1,721,028 research outputs found
Chemical fingerprinting and bioactivity profile of Ayurvedic crude drugs and related preparations
Full text linkMycochemicals against Cancer Stem Cells
No full textSince ancient times, mushrooms have been considered valuable allies of human well-being both from a dietary and medicinal point of view. Their essential role in several traditional medicines is explained today by the discovery of the plethora of biomolecules that have shown proven efficacy for treating various diseases, including cancer. Numerous studies have already been conducted to explore the antitumoural properties of mushroom extracts against cancer. Still, very few have reported the anticancer properties of mushroom polysaccharides and mycochemicals against the specific population of cancer stem cells (CSCs). In this context, β-glucans are relevant in modulating immunological surveillance against this subpopulation of cancer cells within tumours. Small molecules, less studied despite their spread and assortment, could exhibit the same importance. In this review, we discuss several pieces of evidence of the association between β-glucans and small mycochemicals in modulating biological mechanisms which are proven to be involved with CSCs development. Experimental evidence and an in silico approach are evaluated with the hope of contributing to future strategies aimed at the direct study of the action of these mycochemicals on this subpopulation of cancer cells
The Alcoholic Bark Extract of Terminalia Arjuna Exhibits Cytotoxic and Cytostatic Activity on Jurkat Leukemia Cells
No full textBackground: Natural products are characterized by complex chemical composition and
are capable of concurrently modulate several signalling pathways. Considering the biological complexity
of carcinogenesis, natural products represent key components of the therapeutic armamentarium
for oncological diseases. The bark of Terminalia arjuna is used in traditional Ayurvedic
medicine for its astringent, expectorant, cardiotonic, styptic, and antidysenteric properties. Alongside
its traditional uses, Terminalia arjuna exhibits different biological activities including antimutagenic
and anticarcinogenic.
Objective: This study was designed to evaluate the toxic effects of an alcoholic extract obtained
from the bark of T. arjuna on a human T-lymphoblastic cell line (Jurkat). We explored the phytochemical
composition and investigated the cytotoxic, cytostatic, genotoxic, and anti-genotoxic effects.
Methods: The phytochemical composition was analyzed using spectrophotometric methods; all the
biological endpoints were assessed through flow cytometry.
Results: The phytochemical screening showed that polyphenols represent about 64% of the extract.
Moreover, the extract was cytotoxic on Jurkat cells by inducing both apoptosis and necrosis and
blocked the cell cycle in the G2/M phase. Additionally, it was found that the extract lacks any genotoxic
effect, but was not effective in protecting Jurkat cells from the DNA damage induced by H2O2
and etoposide.
Conclusion: The results of our study show the toxic effects of Terminalia arjuna on Jurkat cells
and confirm the pivotal role played by natural compounds in the oncological field. Further studies
should be performed to better understand its clinical potential and deepen its toxicological profile
HP-TLC bioautographic assay as a preliminary research tool to match chemical and biological properties of officinal plant extracts
No full textBioautography is mainly known as a research strategy hyphenated with planar chromatography techniques aimed to detect bioactive chemical classes characterizing plant extracts, pointing out their efficacy directly on the chromatographic support used for their separation. Therefore,thin layer chromatographic (TLC) bioautography gives the opportunity to point out at the same time a semi-quantitative chemical fingerprinting and the bioactivity of the main involved chemical classes in plant extracts (1). Our research group set uppharmaceutical biology studiesdeveloping this particular techniqueemploying high performing thin layer chromatography plates (HP-TLC) to obtain the best separation of the chemical classes together with the best evidence of their possible biological activity,driving further in-depth investigations toward a more focused chemical identification and quantification, and a wider biological activity profile of officinal plant extracts. We optimizedHP-TLC bioautographyfor antimicrobial (antibacterial and antifungal) and antioxidant properties [DPPH, 1,1-diphenyl-2-picrylhydrazyl; and ABTS, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) assays]of different plant extractsevidencingthe chemical classes really involved in the bioactivity (2).Our research strategy of plant extracts is planned to have HP-TLC bioautography as preliminary data giving us the opportunity 1. to point out the chemical compounds with antibacterial, antifungal, antioxidant capacity; 2. to focus on the chemical isolation and identification of fractions characterized by specific bioactive molecules; 3. to check biological capacities ofpure single compounds, or combinations, assaying possible synergic interactions; 4. to explore other biological capacities -i.e. cytotoxic, mutagen and mutagen-preventive activity, etc. - related to those preliminary evaluated through HP-TLC bioautography. In light of these premises, some researches in progress pointing out the role of HP-TLC bioautography in the pharmaceutical biology profile of our studies are shown below:
-Essential oils obtained from plant crude drugs of different geographical origin (for e.g. Cryptocaryamassoia, Lauraceae, from Indonesian regions; Piper aduncuum, Piperaceae; Croton lechleri, Euphorbiaceae from Amazonian Ecuador). Cryptocaryamassoia(Lauraceae) essential oil evidenced on HP-TLC platesrelevant antimicrobial activity related tomassoia lactones,as single pure compounds,versus Gram negative strains (Klebsiellaoxytoca) andyeasts (Candida albicans). These data suggested to test pure compounds mixtures to evaluate their possible synergic potential. The result of combining benzylbenzoate and benzyl salicatewas a specific efficacy against Gram positive bacteria (Enterococcus faecalis). The evidences will also drive the research towards in-depth investigations (cytotoxicity, mutagenicity) of the active isolated compounds and their different qualitative and quantitative combinations. The case of Piper aduncum (Piperaceae) essential oil, characterized by high abundance of dillapiole(45.92%), highlighted this compound as the main responsible of highly selective antibacterial activity against Staphylococcus aureus.Amazonian Croton lechleri essential oil evidenced antibacterial activity against Escherichia colion HP-TLC mainly due to sesquicineole (17.29%).Caryophyllene oxide (1.24%) and 1,10-di-epi-cubenol (4.75%) showed instead the best antioxidant capacity with HP-TLC-DPPH assay.
-126 different plant extracts from industrial (agro-food) and agricultural by-products investigated through HP-TLC bioautography for achieving preliminary suggestions about their possible role as source of bioactive molecules. In this case ethanol, chloroform and acetone extracts have been assayed for matching chemical fingerprinting and biological activity, giving preliminary but clear suggestions about the most promising extracts in terms of bioactivity potential and composition. Among the bioactive extracts, those most interesting were ethanolones obtained from agro-food by-products ofMalusdomestica and Juglansregia, and from agricultural wastes of Allium sativum.
In conclusion, HP-TLC bioautographyrepresent an important tool to quickly join on chromatographic supporta preliminary chemical fingerprinting and important biological evidences of officinal plant extracts.
1) I.M. Choma, E.M. Grzelak (2011) J. Chromatogr. A, 1218, 2684–2691
2) D. Rossi, A. Guerrini, G. Paganetto, G. Bernacchia, F. Conforti, G. Statti, S. Maietti, I. Poppi, M. Tacchini, G. Sacchetti (2013) FoodChem, 139, 439–44
Phytochemical Profile and In Vitro Bioactivities of Plant-Based By-Products in View of a Potential Reuse and Valorization
Full text linkWastes and by-products of plant origin are of particular interest to develop a circular economy approach, which attempts to turn them into resources. In this work, thirty-seven neglected plant matrices, including agricultural residues, pest plants, and by-products from the herbal and food industry were extracted and tested for their in vitro anti-tyrosinase, antioxidant, and antibacterial activity against the phytopathogens Pseudomonas syringae pv. syringae ATCC 19310 and Clavibacter michiganensis subsp. nebraskense ATCC 27822. Antioxidant activity ranged from 0.3 to 5 mg of Tr. eq/mL of plant extract, and extract of Castanea sativa pericarp (Csp), Rosa damascena buds (post-distillation) (Rod), and Prunus amygdalus exocarp and mesocarp (Pam) were the most powerful ones. Csp was also capable of inhibiting tyrosinase (IC50 = 16.5 µg/mL), as well as three distillation by-products, namely: Cupressus sempervirens (Css) (IC50 = 95.5 µg/mL), Salvia officinalis (Sco) (IC50 = 87.6 µg/mL), and Helichrysum italicum (Hei) (IC50 = 90.1 µg/mL). Five residues from distillation showed antibacterial activity against C. michiganensis (MICs ranging from 0.125 to 1 mg/mL), namely: Salvia sclarea L. (Sas), Salvia rosmarinus Schleid (Sar), Sco, Hei, and Css. The 1H NMR fingerprinting of the bioactive matrices was acquired, detecting primary and secondary metabolites (rosmarinic acid, shikimic acid, sclareol, and hydroxycinnamic acids)
CARATTERIZAZIONE CHIMICA E ATTIVITA' BIOLOGICA DELL'OLIO ESSENZIALE DA CORTECCE DI CRYPTOCARYA MASSOIA (Oken) Kostern (LAURACEAE)
No full textL'olio essenziale (o.e.) da cortecce di C. massoia (Lauraceae), specie endemica dell'isola di Nuova Guinea, utilizzata dall'industria dei profumi e scarsamente investigata sotto il profilo fitochimico e funzionale, è stato caratterizzato mediante GC-FID e GC-MS e valutato per le capacità antiossidanti ed antimicrobiche. Dall'indagine chimica è emersa la prevalente ed insolita presenza di diversi lattoni (82%), alcuni dei quali inediti per la specie, tra cui: massoia lattone C8=3.39±0.08%, C10=56.06±0.42%, C12=16.51±0.11%, C14=0.56±0.01%). È stata inoltre verificata la presenza minoritaria di composti benzilici (15%) con prevalenza di benzil benzoato 12.73±0.10% e di benzoil salicilato 1.78±0.01%. Per quanto riguarda i saggi di bioattività, l'o.e. è stato dapprima sottoposto a saggi di valutazione dell'attività antiossidante mediante test spettrofotometrici del DPPH e ABTS che hanno evidenziato una modesta efficacia se confrontata con i dati espressi dall'o.e. di timo commerciale preso a riferimento. La valutazione dell'attività biologica dell'o.e. è stata estesa alla capacità antimicrobica (disk diffusion assay) impiegando 12 ceppi di microrganismi, tra batteri Gram+, Gram- e lieviti. I valori di MIC più interessanti si sono rivelati quelli in riferimento a Klebsiella oxytoca (9.8±1.1μg/μl); con Bacillus brevi e Pseudomonas aeruginosa, l’olio di massoia ha evidenziato MIC (18.6±1.4μg/μl) confrontabili con quelle espresse dal controllo positivo (o.e. di timo). Di particolare interesse è risultata l'efficacia verso Candida albicans (MIC=4.9±0.8μg/μl) con valori circa 4 volte inferiori rispetto al riferimento positivo (o.e. timo commerciale). Le valutazioni di bioattività sono state estese al metodo bioautografico con lastre (HP)TLC per valutare qualitativamente quali classi di metaboliti dell'o.e. di massoia fossero maggiormente responsabili dell'attività del fitocomplesso. I massoia lattoni corrispondenti alle bande risultate più attive sono stati successivamente isolati e sottoposti a caratterizzazione, tutt'ora in corso. Relativamente ad espressioni di sicurezza, sono state effettuate indagini di genotossicità (Ames test) che hanno escluso proprietà mutagene dell'olio essenziale. Da questa indagine preliminare, emerge il singolare profilo fitochimico di questo olio essenziale caratterizzato prevalentemente da composti lattonici, e da una bioattività interessante, degna di ulteriori approfondimenti rispetto ad un potenziale impiego salutistico
UN PROFILO CHIMICO E DI BIOATTIVITÀ DELL'OLIO ESSENZIALE DI CROTON LECHLERI MÜLL. ARG. (EUPHORBIACEAE): DALLA FORESTA AMAZZONICA ALLA FARMACIA?
No full textCortecce di C. lechleri, raccolte da piante adulte cresciute in tre differenti siti nella provincia Morona-Santiago (Ecuador) ai margini della foresta amazzonica sono state distillate in corrente di vapore [olio essenziale (o.e.)=0.61 ml/kg]. L'o.e. presentava una composizione (GC, GC-MS, NMR) di 74 costituenti, con una prevalenza di sesquiterpeni (sesquicineolo, 17,29%; α-calacorene, 11,29%; 1,10-di-epi-cubenolo, 4,75%; β-calacorene, 4,34%; epi-cedrolo, 4,09%). Il profilo di bioattività è stato determinato valutando attività antiossidante, antimicrobica, citotossicità, mutagenicità e mutageno protezione. DPPH assay e β-carotene bleaching test evidenziavano IC50 coerenti con una efficacia antiossidante significativamente superiore ai riferimenti. Il saggio TLC-DPPH-bioautographic assay ha poi evidenziato che 3 frazioni dell’olio caratterizzate da α- (24%), β- (8%) e δ-cadalene (15%) erano le principali responsabili dell'attività. L’attività antibatterica su TLC ha espresso MIC variabili tra 10 μg/spot (E. coli) e 100 μg/spot (P. aeruginosa) e un principale coinvolgimento dei calacoreni. Il saggio di Ames su ceppi di Salmonella typhimurium TA98 e TA100 con e senza attivazione metabolica (S9) ha dimostrato la non citotossicità e la non mutagenicità dell’o.e. (10-2 e 100 mg/piastra) e, per contro, una riduzione delle colonie revertenti sul ceppo TA98 del 30% (+S9) e del 33% (-S9) in presenza di 2-aminoanthracene e nitro fluorene (2 μg/piastra). Il test di mutageno-protezione è stato esteso a mutageni di interesse dietistico (ammine eterocicliche, HCAs) con quantità di o.e. comprese tra 10-2 e 1.0 mg/piastra, tenendo conto della massima dose inattiva (HUD: Highest Uneffective Dose). In presenza di S9, l'o.e. ha evidenziato riduzione dei revertenti prodotti dalla esposizione alle HCAs a 5•10-2 mg/piastra; alla stessa concentrazione, ma in assenza di S9, ha manifestato la stessa capacità verso 2-amino-3-methylimidazo[4,5-f’]quinoline (IQ) e 2-amino-3,4-dimethylimidazo[4,5-f’]quinoline (MeIQ) (10-7 mol/piastra); nessuna efficacia con 2-amino- 3,8-dimethylimidazo[4,5-f’]quinoxaline (MeIQx) e 2-amino-6-methyldipyrido[l,2-a:3',2'-d]imidazole (Glu-P-1). L'o.e. è stato poi saggiato su linee cellulari tumorali LoVo ed HepG2, evidenziando IC50 di 74.95±0.05 μg/ml ed 82.28±0.03 μg/ml rispettivamente, delineandone un possibile utilizzo come ingrediente in prodotti salutistici con efficacia preventiva rispetto all'azione cancerogenetica
“Aspetti preliminari di indagine fitochimica e biologica di un endemismo sardo di tradizione etnomedica: Ribes sandalioticum Arrigoni”
No full textRibes sandalioticum (Grossulariaceae) è un endemismo sardo con areale compreso tra il Monte Limbara, Punta Balestrieri, Cima Giugantinu, Marghine ed il Gennargentu. Dal momento che la pianta, pur caratterizzata da tradizione etnomedica, non è stata mai investigata con finalità salutistiche, si riportano gli esiti preliminari di 1) indagini fitochimiche - relativamente al contenuto in polifenoli, procianidine e flavonoidi, - e 2) di attività biologica (antiossidante ed antimicrobica) di tinture madri (TM) da foglie. Da piante spontanee di R. sandalioticum raccolte sul monte Limbara (Nuoro) (RS) si sono ottenute TM; tutti i risultati ottenuti sono stati confrontati con quanto riscontrato per TM di R. nigrum sardo (RNS) e commerciale (RNC). Analisi (HP)TLC qualitative hanno evidenziato in RS la presenza di kaempferolo-3-glucoside, iperoside, isoquercitrina ed acido clorogenico. Ulteriori indagini sono o in corso per identificare due composti con Rf 0.35 e 0.80 (molto probabilmente questultimo corrispondente a quercetina pentoso). RNS e RNC hanno mostrato il medesimo profilo (HP)TLC fatta eccezione per la presenza di acido clorogenico e per le due bande in corso di identificazione risultate tipiche di RS. RS ha mostrato un contenuto di polifenoli totali valutato per via spettrofotometrica corrispondente a 11.99±1.07 μg di acido gallico/μl TM); RNS, 13.23±0.95 μg di acido gallico/μl TM; RNC, 9.52±0.78 μg di acido gallico/μl TM. Per i flavonoidi totali, considerati come iperoside/μl TM, RS ha rivelato un contenuto più basso del 10.46% (4.45±0.30) rispetto a RNS (4.97±0.39), ma 54.83% più elevato rispetto a RNC (2.01±0.11). Le procianidine erano sempre più abbondanti in RS (2.18±0.18 μg cyanidin chloride/μl TM; RNS=2.03±0.27; RNC=0.37±0.04). La capacità antiossidante (IC50 μg/ml) è stata saggiata mediante saggi spettrofotometrici (DPPH, ABTS) ed HPTLC-bioautografica: RS ha rivelato sempre una efficacia intermedia tra RNS ed RNC. I flavonoidi sono risultati essere i maggiori responsabili dell'attività, che risultava curiosamente aumentata a distanza di 24hs. L'attività antimicrobica (batteri e lieviti; disk diffusion assay e (HP)TLC-bioautografica) ha evidenziato una scarsa attività degli estratti, principalmente determinata in RS da flavonoidi corrispondenti ad Rf 0.35 e 0.80. Queste prime indagini relative a R. sandalioticum sono il punto di partenza per qualificare ulteriormente la chemodiversità dell'endemismo ed una sua possibile proiezione salutistica
Antioxidant and antimicrobial extracts obtained from agricultural by-products: Strategies for a sustainable recovery and future perspectives
No full textDurum wheat and rice brans are by-products deriving from the milling industry and source of important phytochemicals, mostly phenolics in bound form. The objectives of this work were to evaluate the most effective method for the extraction of phenolic acids from these by-products with antioxidant and antimicrobial activity and to standardize the obtained extracts to encourage their commercialization in health field. Free phenolics were extracted with ultrasound-assisted extraction (UAE) and bound phenolics with alkaline hydrolysis (AH) and ultrasound-assisted alkaline hydrolysis (UAAH). Extracts were analyzed with HPTLC (high-performance thin-layer chromatography) and RPHPLC-DAD-ESIMS (reversed-phase high-performance liquid chromatography-diode array detector-electrospray ionization mass spectrometry); the content of trans-ferulic acid, p-coumaric acid, total phenolics were also quantified. The antioxidant activity was investigated using DPPH and ABTS methods. The antimicrobial activity was evaluated against Staphylococcus aureus and Staphylococcus epidermidis strains. Results obtained using UAAH showed the most interesting data, suggesting this method as the most effective to obtain active extracts from the by-products. Durum wheat, extracted with UAAH, exhibited the highest content of trans-ferulic acid (406.14 ± 0.65 μg FA/mg extract), total phenolics (610.58 ± 57.60 mg GAE/g dried extract) and good antioxidant and antimicrobial activities and it has been selected to formulate oil-in-water cosmetic products
CHEMICAL CHARACTERIZATION AND BIOACTIVITY OF AYURVEDIC CRUDE DRUGS AND RELATED PREPARATIONS: BOERHAAVIA DIFFUSA L., CONVOLVULUS PLURICAULIS CHOISY AND CURCULIGO ORCHIOIDES
No full textAyurveda, the traditional Indian medicine, is recognized by the European Union as non-conventional medicine and it includes more than 7000 plants used for therapeutic purposes in complex formulations poorly investigated under a chemical and biological point of view (Guerrini and Sacchetti, 2012). On these premises, preparations (decoction, DEC, and hydro-alcoholic extract, HE) of Boerhaavia diffusa L. (roots), Convolvulus pluricaulis Choisy (whole plant) and Curculigo orchioides Gaertn. (roots) were studied for the first time through a chemical and bioactivity approach. GC-FID, GC-MS, HPLC and HPTLC, and NMR strategies were employed to identify and quantify the main chemical compounds and to verify the repeatability of their fingerprinting. The study of biological activities was driven both by the ethnomedical traditional uses of the species in the Ayurvedic culture (Agrawal et al., 2011; Bhowmik et al., 2012; Chauhan et al., 2010) and by those aspects related to modern western phytotherapic culture: antioxidant activity; genotoxic and anti-genotoxic potential; and cytotoxicity against cancer and normal human cell lines. Ferulic acid and vanillin were identified and quantified in DEC and in HE of B. diffusa. However, HE showed the presence of other two characterising molecules: boeravinone B and eupalitin. β-sitosterol was identified and quantified in both preparations, but resulted more abundant in DEC. Ferulic acid showed antioxidant activity by ABTS assay higher than positive control. Preparations and pure compounds did not show anti-genotoxic activity towards two compounds with mutagenic properties. The study of cytotoxicity using DEC, HE and pure molecules against human cancer cell lines (A549, CaCo-2, MCF7, LoVo and HepG2), showed once more data far from those stated by the American National Cancer Institute (Suffness and Pezzuto, 1991). DEC of Convolvulus pluricaulis was characterised by the presence of phenolic acids (caftaric acid, caffeic acid, p-coumaric acid, iso-ferulic acid and tr-ferulic acid). Stigmasterol, β-sitosterol, lupeol and vanillin isomers and derivatives (2H4MB, 3H4MB and acetovanillone) were also detected in the same preparation. HE showed the presence of p-coumaric acid, vanillin, 2H4MB, acetovanillone, and vanillic acid, but the absence of phytosterols. The antioxidant activity evaluation indicated DEC as the preparation that exhibited always the best efficacy. HE showed instead an higher activity than DEC in the ABTS assay, no activity against DPPH radical and a lower capacity of blocking the radical propagation than DEC in the β-carotene bleaching test. Cytotoxic activity of the considered preparations against A549, CaCo-2, MCF7, LoVo and HepG2 cancer cell lines are not significant. The tests carried out with DEC and HE extracts against two leukaemia cell lines, drug-sensitive (CCRF-CEM) and multi-drug-resistant (CEM/ADR5000), showed, instead, interesting results: DEC CHCl3 extract and the HE soxhlet extract exhibit experimental data in line with the one stated by the American National Cancer Institute against the CCRF-CEM cell line, but respectively about 2 and 3 fold higher in the tests against CEM/ADR5000, showing cross-resistance phenomena. Curculigoside A and orcinol-β-D-glucoside were identified and quantified through HPLC methods in C. orchioides, and chosen as characterising compounds of preparations. β-sitosterol was also identified and quantified using GC-FID. The HE samples showed the highest antioxidant activity in every performed test. Regarding the anti-genotoxic activity, DEC resulted slightly more active than HE, but the highest activity was showed by orcinol-β-D-glucoside, even if it did not reach the 50% inhibition at the maximum concentration tested. The evaluation of the cytotoxic activity against human cancer cell lines exhibited an opposite trend, pointing out DEC as more active than HE for A549, CaCo-2, and HepG2. HE was instead more active against CCRF-CEM and CEM/ADR5000, but with IC50 data far from significant indication given by the American National Cancer Institute. Pure molecules did not exhibit any activity. However, further chemical and biological investigations will be carried out to shed an even more clear light on efficacy and safety of Ayurvedic preparations
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