Activity Of Different Compounds Research Articles

A Quick, High-Yield Biogenic Synthesis of Antibacterial AgNPs (Silver Nanoparticles) via Carica papaya Seeds

Carica papaya seeds were used in this research for the synthesis of AgNPs. The production of silver nanoparticles was characterized using UV–Vis spectroscopy, FTIR, XRD and SEM-EDX analysis. The antibacterial activity of the prepared AgNPs was evaluated by the Kirby–Bauer disc diffusion method with the antibacterial activity of different compounds against Bacillus aerogenes. UV–Vis spectral peaks are found at 8–18 nm. SEM and TEM analysis revealed several spherical structures between 10 nm and 50 nm. XRD analysis also confirmed its 50 nm size. Experimental data revealed that AgNPs inhibited bacterial growth. This study shows that papaya seed extract contributes to the bioreduction and stabilization of the synthesized silver nanoparticles.

Exploring the Antifungal Activity of Various Natural Extracts in a Sustainable Saccharomyces cerevisiae Model Using Cell Viability, Spot Assay, and Turbidometric Microbial Assays

Saccharomyces cerevisiae is a sustainable yeast with many applications in the food industry. Here, we study the use of a Saccharomyces cerevisiae model composed of three different industrial strains (a wine, a beer and a baker’s strain) to assess the antifungal activity of three organic plant-based extracts (Hypericum perforatum 10% w/w, Pistacia lentiscus var. Chia 20% w/w and Rosmarinus officinalis 6% w/w). Three different methods were employed (agar disc diffusion, spot assay, and growth curve analysis). Only the Rosmarinus officinalis extract (6% w/w) exhibited inhibitory activity against all the tested yeast strains in the agar disc diffusion method. In the spot assay, all extracts and their carrier oils (sunflower oil and caprylic triglyceride) exerted similar mild antifungal activity. In the growth curve analysis, all extracts significantly lowered the growth rate of the yeasts, but this was not observed for the carrier oils. The results highlighted that it is important to consider more than one method for testing the antimicrobial activity of different compounds. The three yeast strains exhibited differences in their susceptibility to pharmaceutical antifungals, and the beer and baker’s yeasts were resistant to itraconazole. Moreover, polyphenols were detected in all natural extracts which may be linked to their antifungal activity. Our results suggest that we might consider multiple use of these natural extracts in the food industry as food additives or even preservatives to delay food spoilage.

Identification of potential natural products derived from fungus growing termite, inhibiting Pseudomonas aeruginosa quorum sensing protein LasR using molecular docking and molecular dynamics simulation approach

Pseudomonas aeruginosa, the most common opportunistic pathogen, is becoming antibiotic-resistant worldwide. The fate of P. aeruginosa, a multidrug-resistant strain, can be determined by multidrug efflux pumps, enzyme synthesis, outer membrane protein depletion, and target alterations. Microbial niches have long used quorum sensing (QS) to synchronize virulence gene expression. Computational methods can aid in the development of novel P. aeruginosa drug-resistant treatments. The tripartite symbiosis in termites that grow fungus may help special microbes find new antimicrobial drugs. To find anti-quorum sensing natural products that could be used as alternative therapies, a library of 376 fungal-growing termite-associated natural products (NPs) was screened for their physicochemical properties, pharmacokinetics, and drug-likeness. Using GOLD, the top 74 NPs were docked to the QS transcriptional regulator LasR protein. The five lead NPs with the highest gold score and drug-like properties were chosen for a 200-ns molecular dynamics simulation to test the competitive activity of different compounds against negative catechin. Fridamycin and Daidzein had stable conformations, with mean RMSDs of 2.48 and 3.67 Å, respectively, which were similar to Catechin’s 3.22 Å. Fridamycin and Daidzein had absolute binding energies of −71.186 and −52.013 kcal/mol, respectively, which were higher than the control’s −42.75 kcal/mol. All the compounds within the active site of the LasR protein were kept intact by Trp54, Arg55, Asp67, and Ser123. These findings indicate that termite gut and fungus-associated NPs, specifically Fridamycin and Daidzein, are potent QS antagonists that can be used to treat P. aeruginosa’s multidrug resistance. Communicated by Ramaswamy H. Sarma

Antibacterial Activity of Combined Nanodiamonds and Snail Fractions with Biocompounds with MW below 10 kDa and above 30 kDa

The use of nanomaterials for enhancement of the antibacterial activity of different compounds is a new approach contributing to the efforts of overcoming the emerging antibiotics resistance. This study explores the combined antibacterial activity of nanodiamonds and snail peptides against Brevibacillus laterosporus BT271. Two peptide/protein fractions from Cornu aspersum mucus were used – with molecular weight (MW) below 10 kDa and with MW above 30 kDa. Four types of nanodiamonds (ND) were tested (positively charged, single digit and two types of detonation ND). Peptide fractions were characterized by using MALDI-TOF. The fraction with MW below 10 kDa consisted of many different peptides, while the fraction with proteins above 30 kDa showed proteins at m/z 26879.2 Da, 33903.11 Da, 43583.81 Da, 53986.81 Da, 79091.82 Da, 100650.42 Da, and 141 550.82 Da. When mixture peptides+ND was applied directly on the bacterial culture, the nanodiamonds showed enhanced antibacterial effect from 8% up to 42%. The combination of nanodiamonds and the mucus fraction with MW above 30 kDa had strongest bactericidal effect (1593.04 mm2/mgP*μL). The results demonstrated that ND have potential to enhance the antibacterial activity of the snail peptides but also highlighted that their effects should be carefully studied.

Microbiological Quality of Raw Donkey Milk from Serbia and Its Antibacterial Properties at Pre-Cooling Temperature.

The aim of this study was to examine the microbiological quality of raw donkey milk of an indigenous Serbian breed as well as the changes in the microbial populations during storage at 4 °C. In addition, antibacterial activity of donkey milk against E. coli, L. monocytogenes and S. aureus at 15 °C as well as the content of the two main antibacterial proteins lysozyme and lactoferrin were investigated. Microbiological examination of 137 individual milk samples collected over a period of 21 months showed good microbiological quality since foodborne pathogens such as Salmonella spp. and L. monocytogenes were not detected in any of the analyzed samples, while the number of E. coli, Enterobacteriaceae, total coliform bacteria, sulfite-reducing Clostridia and aerobic sporogenic bacteria was below the limit of quantification (<1 cfu mL-1). During the six-days storage at 4 °C, total bacterial counts and the counts of lactic acid bacteria remained at the initial level while pathogenic bacteria were not detected. The strongest antibacterial activity of the tested milk was observed against E. coli, while S. aureus was the least sensitive to milk antibacterial compounds. Although further research is needed to fully elucidate the antibacterial mechanism and synergistic activity of different compounds in donkey milk, the high content lysozyme (2.63 ± 0.03 g L-1) and lactoferrin (15.48 mg L-1) observed in tested milk could contribute to its strong antibacterial activity and extension of the storage period during which it can be safely consumed.

In silico Studies, Synthesis and Antibacterial Activity of Heterocyclic Compounds with Mannich Bases

Aim The present study aimed to identify the potent 123-triazole derivatives for synthesis and also assess their anti-bacterial activity.Methodology In silico design of novel analogues was carried out for ten derivatives using Auto Dock Vina and compared with standard drug Ciprofloxacin. Swiss ADME software was used to analyze lsquoLipinski Rule of Fiversquo and drug likeness properties. Three derivatives which obeyed rule of five having desired physicochemical properties and highest docking score were synthesized PDB code 2K35. The synthesis was carried out in two step process to determine their antibacterial activity. The synthesized compounds were structurally elucidated using Fourier-transform infrared spectroscopy FTIR Nuclear Magnetic Resonance 1H NMR and Mass spectroscopy .Results Antibacterial activity of different compounds was observed by disc diffusion method against two organisms E. coli and Streptococcus. Among the tested compounds 4A showed significant antibacterial activity. Compounds 6A and 8A also exhibited appreciable antibacterial activity against E. coli while compound 6A showed appreciable antibacterial activity against Streptococcus.Conclusion According to data obtained from the present study piperazine incorporated triazole derivatives were found to possess effective antibacterial activity. Further modifications of triazole based compounds at different positions to generate new molecules with potent anti-tumor activities will be described in future.

Assessing the In Vitro Activity of Selected Porphyrins in Human Colorectal Cancer Cells.

Standard in vitro analyses determining the activity of different compounds included in the chemotherapy of colon cancer are currently insufficient. New ideas, such as photodynamic therapy (PDT), may bring tangible benefits. The aim of this study was to show that the biological activity of selected free-base and manganese (III) metallated porphyrins differs in the limitation of colon cancer cell growth in vitro. White light irradiation was also hypothesized to initiate a photodynamic effect on tested porphyrins. Manganese porphyrin (>1 μM) significantly decreased the viability of the colon tumor and normal colon epithelial cells, both in light/lack of light conditions, while decreasing a free-base porphyrin after only 3 min of white light irradiation. Both porphyrins interacted with cytostatics in an antagonistic manner. The manganese porphyrin mainly induced apoptosis and necrosis in the tumor, and apoptosis in the normal cells, regardless of light exposure conditions. The free-base porphyrin conducted mainly apoptosis and autophagy. Normal and tumor cells released low levels of IL-1β and IL-10. Tumor cells released a low level of IL-6. Light conditions and porphyrins were influenced at the cytokine level. Tested manganese (III) metallated and free-base porphyrins differ in their activity against human colon cancer cells. The first showed no photodynamic, but a toxic activity, whereas the second expressed high photodynamic action. White light use may induce a photodynamic effect associated with porphyrins.

Crotoxin Conjugated to SBA-15 Nanostructured Mesoporous Silica Induces Long-Last Analgesic Effect in the Neuropathic Pain Model in Mice.

Neuropathic pain is a disease caused by structural and functional plasticity in central and peripheral sensory pathways that produce alterations in nociceptive processing. Currently, pharmacological treatment for this condition remains a challenge. Crotoxin (CTX), the main neurotoxin of Crotalus durissus terrificus rattlesnake venom, has well described prolonged anti-inflammatory and antinociceptive activities. In spite of its potential benefits, the toxicity of CTX remains a limiting factor for its use. SBA-15 is an inert nanostructured mesoporous silica that, when used as a vehicle, may reduce toxicity and potentiate the activity of different compounds. Based on this, we propose to conjugate crotoxin with SBA-15 (CTX:SBA-15) in order to investigate if when adsorbed to silica, CTX would have its toxicity reduced and its analgesic effect enhanced in neuropathic pain induced by the partial sciatic nerve ligation (PSNL) model. SBA-15 enabled an increase of 35% of CTX dosage. Treatment with CTX:SBA-15 induced a long-lasting reduction of mechanical hypernociception, without modifying the previously known pathways involved in antinociception. Moreover, CTX:SBA-15 reduced IL-6 and increased IL-10 levels in the spinal cord. Surprisingly, the antinociceptive effect of CTX:SBA-15 was also observed after oral administration. These data indicate the potential use of the CTX:SBA-15 complex for neuropathic pain control and corroborates the protective potential of SBA-15.

QSAR, molecular docking approach on the estrogenic activities of persistent organic pollutants using quantum chemical disruptors

Quantitative structure–activity relationship (QSAR), for predicting estrogenic activity of persistent organic pollutants (POPS) activity of different compounds used as dataset. Density functional theory using B3LYP/6-31G* quantum chemical calculation method was used to find the optimized geometry of the studied chemical disruptor compounds. Fourteen types of molecular descriptors were used to find out the relation between POPS activity and structural properties. Relevant molecular descriptors were selected by genetic function algorithms. The best model obtained was given a distinct validated, good and robust statistical parameters which include; Square correlation coefficient R2 value of (0.9289), Adjusted determination coefficient, $$R^{2}_{\text{adj}}$$ value of (0.9284), leave one out cross validation determination coefficient Q2 value of (0.9548) and external validation as predicted determination coefficient R value of R2 (0.819335). Molecular docking analysis find out, the best lead-compound with the higher negative value score of (− 11.8 kcal/mol) were formed hydrophobic interaction and H-bonding with amino acid residue between the disruptor compounds with their 1 × 7j as receptor. The result obtained from the study is expected to be significant and predict estrogenic activities disruptors of the POPS.

PREDICTION OF ANTI-PARKINSON POTENTIAL OF PHYTOCONSTITUENTS USING PREDICTION OF ACTIVITY SPECTRA OF SUBSTANCES SOFTWARE

Objective: Neurodegenerative disorders are group of diseased conditions in which there is loss of neuron cells occur. The main objective of this study to find/search out the phytochemical with the help of prediction of activity spectra of substances (PASSs), those show maximum activity over the selected targets of the Parkinson’s disease (PD).Methods: PASSs is a valuable software which is used in this study, to predict the anti-Parkinson activity of different compounds. Canonical simplified molecular-input line-entry system is used for the prediction of anti-Parkinson activity which is obtained from PubChem website. The predicted activity also compared with marketed compound like levodopa.Results: From the study, it was found that resveratrol was the only compound which has the activity on all the selected targets. On the other hand, stemazole and celastrol were found to have the least active compounds as both have the activity only on a single target.Conclusion: In this research work, we tried to compile the information regarding the PASS predicted anti-Parkinson activity of some important phytoconstituents. We found that resveratrol can be a target for further investigation in the development of drug therapy for PD.

LB976 Effects of TRP-regulin, pongamia oil and hesperidin methyl chalcone on anti-redness treatment

Rosacea is a chronic skin disorder characterized by inflammation and vascular abnormalities of the facial skin. Skin biopsies of rosacea are also characterized by an increase on the activation of the capsaicin receptor, the transient receptor potential vanilloid 1 (TRPV1). The aim of this study was to evaluate the activity of different compounds on the inflammatory and vascular responses implicated in rosacea. In one hand, the activity of Hesperidine Methyl Chalcone (HMC) compound was assessed to modulate vascular responses and IL-8 cytokine production after a Substance P (SP) stimulation on human skin explants. On the other hand, we evaluated the effect of TRP-regulin® (pentylene glycol 4-t-butylcyclohexanol) on TRPV1 activation, and the effect of the association of TRP-regulin® and pongamia oil on the inflammatory response of normal human epidermal keratinocytes (NHEK) in a rosacea environment. In the SP stimulated-skin model, HMC significantly decreased the proportion of dilated vessels, the total vessel area and the IL8 production. Moreover, we showed that TRP-regulin® significantly inhibited TRPV1 activation by capsaicin. Finally, we evaluated the effect of TRP-regulin®, pongamia oil and their association on the inflammatory response of NHEK in a rosacea environment. These experiments showed a synergy of these two compounds association on the inhibition of IL8 production. Altogether these results showed that HMC, TRP-regulin® and pongamia oil compounds have complementary and very interesting soothing and anti-redness properties and could be suitable for topical adjunctive treatment in rosacea.

In search of a small molecule agonist of the relaxin receptor RXFP1 for the treatment of liver fibrosis

The peptide hormone human relaxin-2 (H2-RLX) has emerged as a potential therapy for cardiovascular and fibrotic diseases, but its short in vivo half-life is an obstacle to long-term administration. The discovery of ML290 demonstrated that it is possible to identify small molecule agonists of the cognate G-protein coupled receptor for H2-RLX (relaxin family peptide receptor-1 (RXFP1)). In our efforts to generate a new medicine for liver fibrosis, we sought to identify improved small molecule functional mimetics of H2-RLX with selective, full agonist or positive allosteric modulator activity against RXFP1. First, we confirmed expression of RXFP1 in human diseased liver. We developed a robust cellular cAMP reporter assay of RXFP1 signaling in HEK293 cells transiently expressing RXFP1. A high-throughput screen did not identify further specific agonists or positive allosteric modulators of RXFP1, affirming the low druggability of this receptor. As an alternative approach, we generated novel ML290 analogues and tested their activity in the HEK293-RXFP1 cAMP assay and the human hepatic cell line LX-2. Differences in activity of compounds on cAMP activation compared with changes in expression of fibrotic markers indicate the need to better understand cell- and tissue-specific signaling mechanisms and their disease-relevant phenotypes in order to enable drug discovery.

Antiproliferative constituents from Aphananthe aspera leaves

Extensive screening for the antiproliferative activity of different compounds found in trees was performed by extracting the leaves of Aphananthe aspera (Thunb.) Planch and then using chromatographic separation to afford 2 new compounds, (2S,4R)-2-carboxy-4-(E)-p-caffeoyl-1-methyl-hydroxyproline (1) and 5-O-caffeoyl quinic acid-(7′R,8′S,7′′E)-3′,4′,3′′-dihydroxy-4′′,7′-epoxy-8′,5′′-neolign-7′-ene-9- carboxyl (2). In addition, 6 known compounds were discovered from the leaves of this plant. The structural determination of all compounds, including their absolute configurations, was established by UV, IR, HRESIMS, 1D and 2D NMR, and CD spectroscopy. The novel compound 1 showed strong antiproliferative activity against human breast adenocarcinoma cells MCF-7 and MDA-MB-231.

Investigation of antiaromatase activity using hepatic microsomes of Nile tilapia (Oreochromis niloticus).

Microsomal aromatase enzymes of humans and rats have been used in antiaromatase assays, but enzyme activity is species-specific. The current study extracted hepatic microsomes of Nile tilapia (Oreochromis niloticus) to investigate and compare the antiaromatase activity of chrysin, quercetin, and quercitrin. This activity was evaluated using a dibenzylfluorescein (DBF) assay. Results revealed that the age and body weight of Nile tilapia affected the yield of extracted microsomes. Extraction of hepatic microsomes of Nile tilapia was most effective when using a reaction medium with a pH of 8.0. A DBF assay using Nile tilapia microsomes revealed significant differences in levels of antiaromatase activity for chrysin, quercetin, and quercitrin. Chrysin was the most potent aromatase inhibitor, with an IC50 of 0.25 mg/mL. In addition, chrysin is an aromatase inhibitor that also inhibits the proliferation of cancer cells. Hepatic microsomes of Nile tilapia can be used to investigate and compare the antiaromatase activity of different compounds.

Anti-tumoral activity of native compound morelloflavone in glioma.

The aim of the study was to investigate the anti-tumoral activity of morelloflavone substances with different structures. We also studied the possible link between morelloflavone structure and its function. Various types of chromatographic techniques were used to isolate and screen morelloflavone substances from the extracts of gambogic tree trunk and the morelloflavone structures were identified by analytical techniques such as high resolution mass spectrometry and nuclear magnetism. Anti-tumoral activities of different compounds were investigated and the link between the antitumor activity and the structure of compound was exaimed. Our results showed that the isolated morelloflavone substances demonstrated a certain level of antitumor activity. The compound no. 1 had the strongest effect to inhibit glioma U87 and C6 cells followed by compound no. 2 while compound no. 5 was the weakest among them. We conducted a preliminary analysis on the structure-function relationship through the structure comparison and we concluded that the antitumor effects of morelloflavone substances with different structures were significantly different from each other. Thus, the glucose chain in C4 position of biflavone structure can enhance the antitumor activity of the compound in glioma cells. Additionally, the formation of intramolecular hydrogen bonds in biflavone compounds may also play a role in enhancing the antitumor activity and inhibition rate.

Larvicidal activity and structure activity relationship of cinnamoyl amides from Zanthoxylum armatum and their synthetic analogues against diamondback moth, Plutella xylostella.

Cinnamoyl amides isolated from Zanthoxylum armatum (Rutaceae) and their synthetic analogues were tested for their insecticidal activity against the second instar larvae of diamondback moth, Plutella xylostella (L.) (Lepidoptera: Yponomeutidae) to determine the promising structures with insecticidal activity. Most of the test compounds showed promising activity against larvae of P. xylostella. However, the activities of different compounds varied depending on the presence of different substituents at various positions of both the aromatic rings A and B. Among the tested compounds, 8, N-(3-bromo-4-methoxyphenethyl)cinnamamide showed best larvicidal activity with an LC50 = 62.13 mg/L followed by 6, N-(3׳-bromophenethyl)cinnamamide (LC50=128.49 mg/L) and 2 N-(4׳-methoxyphenylethyl)cinnamamide (LC50 = 225.65 mg/L).

Bioassay-Guided Isolation of Sesquiterpene Coumarins from Ferula narthex Bioss: A New Anticancer Agent.

The main objective of cancer management with chemotherapy (anticancer drugs) is to kill the neoplastic (cancerous) cell instead of a normal healthy cell. The bioassay-guided isolation of two new sesquiterpene coumarins (compounds 1 and 2) have been carried out from Ferula narthex collected from Chitral, locally known as “Raw.” Anticancer activity of crude and all fractions have been carried out to prevent carcinogenesis by using MTT assay. The n-hexane fraction showed good activity with an IC50 value of 5.434 ± 0.249 μg/mL, followed by crude MeFn extract 7.317 ± 0.535 μg/mL, and CHCl3 fraction 9.613 ± 0.548 μg/mL. Compounds 1 and 2 were isolated from chloroform fraction. Among tested pure compounds, compound 1 showed good anticancer activity with IC50 value of 14.074 ± 0.414 μg/mL. PASS (Prediction of Activity Spectra) analysis of the compound 1 was carried out, in order to predicts their binding probability with anti-cancer target. As a results the compound 1 showed binding probability with human histone acetyltransferase with Pa (probability to be active) value of 0.303. The compound 1 was docked against human histone acetyltransferase (anti-cancer drug target) by using molecular docking simulations. Molecular docking results showed that compound 1 accommodate well in the anti-cancer drug target. Moreover the activity support cancer chemo preventive activity of different compounds isolated from the genus Ferula, in accordance with the previously reported anticancer activities of the genus.

Study of the mechanisms of antioxidative action of different antioxidants

The reaction mechanisms by which antioxidants can exert their activity are: hydrogen atom transfer (HAT), proton coupled electron transfer (PCET), sequential proton loss electron transfer (SPLET), single electron transfer - proton transfer (SET-PT), radical adduct formation, and sequential proton loss hydrogen atom transfer. The antioxidative activity of different compounds (flavones, flavonols, and Schiff basis) was investigated by the trolox equivalent antioxidative capacity and electron paramagnetic resonance methods. The mechanisms of the antioxidative action (HAT, PCET, SPLET, and SET-PT) were investigated by using the thermodynamic parameters: bond dissociation enthalpy, ionization potential, proton dissociation enthalpy, proton affinity, and electron-transfer enthalpy. The influence of different radicals was investigated using appropriate isodesmic reactions. The mechanistic approach to the investigation of the influence of different radicals to the HAT mechanism, and the second step of the SET-PT mechanism) was applied. These investigations contribute to the elucidation and understanding of complex processes involved in the antioxidative action.

Method for Systematic Assessment of Chemical Changes in Molecular Scaffolds with Conserved Topology and Application to the Analysis of Scaffold-Activity Relationships.

Sets of scaffolds with conserved molecular topology are abundant among drugs and bioactive compounds. Core structure topology is one of the determinants of biological activity. Heteroatom replacements and/or bond order variation render topologically equivalent scaffolds chemically distinct and also contribute to differences in the biological activity of compounds containing these scaffolds. Relationships between core structure topology, chemical modifications, and observed activity profiles are difficult to analyze. A computational method is introduced to consistently assess chemical transformations that distinguish scaffolds with conserved topology. The methodology is applied to quantify chemical differences in conserved topological environments and systematically relate chemical changes in topologically equivalent scaffolds to associated activity profiles.

Antiproliferative activity of cardenolide glycosides from Asclepias subulata

Ethnopharmacological relevanceAsclepias subulata Decne. is a shrub occurring in Sonora–Arizona desert (Mexico–USA). The ethnic groups, Seris and Pimas, use this plant for the treatment of sore eyes, gastrointestinal disorders and cancer. Aim of the studyTo isolate the compounds responsible for antiproliferative activity of the methanol extract of A. subulata. Materials and methodsA bioguided fractionation of methanol extract of A. subulata was performed using MTT assay to measure the antiproliferative activity of different compounds on three human cancer cell lines (A549, LS 180 and PC-3), one murine cancer cell line (RAW 264.7) and one human normal cell line (ARPE-19). The methanol extract was partitioned with hexane, ethyl acetate and ethanol. The active fractions, ethanol and residual, were fractioned by silica-column chromatography and active sub-fractions were separated using HPLC. The chemical structures of isolated compounds were elucidated with different chemical and spectroscopic methods. ResultsA new cardenolide glycoside, 12, 16-dihydroxycalotropin, and three known, calotropin, corotoxigenin 3-O-glucopyranoside and desglucouzarin, were isolated of active sub-fractions. All isolated compounds showed a strong antiproliferative activity in human cancer cells. Calotropin was the more active with IC50 values of 0.0013, 0.06 and 0.41µM on A549, LS 180 and PC-3 cell lines, respectively; while 12, 16-dihydroxycalotropin reached values of 2.48, 5.62 and 11.70µM, on the same cells; corotoxigenin 3-O-glucopyranoside had IC50 of 2.64, 3.15 and 6.62µM and desglucouzarin showed values of 0.90, 6.57 and 6.62,µM. Doxorubicin, positive control, showed IC50 values of 1.78, 6.99 and 3.18µM, respectively. The isolated compounds had a weak effect on murine cancer cells and human normal cells, exhibiting selectivity to human cancer cells. ConclusionIn this study, we found that 12, 16-dihydroxicalotropin, calotropin, corotoxigenin 3-O-glucopyranoside and desglucouzarin are responsible of antiproliferative properties of A. subulata, and that these compounds are highly selective to human cancer cells. Further studies are needed in order to establish the action mechanisms of the isolated compounds.