Antimicrobial and Antibiofilm Potential of Flourensia retinophylla against Staphylococcus aureus.

Staphylococcus aureus is a Gram-positive bacteria with the greatest impact in the clinical area, due to the high rate of infections and deaths reaching every year. A previous scenario is associated with the bacteria's ability to develop resistance against conventional antibiotic therapies as well as biofilm formation. The above situation exhibits the necessity to reach new effective strategies against this pathogen. Flourensia retinophylla is a medicinal plant commonly used for bacterial infections treatments and has demonstrated antimicrobial effect, although its effect against S. aureus and bacterial biofilms has not been investigated. The purpose of this work was to analyze the antimicrobial and antibiofilm potential of F. retinophylla against S. aureus. The antimicrobial effect was determined using an ethanolic extract of F. retinophylla. The surface charge of the bacterial membrane, the K+ leakage and the effect on motility were determined. The ability to prevent and remove bacterial biofilms was analyzed in terms of bacterial biomass, metabolic activity and viability. The results showed that F. retinophylla presents inhibitory (MIC: 250 µg/mL) and bactericidal (MBC: 500 µg/mL) activity against S. aureus. The MIC extract increased the bacterial surface charge by 1.4 times and the K+ concentration in the extracellular medium by 60%. The MIC extract inhibited the motility process by 100%, 61% and 40% after 24, 48 and 72 h, respectively. The MIC extract prevented the formation of biofilms by more than 80% in terms of biomass production and metabolic activity. An extract at 10 × MIC reduced the metabolic activity by 82% and the viability by ≈50% in preformed biofilms. The results suggest that F. retinophylla affects S. areus membrane and the process of biofilm formation and removal. This effect could set a precedent to use this plant as alternative for antimicrobial and disinfectant therapies to control infections caused by this pathogen. In addition, this shrub could be considered for carrying out a purification process in order to identify the compounds responsible for the antimicrobial and antibiofilm effect.

Biological Activity of Ganoderma Species (Agaricomycetes) from Sonoran Desert, Mexico.

Ganoderma species have been used in folk medicine against different illnesses and are characterized by producing a diversity of bioactive metabolites (triterpenoids, polysaccharides, flavonoids, and phenols) with numerous medicinal effects (anti-proliferative, antioxidant, anti-inflammatory, and antibacterial). This work aims to evaluate ethanolic extracts of fruiting bodies of Ganoderma oerstedii, G. weberianum, and G. subincrustatum strains from the Sonoran Desert in the anti-proliferative activity by the MTT assay on cancer cell lines; anti-inflammatory effect by quantifying nitric oxide (NO) production; antioxidant activity by DPPH, ABTS, and FRAP assays; total phenolic and flavonoid content by Folin-Ciocalteu and AlCl3 method, respectively; antibacterial activity by the broth microdilution method against Escherichia coli and Staphylococcus aureus. Extracts showed anti-proliferative activity with IC50 < 100 µg/mL on the cancer cell lines MDA-MB-231, A549, and HeLa, except G. subincrustatum extract with an IC50 > 100 µg/mL; anti-proliferative activity was not selective, being affected non-cancerous cell line ARPE-19. Extracts showed significant inhibition of NO release in cells stimulated by LPS, up to 60% with G. subincrustatum and G. oerstedii, and 47% with G. weberianum. All tested assays showed moderate antioxidant potential; the most active was G. lucium (control strain) with IC50 of 69 and 30 µg/mL by DPPH and ABTS respectively; and 271 µg Trolox equivalents/g by FRAP. Total phenols and flavonoids ranged from 38 to 56 mg GAE/g and 0.53 to 0.93 mg QE/g, respectively. A significant correlation was found between the antioxidant activities revealed by DPPH, ABTS, and FRAP with total phenol and flavonoid contents. Antibacterial activity was weak against S. aureus (MIC50 > 10 mg/mL). These results demonstrate that tested Ganoderma mushrooms have medicinal potential such as anti-inflammatory and anti-proliferative.

Inhibition of the CYP Enzymatic System Responsible of Heterocyclic Amines Bioactivation by an Asclepias subulata Extract.

Asclepias subulata plant extract has previously demonstrated antiproliferative activity and antimutagenicity against heterocyclic aromatic amines (HAAs) commonly found in cooked meat. The objective of this work was to evaluate the in vitro ability of an ethanolic extract from the medicinal plant Asclepias subulata extract (ASE), non-heated and heated (180 °C), to inhibit the activity of CYP1A1 and CYP1A2, which are largely responsible for HAAs bioactivation. Ethoxyresorufin and methoxyresorufin O-dealkylation assays were performed in rat liver microsomes exposed to ASE (0.002-960 µg/mL). ASE exerted an inhibitory effect in a dose-dependent manner. The half inhibitory concentration (IC50) for unheated ASE was 353.6 µg/mL and 75.9 µg/mL for heated ASE in EROD assay. An IC40 value of 288.4 ± 5.8 µg/mL was calculated for non-heated ASE in MROD assay. However, after heat treatment, the IC50 value was 232.1 ± 7.4 µg/mL. Molecular docking of corotoxigenin-3-O-glucopyranoside, one of the main components of ASE, with CYP1A1/2 structure, was performed. Results show that the interaction of corotoxigenin-3-O-glucopyranoside with CYP1A1/2s' α-helices, which are related with the active site and the heme cofactor, may explain the plant extract's inhibitory properties. Results showed that ASE inhibits CYP1A enzymatic subfamily and may potentially act as a chemopreventive agent by inhibiting bioactivation of promutagenic dietary HAAs.

Association of Different ABO and Rh Blood Groups with the Erythroprotective Effect of Extracts from Navicula incerta and Their Anti-Inflammatory and Antiproliferative Properties.

Previous studies have reported that different blood groups are associated with the risk of chronic degenerative diseases that mainly involve inflammation and neoplastic processes. We investigate the relationship between blood groups and the erythroprotective effect of extracts from Navicula incerta against oxidative damage as a proposal to develop drugs designed for people with a specific blood type related to chronic pathology. The study was carried out through the elucidation of the erythroprotective potential, anti-inflammatory and antiproliferative activity of Navicula incerta. Research suggests that the presence or absence of certain blood groups increases or decreases the abilities of certain phytochemicals to inhibit oxidative stress, which is related to the systemic inflammatory response involved in the development of different types of cancer. The pigment-rich extracts from Navicula incerta inhibit ROO•- induced oxidative stress in human erythrocytes on the A RhD+ve antigen without compromising the structure of the cell membrane. This result is very important, since the A antigen is related to the susceptibility of contracting prostate cancer. Similarly, it was possible to inhibit the proliferation of cervical (HeLa) and prostate (PC-3) carcinoma. The combinatorial analysis of different biological activities can help design phytochemicals as new candidates for preventive drugs treating the chronic degenerative diseases associated with a specific blood group.

Dogs Detecting COVID-19 From Sweat and Saliva of Positive People: A Field Experience in Mexico.

Context: Molecular tests are useful in detecting COVID-19, but they are expensive in developing countries. COVID-19-sniffing dogs are an alternative due to their reported sensitivity (>80%) and specificity (>90%). However, most of the published evidence is experimental, and there is a need to determine the performance of the dogs in field conditions. Hence, we aimed to test the sensitivity and specificity of COVID-19-sniffing dogs in the field. Methods: We trained four dogs with sweat and three dogs with saliva of COVID-19-positive patients, respectively, for 4.5 months. The samples were obtained from a health center in Hermosillo, Sonora, with the restriction to spend 5 min per patient. We calculated sensitivity, specificity, and their 95% confidence intervals (CI). Results: Two sweat-sniffing dogs reached 76 and 80% sensitivity, with the 95% CI not overlapping the random value of 50%, and 75 and 88% specificity, with the 95% CI not overlapping the 50% value. The 95% CI of the sensitivity and specificity of the other two sweat dogs overlapped the 50% value. Two saliva-sniffing dogs had 70 and 78% sensitivity, and the 95% CI of their sensitivity and specificity did not overlap the 50% value. The 95% CI of the third dog's sensitivity and specificity overlapped the 50% value. Conclusion: Four of the six dogs were able to detect positive samples of patients with COVID-19, with sensitivity and specificity values significantly different from random in the field. We considered the performance of the dogs promising because it is reasonable to expect that with gauze exposed for a longer time to sweat and saliva of people with COVID-19, their detection capacity would improve. The target is to reach the sensitivity range requested by the World Health Organization for the performance of an antigen test (≥80% sensitivity, ≥97% specificity). If so, dogs could become important allies for the control of the COVID-19 pandemic, especially in developing countries.

Antiproliferative activity of standardized herbal phytopreparation from Asclepias subulata.

Background: Several studies have shown that active compounds of Asclepias subulata (cardenolides) have antiproliferative effect on human cancer cells. Cardenolides isolated from A. subulata can be used as active chemical markers to elaborate phytopharmaceutical preparations. To evaluate the antiproliferative effect of a standardized extract of the aerial parts, based on Asclepias subulata cardenolides. Methods: Four standardized extracts were prepared by HPLC-DAD depending on the concentration of calotropin and the antiproliferative activity was measured for the MTT assay, on the A549, MCF-7, HeLa, PC3 and ARPE cell lines. The concentrations of calotropin used for the standardization of the extracts were 10, 7.6, 5 and 1 mg/dL. Results: Standardization of the A. subulata extract based on calotropin at 7.6 mg/g dry weight was achieved and the antiproliferative activity was evaluated over A549, HeLa and MCF-7 cell lines, obtaining proliferation percentages of 3.8 to 13.4% . Conclusions: The standardized extracts of A. subulata at different concentrations of calotropin showed antiproliferative activity against all the cell lines evaluated. The greatest effect was observed against the HeLa cell line.

"Immunoinformatic Identification of T-Cell and B-Cell Epitopes From Giardia lamblia Immunogenic Proteins as Candidates to Develop Peptide-Based Vaccines Against Giardiasis".

Giardiasis is one of the most common gastrointestinal infections worldwide, mainly in developing countries. The etiological agent is the Giardia lamblia parasite. Giardiasis mainly affects children and immunocompromised people, causing symptoms such as diarrhea, dehydration, abdominal cramps, nausea, and malnutrition. In order to develop an effective vaccine against giardiasis, it is necessary to understand the host-Giardia interactions, the immunological mechanisms involved in protection against infection, and to characterize the parasite antigens that activate the host immune system. In this study, we identify and characterize potential T-cell and B-cell epitopes of Giardia immunogenic proteins by immunoinformatic approaches, and we discuss the potential role of those epitopes to stimulate the host´s immune system. We selected the main immunogenic and protective proteins of Giardia experimentally investigated. We predicted T-cell and B-cell epitopes using immunoinformatic tools (NetMHCII and BCPREDS). Variable surface proteins (VSPs), structural (giardins), metabolic, and cyst wall proteins were identified as the more relevant immunogens of G. lamblia. We described the protein sequences with the highest affinity to bind MHC class II molecules from mouse (I-Ak and I-Ad) and human (DRB1*03:01 and DRB1*13:01) alleles, as well as we selected promiscuous epitopes, which bind to the most common range of MHC class II molecules in human population. In addition, we identified the presence of conserved epitopes within the main protein families (giardins, VSP, CWP) of Giardia. To our knowledge, this is the first in silico study that analyze immunogenic proteins of G. lamblia by combining bioinformatics strategies to identify potential T-cell and B-cell epitopes, which can be potential candidates in the development of peptide-based vaccines. The bioinformatics analysis demonstrated in this study provides a deeper understanding of the Giardia immunogens that bind to critical molecules of the host immune system, such as MHC class II and antibodies, as well as strategies to rational design of peptide-based vaccine against giardiasis.

Therapeutic effects of chitosan in veterinary dermatology: A systematic review of the literature.

Chitosan is a natural polysaccharide with biocompatibility, biodegradability, nontoxicity, antimicrobial, and hemostatic properties. This biopolymer has been used in different pharmaceutical forms; therefore, it has an attractive potential for dermal applications in veterinary medicine. The aim of this review is to assess the healing potential of chitosan, based on its dermatological effects on animals, to enrich the therapeutic options of veterinary clinicians. A systematic review was conducted based on the Preferred Reporting Items for Systematic reviews and Meta-Analyses (PRISMA) strategy, retrieving 1,032 studies and selecting 39 after the inclusion and exclusion criteria were applied. The studies included reports with confirmed positive effects (n = 46/99, 46.5 %) (P < 0.05), with positive effects (n = 49.5/99, 49.5 %), and with no effect (n = 4/99, 4 %); none of the studies reported adverse effects. There is an association between frequency of application and a decrease in healing time (P = 0.038); applying chitosan "every 48-72 hours" was the most recommended frequency (n = 10/19, 52.9 %). Chitosan, when applied to skin lesions on animals, produces positive effects on healing, potentially becoming a safe biomaterial for skin treatments in veterinary practice. As an initial protocol, we suggest applying chitosan every 48-72 hours for at least 2 weeks (7 applications).

Optimization of growing conditions for pigments production from microalga Navicula incerta using response surface methodology and its antioxidant capacity.

Navicula incerta is a marine microalga distributed in Baja California, México, commonly used in aquaculture nutrition, and has been extended to human food, biomedical, and pharmaceutical industries due to its high biological activity. Therefore, the study aimed to optimize culture conditions to produce antioxidant pigments. A central composite experimental design and response surface methodology (RSM) was employed to analyze the best culture conditions. The medium (nitrogen-deficient concentrations), salinity (PSU = Practical Salinity Unity [g/kg]), age of culture (days), and solvent extraction (ethanol, methanol, and acetone) were the factors used for the experiment. Chlorophyll a (Chl a) and total carotenoids (T-Car), determined spectroscopically, were used as the response variables. The antioxidant capacity was evaluated by DPPH• and ABTS•+ radical inhibition, FRAP, and anti-hemolytic activity. According to the overlay plots, the optimum growth conditions for Chl a and T-Car production were the following conditions: medium = 0.44 mol·L-1 of NaNO3, salinity = 40 PSU, age of culture: 3.5 days, and solvent = methanol. The pigment extracts obtained in these optimized conditions had high antioxidant activity in ABTS•+ (86.2-92.1% of inhibition) and anti-hemolytic activity (81.8-96.7% of hemolysis inhibition). Low inhibition (33-35%) was observed in DPPH•. The highest value of FRAP (766.03 ± 16.62 µmol TE/g) was observed in the acetonic extract. The results demonstrated that RSM could obtain an extract with high antioxidant capacity with potential applications in the biomedical and pharmaceutical industry, which encourages the use of natural resources for chemoprevention of chronic-degenerative pathologies.

Antiproliferative activity of cardenolides on cell line A549: structure-activity relationship analysis.

Since the beginning, natural products have represented an important source of bioactive molecules for cancer treatment. Among them, cardenolides attract the attention of different research groups due to their cardiotonic and antitumor activity. The observed biological activity is closely related to their Na+/K+-ATPase inhibition potency. Currently, the discovery of new compounds against cancer is an urgent need in modern pharmaceutical research. Thus, the aim of this work is to determine the physicochemical properties and substituent effects that module the antiproliferative activity of cardenolides on the human lung cancer cell line A549. We build and curate a library with results obtained from literature; molecular descriptors were calculated in PaDEL software, and SAR/QSAR analysis was performed. The SAR results showed that cardenolides were sensitive to modifications in C and D steroidal ring and required substituent groups with the function of hydrogen bond acceptor at the C3 position. QSAR models to doubly linked-type cardenolides indicated that properties as lipoaffinity and atoms with the capacity to be hydrogen bond acceptors are involved in the increment of antiproliferative activity on A549 cell line. In contrast, the presence and position of very electro-negative atoms on the molecule decreased the antiproliferative effect on A549 cells. These results suggest that the antiproliferative capacity of cardenolides on the cell line A549 is strongly related to substituent groups on the C3 position, which must not be carbohydrate. Additionally, the steroidal rings C and D must remain without modifications.

Quantitative analysis of cucurbitane-type triterpenes in Ibervillea sonorae extracts: Relationship study with their antiproliferative activity.

Ibervillea sonorae (Cucurbitaceae) is a Mexican plant commonly used by local population for its hypoglycaemic activity. Root extracts showed also other different biological activities, including antimicrobial, antifungal, antioxidant and anti-inflammatory activity. Main components of this plant are cucurbitacins, steroid-like triterpenes that possess, among others, antiproliferative activity. In previous studies, kinoin A and cucurbitacin IIb extracted from I. sonorae showed antiproliferative and apoptotic effects against different cancer cell lines. Based on all the above, a RP-HPLC method was developed and validated for the quantitative analysis of these two compounds in I. sonorae root extracts obtained with different extraction conditions. In the present study, the quantitative analysis of kinoin B diglycoside in all the extracts was performed as well. As a result, no direct correlation was found between the antiproliferative activity (IC50) against human cervical cancer cell line (HeLa) and the composition of the above three compounds. Only a slight statically significant negative correlation was observed between IC50s and the content of kinoin A (r = 0.29, p = 0.12), meaning that, at least in part, this is the main compound among the three, contributing to the antiproliferative activity on the real samples. Accordingly, a synergistic effect by the phytocomplex components can account for the observed antiproliferative activity of the methanolic extracts towards HeLa cells.

Cucurbitacin IIb, a steroidal triterpene from Ibervillea sonorae induces antiproliferative and apoptotic effects on cervical and lung cancer cells.

Chemical studies on Ibervillea sonorae (S. Watson) Greene root led to isolation and chemical characterization of diverse cucurbitacin triterpenoid compounds such as kinoin A, B, C, and their glucosides. In previous studies, we demonstrated that kinoin A inhibits the cell proliferation on diverse cell line and induce apoptosis in HeLa cells. Therefore, the study of the isolated compounds from the extracts continued to be necessary. The objective of the present work was to isolate and chemically characterize the active compounds of the methanolic extract of the roots of I. sonorae and to evaluate their antiproliferative activity and induction of apoptosis. By chromatographic column separation and using NMR spectroscopy experiments, cucurbitacin IIb (CIIb), known as 23,24-dihydrocucurbitacin F or hemslecin B, was isolated and identified for the first time as a chemical constituent of the crude methanolic extract of this plant. The antiproliferative activity of CIIb was evaluated by MTT assay, and the apoptosis induction capacity was monitored by annexin V-FITC/propidium iodide using flow cytometry. CIIb showed a pronounced effect on the proliferation of HeLa and A549 tumor cells, with IC50 of 7.3 and 7.8 µM, respectively, but was less effective against L929 non-cancerous murine cell line. Apoptosis induction capacity of CIIb on HeLa and A549 was monitored by annexin V-FITC/propidium iodide using flow cytometry. Exposure of HeLa and A549 with CIIb (8 µM) for 24 h increased 56.9 and 52.3% respectively of the total apoptosis compared to the negative control (p < 0.005). CIIb, isolated for the first time from I. sonorae, showed antiproliferative activity against HeLa and A549 cell lines by inducing cell death by apoptosis.

Plant origin authentication of Sonoran Desert propolis: an antiproliferative propolis from a semi-arid region.

The main chemical composition of Sonoran propolis (SP), as well as its antiproliferative activity on cancer cells through apoptosis induction, has been reported. The chemical constitution of SP remained qualitatively similar throughout the year, whereas the antiproliferative effect on cancer cells exhibited significant differences amongst seasonal samples. The main goal of this study was to provide phytochemical and pharmacological evidence for the botanical source of SP and its antiproliferative constituents. A chemical comparative analysis of SP and plant resins of species found in the surrounding areas of the beehives was carried out by HPLC-UV-DAD, as well as by 1H NMR experiments. The antiproliferative activity on cancerous (M12.C3.F6, HeLa, A549, PC-3) and normal cell lines (L-929; ARPE-19) was assessed through MTT assays. Here, the main polyphenolic profile of SP resulted to be qualitatively similar to Populus fremontii resins (PFR). However, the antiproliferative activity of PFR on cancer cells did not consistently match that exhibited by SP throughout the year. Additionally, SP induced morphological modifications on treated cells characterised by elongation, similar to those induced by colchicine, and different to those observed with PFR treatment. These results suggest that P. fremontii is the main botanical source of SP along the year. Nevertheless, the antiproliferative constituents of SP that induce that characteristic morphological elongation on treated cells are not obtained from PFR. Moreover, the presence of kaempferol-3-methyl-ether in SP could point Ambrosia ambrosioides as a secondary plant source. In conclusion, SP is a bioactive poplar-type propolis from semi-arid zones, in which chemical compounds derived from other semi-arid plant sources than poplar contribute to its antiproliferative activity.

Effect of Extrusion Conditions and the Optimization of Phenolic Compound Content and Antioxidant Activity of Wheat Bran Using Response Surface Methodology.

The extrusion process (EP) consists of heat and mechanical treatments under different conditions of moisture, shear, and pressure and rapidly causes structural alterations and changes in the functional properties of the extruded material. The aim of this study was to evaluate the effect of extrusion conditions and optimize the wheat bran extrusion conditions to achieve the greatest content of phenolic compounds and antioxidant activity using response surface methodology. The EP factors evaluated were feed moisture (FM) (25-33.54%) and final extrusion temperature (T) (140-180 °C). The properties evaluated in the extruded material were bound total phenol content (BTPC), total phenolic compounds and antioxidant activity (AOX). Analysis of variance (ANOVA) and response surface methodology were used in the evaluation. The determination coefficients, (FM)2 and (T)2, very significantly affected the BTPC and bound 2,2-diphenyl-1-picrylhydrazyl content (BDPPHC). The optimization was performed by overlaying two contour plots to predict the best combination regions. The optimized extrusion conditions were the following: FM = 30% and T = 140 °C, which provided BTPC = 3547.01 µgGAE/g (predicted: 3589.3 µgGAE/g) and BDPPHC = 9.5 µmolTE/g (predicted: 10.4 µmolTE/g); and FM = 30% and T = 180 °C, which provided BTPC = 3342.3 µgGAE/g (predicted: 3727.7 µgGAE/g) and BDPPHC = 9.5 µmolTE/g (predicted: 9.3 µmolTE/g). The EP increased the phenolic compounds and AOX, and enhancement of these properties in wheat bran products could make them functional foods.

Antiproliferative and Apoptotic Activities of the Medicinal Plant Ziziphus obtusifolia.

BACKGROUND: Ziziphus obtusifolia is a spiny shrub found in Northwest Mexico desert, with traditional medicinal use to treat several diseases including cancer. OBJECTIVE: The aims of the present study were to evaluate the antiproliferative and apoptotic activities of the aerial parts of this plant. MATERIALS AND METHODS: The methanol extract and its fractions were prepared using several solvents. The antiproliferative activity was evaluated by the (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium) (MTT) assay on HeLa, A549, RAW 264.7, M12.C3.F6, and L-929 cell lines, and the apoptotic activity using Annexin V and (5,50,6,60-tetra-chloro-1,10,3,30-tetra-ethylbenzimidazol-carbocyanine iodide) staining. The most active fraction was further separated by column chromatography. RESULTS: The most active fraction was hexane with an IC50 of 90.4 µg/mL against RAW 264.7, 94 µg/mL against M12.C3.F6, 165.5 µg/mL against HeLa and 187.7 µg/mL against A549 cell lines. In apoptotic activity assays the methanol extract and its n-hexane fraction were found to induce mitochondrial depolarization in HeLa cells (83 and 87% respectively), and both induced the externalization of the phosphatidylserine increasing the percentage of cells in early apoptosis from 1.4% in untreated control cells, to 1.9% and 3.5% for methanol extract and n-hexane fraction-treated cells, respectively, statistically different for the total percentage of apoptotic cells (P < 0.05). CONCLUSIONS: These results show that Z. obtusifolia has antiproliferative and apoptotic activities in vitro and confirms its use in traditional medicine. SUMMARY: The methanol extract and its fractions using several solvents were evaluated in the antiproliferative activity by the MTT assay on HeLa, A549, RAW 264.7, M12.C3.F6, and L-929 cell lines, and the apoptotic activity using Annexin V and (5,50,6,60-tetra-chloro-1,10,3,30-tetra-ethylbenzimidazol-carbocyanine iodide) staining. The most active fraction against cell lines was hexane. In apoptotic activity assays, the methanol extract and its n-hexane fraction were found to induce mitochondrial depolarization. This results we showed that Ziziphus obtusifolia has antiproliferative and apoptotic activities in vitro.Abbreviations Used: DMEM: Dulbecco's modified eagle's medium, DMSO: Dimethyl sulfoxide, MTT: (3-4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium), JC-1: (5,50,6,60-tetra-chloro-1,10,3,30-tetra-ethylbenzimidazol-carbocyanine iodide), FBS: Fetal bovine serum, CAPE: Caffeic acid phenethyl ester, PBS: Phosphate-buffered saline.

Antiproliferative activity of spinasterol isolated of Stegnosperma halimifolium (Benth, 1844).

Cancer is the major cause of death in the world, representing a significant public health problem. Plants have been shown as a great source of secondary metabolites with anticancer activity. The aim of this work was evaluated the antiproliferative activity of the methanolic extracts, chemical fractions and the compound spinasterol isolated of medicinal plant Stegnosperma halimifolium. The methanolic extracts of stem, leaf and stem/leaf was obtained by maceration. The methanolic extract of stem was purified by successive extractions with solvents as n-hexane, ethyl acetate and ethanol. The n-hexane fraction was separated by column chromatographic and monitored by thin layer chromatographic. The compound spinasterol was characterized by 1H NMR, 13C NMR and Mass Spectrometry. Methanolic extracts, chemical, chromatographic fractions and spinasterol was evaluated against RAW 264.7, M12.C3.F6, PC-3, LS-180, A549 and HeLa cancer cell lines by the standardized method MTT for determinate the antiproliferative activity. Methanolic extract of stem shown the better antiproliferative activity against the murine macrophage cancer cell line RAW 264.7. n-Hexane chemical fraction shown antiproliferative activity against human alveolar cancer cell line A549 and RAW 264.7. Was isolated and characterized a compound by NMR 1H and 13C, revealing the presence of sterol spinasterol. Spinasterol shown to have antiproliferative activity against cervical cancer cell line HeLa and RAW 264.7, indicating that spinasterol can be a responsible compound of antiproliferative activity found in the methanolic extract of Stegnosperma halimifolium.

Antimycobacterial activity of medicinal plants used by the Mayo people of Sonora, Mexico.

ETHNOPHARMACOLOGICAL RELEVANCE: Tuberculosis (TB) is an infectious disease mainly caused by Mycobacterium tuberculosis (Mtb), which generates 9 million new cases worldwide each year. The Mayo ethnicity of southern Sonora, Mexico is more than 2000 years old, and the Mayos possess extensive knowledge of traditional medicine. AIMS OF THE STUDY: To evaluate the antimycobacterial activity levels of extracts of medicinal plants used by the Mayos against Mtb and Mycobacterium smegmatis (Msm) in the treatment of TB, respiratory diseases and related symptoms. MATERIALS AND METHODS: A total of 34 plant species were collected, and 191 extracts were created with n-hexane, dichloromethane, ethyl acetate (EtOAc), methanol and water. Their minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were determined against Mtb H37Rv using the microplate alamar blue assay (MABA) and against Msm using the resazurin microplate assay (REMA) at 6 and 2 days of exposure, respectively, and at concentrations of 250-1.9µg/mL (n-hexane extracts) and 1000-7.81µg/mL (extracts obtained with dichloromethane, EtOAc, methanol and water). RESULTS: Rhynchosia precatoria (Willd.) DC. (n-hexane root extract), Euphorbia albomarginata Torr. and A. Gray. (EtOAc shoot extract) and Helianthus annuus L. (n-hexane stem extract) were the most active plants against Mtb H37Rv, with MICs of 15.6, 250, 250µg/mL and MBCs of 31.25, 250, 250µg/mL, respectively. R. precatoria (root) was the only active plant against Msm, with MIC and MBC values of ≥250µg/mL. None of the aqueous extracts were active. CONCLUSIONS: This study validates the medicinal use of certain plants used by the Mayo people in the treatment of TB and related symptoms. R. precatoria, E. albomarginata and H. annuus are promising plant sources of active compounds that act against Mtb H37Rv. To our knowledge, this is the first time that their antimycobacterial activity has been reported. Crude extracts obtained with n-hexane, EtOAc and dichloromethane were the most active against Mtb H37Rv.

Diterpenoids and Triterpenoids from the Resin of Bursera microphylla and Their Cytotoxic Activity.

A chemical study of the nonpolar fraction of a methanol-soluble extract of Bursera microphylla resin yielded a variety of di- and triterpenoids. In total, 15 compounds were isolated, of which three are new, namely, malabaricatrienone (1), malabaricatrienol (2), and microphyllanin (3). The antiproliferative activity of the major compounds was evaluated in different murine cancer cell lines (M12.C3.F6 and RAW264.7) and human cancer cells (A549, HeLa, and PC-3). The new compounds (1-3) did not show significant antiproliferative activity. The known compounds ariensin (4), burseran (5), and dihydroclusin diacetate (6) were effective against the RAW264.7 cell line, with IC50 values in the micromolar range.

In vitro anti-proliferative activity of Argemone gracilenta and identification of some active components.

BACKGROUND: Cancer is one of the leading causes of death worldwide. Natural products have been regarded as important sources of potential chemotherapeutic agents. In this study, we evaluated the anti-proliferative activity of Argemone gracilenta's methanol extract and its fractions. We identified those compounds of the most active fractions that displayed anti-proliferative activity. METHODS: The anti-proliferative activity on different cancerous cell lines (M12.C3F6, RAW 264.7, HeLa) was evaluated in vitro using the MTT colorimetric method. Identification of the active compounds present in the fractions with the highest activity was achieved by nuclear magnetic resonance (NMR) and gas chromatography-mass spectrometry (GC-MS) analyses. RESULTS: Both argemonine and berberine alkaloids, isolated from the ethyl acetate fraction, displayed high anti-proliferative activity with IC50 values of 2.8, 2.5, 12.1, and 2.7, 2.4, 79.5 µg/mL on M12.C3F6, RAW 264.7, and HeLa cancerous cell lines, respectively. No activity was shown on the normal L-929 cell line. From the hexane fraction, a mixture of fatty acids and fatty acid esters of 16 or more carbon atoms with anti-proliferative activity was identified, showing a range of IC50 values of 16.8-24.9, 34.1-35.4, and 67.6-91.8 µg/mL on M12.C3F6, RAW 264.7, and HeLa cancerous cell lines, respectively. On the normal L-929 cell line, this mixture showed a range of IC50 values of 85.1 to 100 µg/mL. CONCLUSION: This is the first study that relates argemonine, berberine, and a mixture of fatty acids and fatty acid esters with the anti-proliferative activity displayed by Argemone gracilenta.

In vitro anti-mycobacterial activity of nine medicinal plants used by ethnic groups in Sonora, Mexico.

BACKGROUND: Sonoran ethnic groups (Yaquis, Mayos, Seris, Guarijíos, Pimas, Kikapúes and Pápagos) use mainly herbal based preparations as their first line of medicinal treatment. Among the plants used are those with anti-tuberculosis properties; however, no formal research is available. METHODS: Organic extracts were obtained from nine medicinal plants traditionally used by Sonoran ethnic groups to treat different kinds of diseases; three of them are mainly used to treat tuberculosis. All of the extracts were tested against Mycobacterium tuberculosis H37Rv using the Alamar Blue redox bioassay. RESULTS: Methanolic extracts from Ambrosia confertiflora, Ambrosia ambrosioides and Guaiacum coulteri showed minimal inhibitory concentration (MIC) values of 200, 790 and 1000 µg/mL, respectively, whereas no effect was observed with the rest of the methanolic extracts at the concentrations tested. Chloroform, dichloromethane, and ethyl acetate extracts from Ambrosia confertiflora showed a MIC of 90, 120 and 160 µg/mL, respectively. CONCLUSIONS: A. confertiflora and A. ambrosioides showed the best anti-mycobacterial activity in vitro. The activity of Guaiacum coulteri is consistent with the traditional use by Sonoran ethnic groups as anti-tuberculosis agent.For these reasons, it is important to investigate a broader spectrum of medicinal plants in order to find compounds active against Mycobacterium tuberculosis.