health benefits is more strongly endorsed.

SUMMARY OBJECTIVE: Crude oil extracts, components of extracts, and ethanolic extracts of Inula graveolens possess various pharmacological activities on various cancer cells including antioxidative and antiproliferative effects. Aqueous extract of this species has not been investigated on the liquid malignancies and solid tumors with a high incidence of treatment refractoriness and poor survival outcomes such as glioblastoma and leukemia. Hence, the present study aimed to evaluate the cytotoxic efficiency of I. graveolens aqueous extracts on human glioblastoma multiforme and chronic myelogenous leukemia cell lines in comparison to non-cancerous primary rat cerebral cortex and human peripheral blood mononuclear cells. METHODS: The cells were treated with the extracts of I. graveolens (125–1000 μg/mL) for 48 h, the cellular viability was identified using 3'-(4,5dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay, and lactate dehydrogenase release was measured to determine the cytotoxic potential. Total oxidant status and apurinic/apyrimidinic endodeoxyribonuclease 1 assays were used to determine the oxidative status of cells and DNA damage, respectively. RESULTS: I. graveolens showed selective cytotoxicity toward human glioblastoma multiforme and chronic myelogenous leukemia cell lines and exhibited a higher antiproliferative effect against cancer cells in comparison to non-cancerous cells. Moreover, it significantly reduced the apurinic/apyrimidinic endodeoxyribonuclease 1 levels on both cancer cell lines as compared with their control cells without changing the levels of an oxidative stress marker. CONCLUSION: The extracts of I. graveolens have anti-cancer potential on human glioblastoma multiforme and chronic myelogenous leukemia cell lines without causing oxidative stress.

The nutritional composition and productivity of halophytes is strongly related to the biotic/abiotic stress to which these extremophile salt tolerant plants are subjected during their cultivation cycle. In this study, two commercial halophyte species (Inula crithmoides and Mesembryanthemum nodiflorum) were cultivated at six levels of salinity using a soilless cultivation system. In this way, it was possible to understand the response mechanisms of these halophytes to salt stress. The relative productivity decreased from the salinities of 110 and 200 mmol L−1 upwards for I. crithmoides and M.&nbsp, nodiflorum, respectively. Nonetheless, the nutritional profile for human consumption remained balanced. In general, I. crithmoides vitamin (B1 and B6) contents were significantly higher than those of M. nodiflorum. For both species, β-carotene and lutein were induced by salinity, possibly as a response to oxidative stress. Phenolic compounds were more abundant in plants cultivated at lower salinities, while the antioxidant activity increased as a response to salt stress. Sensory characteristics were evaluated by a panel of culinary chefs showing a preference for plants grown at the salt concentration of 350 mmol L−1. In summary, salinity stress was effective in boosting important nutritional components in these species, and the soilless system promotes the sustainable and safe production of halophyte plants for human consumption.

Research goal:Based on the information obtained from the literature onInula viscosa, in particular on the insecticidal and antifungal capacities of this plant, the aim of this work was to carry out further experiments on a macerate based onInula viscosa, microorganisms and algae in order to evaluate the bio stimulant and biocontrol capacities on rose plants obtained from seed. Materials and Methods:The experiments, which started in January 2021, were conducted in the greenhouses of CREA-OF in Pescia (Pt). The experiment was divided into two parts. A seed germination test and a plant growth test, both conducted during the same experiment. The four experimental groups in cultivation were: i) group without biofertilizer, irrigated with water and previously fertilized substrate; ii) group with Inula biofertilizer, microorganisms and algae (INORT); iii) group with algae (Ascophyllum nodosumextract); iv) group with beneficial bacteria. Results and Discussion:The test showed a significant increase in the agronomic parameters analysed in plants treated with the INORT biofertilizer on seed roses. The test also showed greater control of the pathogenSphaerotheca pannosa var. rosaein seedlings sprayed with the biofertilizer. In fact, all plants treated with INORT showed a significant increase in the height and number of leaves per plant, in the vegetative and root weight of the plants, in the number and duration of flowers, a reduction in the attack of the pathogenSphaerotheca pannosa var. rosae, an increase in seed germination and a reduction in the average germination time. Conclusions:The experiment at CREA-OF in Pescia has therefore demonstrated how the application of a macerate based onInula viscosa, microorganisms and algae can significantly improve the cultivation and quality of seed rose plants. As in other experiments, the application of this biostimulant also determined positive effects in the control of pathogenic fungi, in particularSphaerotheca pannosa var. rosae. Other investigations are currently underway to study the biostimulant and desiccant capacities of the Inula plant, depending on the harvesting methods, the physiological state of the plants, the extraction method, the type of culture medium, the type and timing of maceration. The association with various microbial consortia and other plant-derived biostimulants will also be evaluated.

Background General antiviral agents such as oseltamivir are associated with certain adverse effects and the emergence of resistance. This study investigated the phytochemical properties, antiviral activities, and safety of three herbs used in traditional Korean medicine. Methods Extracts of three medicinal herbs (Brassica juncea, Forsythia suspensa, and Inula britannica) were prepared using ethanol or water. The total phenolic, flavonoid, and saponin content, condensed tannin content, and reducing sugar content of the herb extracts were determined via phytochemical screening. Tandem mass analysis was performed using an ultra-performance liquid chromatography (UPLC)-electrospray ionization (ESI)-Q/Orbitrap instrument. Virus titrations were determined via tissue culture infective dose (TCID50) and cytotoxicity assays. Hemolysis and hepatotoxicity were measured to determine safety. Results Among the three medicinal herbs, F. suspensa showed the highest concentration of phenolic compounds, flavonoids, and saponins. The number of phytochemical compounds detected via tandem mass analysis of B. juncea, F. suspensa, and I. britannica was 5 (including sinigrin, m/z [M-H] = 358.02), 14 (including forsythoside A, m/z [M-H] = 623.19), and 18 (including chlorogenic acid, m/z [M-H] = 353.20), respectively. The antiviral effects of the B. juncea extracts (ethanol and water) and I. britannica extract (ethanol) were further investigated. The ethanol extract of B. juncea showed a 3 Log TCID50/25 μL virus titration reduction and the water extract showed a selectivity index of 13.668 against infected influenza H1N1 virus A/NWS/33. The B. juncea extracts did not show hemolysis activities and hepatotoxicity (I. britannica showed the most effective virus titration decrease, whereas its hemolytic and hepatotoxicity values were the most significantly different compared to the control. Despite the high concentration of phytochemicals detected in F. suspensa, the extract showed approximately 1 Log TCID50/25 μL at the highest concentration. Conclusion B. juncea may show antiviral effects against H1N1 in a host. In addition, B. juncea may also show decreased disadvantages compared to other antiviral agents.

One new eudesmane sesquiterpenoid, 11β-hydroxy-13-chloro-eudesm-5-en-12, 8-olide (1), was isolated from the roots of Inula helenium together with nine eudesmanolides (2–10) and one germacranolide (11). Their structures were elucidated on the basis of detailed spectroscopic analyses. All isolates were evaluated for their antiproliferative activities against human leukemia stem-like cell line KG1a. Compound 10 exhibited the most potent effect with the IC50 value of 3.36 ± 0.18 μM. A further investigation revealed that compound 10 could significantly induce apoptosis of KG1a cells. Additionally, compound 10 had an obvious effect on the levels of apoptosis-related proteins (Bcl-2, Bax, cytochrome c, caspase 9 and caspase 3), indicating that the antiproliferative effect of compound 10 on KG1a cells might be mediated through a mitochondria-dependent apoptotic pathway.

Heliaquanoid A (1), the first exo-2,4-linked Diels−Alder adduct between a pseudoguaianolide dienophile and a guaianolide diene, and heliaquanoids B−E (2−5), four new 2,4-linked Diels−Alder adducts between a xanthanolide dienophile and a guaianolide diene, were isolated from stems and leaves of Inula helianthus-aquatica. Their structures were determined by the NMR spectroscopy, modified Mosher′s method, electronic circular dichroism, and X-ray diffraction analysis. Compounds 2 and 3 exhibited moderate cytotoxic activities against HL-60 cells with IC50 values of 7.5 and 4.9 μM, respectively.

Objective: To evaluate the antibacterial and antifungal activity of three different medicinal plants invitro. Oil extracts of the plants from three different families (Hedyotis corymbosa, Inula racemose, Holostemma adakodien) are used to find the antibacterial and antifungal activity. Methods: Study of anti-microbial activity using agar cup diffusion method, inoculums preparation, Anti-bacterial activity screening (well diffusion method), Anti-fungal activity screening (well diffusion method) are the different methods which are used to find the anti-bacterial and anti-fungal activities of the oil extracts of the above medicinal plants. The activity of these oil extracts and the selected antibiotics are evaluated against four bacterial strains (E. Coli, S. aureus and P. aeruginosa) and three Candida fungal strains (albicans, parapsilosis and tropicalis.). The anti microbial activity of Hedyotis corymbosa, Inula racemose, Holostemma adakodien oil extracts zone of inhibition evaluation was compared with positive control of fungal strain Fluconozole and bacterial strain Norfloxacin, Cefepime and Gatifloxacin. Results: The anti microbial activity of Hedyotis corymbosa, Inula racemose, Holostemma adakodien oil extracts zone of inhibition evaluation was compared with positive control of fungal strain Fluconozole and bacterial strain Norfloxacin, Cefepime and Gatifloxacin. Further studies are needed to explore the novel antibacterial bioactive molecules. Conclusion: The plants Hedyotis corymbosa, Inula racemose and Holostemma adakodien have shown significant anti-bacterial and anti-fungal activity.

The level of studying of Inula L. genus species, growing on the territory of Ukraine, is insufficient today. The study of chemical composition, accumulation of biologically active substances, pharmacological action of investigated grass species’ extracts of Inula L. genus of Ukrainian flora are of current interest. The aim of the work is making qualitative and comparative analysis of ascorbic, organic acids and tannic substances content in the raw material of investigated species of Inula L. genus ( Inula britannica L. and Inula helenium L.). Quantitative determination was carried out by volume titration method. The presence of ascorbic acid, organic acids and tannic substances in the raw material of Inula L. genus investigated species was established with the help of paper chromatography and thin-layer chromatography methods. The quantitative determination of total organic acids was carried out according to XI edition of State Pharmacopoeia methods in terms of malic acid. Water extracts were studied for the tannins presence in raw material of Inula L. genus investigated species. Compounds identification was carried out through chemical reactions in accordance with Ukrainian State Pharmacopeia. The results obtained showed the perspective of further study of the biological activity of Inula britannica L. and Inula helenium L.

The article presents the geobotanical and some bioecological features of species of the genus Inula L., family Asteraceae (Compositae). The water regime, as well as the water holding capacity, transpiration rate and adaptive ability of plants to drought in the arid zone, is considered. The results of studies on the introduction into the culture based on indicators of the osmotic pressure of cell juice are presented.