DCM Extracts Research Articles

Exploring the Bioactive Potential of Taraxacum officinale F.H. Wigg Aerial Parts on MDA Breast Cancer Cells: Insights into Phytochemical Composition, Antioxidant Efficacy, and Gelatinase Inhibition within 3D Cellular Models

In this work, aerial parts of Taraxacum officinale F.H. Wigg. produced in Umbria, Italy, were chemically investigated by solid-phase microextraction/gas chromatography–mass spectrometry (SPME/GC-MS) to describe their volatile profile. The results obtained showed the preponderant presence of monoterpenes, with limonene and 1,8-cineole as the main components. Further analyses by GC/MS after derivatization reaction were performed to characterize the non-volatile fraction highlighting the presence of fatty acids and di- and triterpenic compounds. T. officinale methanol and dichloromethane extracts, first analyzed by HRGC/MS, were investigated to evaluate the antioxidant activity, cytotoxicity, and antiproliferative properties of MDA cells on the breast cancer cell line and MCF 10A normal epithelial cells as well as the antioxidant activity by colorimetric assays. The impact on matrix metalloproteinases MMP-9 and MMP-2 was also explored in 3D cell systems to investigate the extracts’ efficacy in reducing cell invasiveness. The extracts tested showed no cytotoxic activity with EC50 > 250 µg/mL on both cell lines. The DPPH assay revealed higher antioxidant activity in the MeOH extract compared with the DCM extract, while the FRAP assay showed a contrasting result, with the DCM extract exhibiting slightly greater antioxidant capacity. After treatment for 24 h with a non-cytotoxic concentration of 500 µg/mL of the tested extracts, gelatin zymography and Western blot analyses demonstrated that both MeOH and DCM extracts influenced the expression of MMP-9 and MMP-2 in MDA cells within the 3D cell model, leading to a significant decrease in the levels of these gelatinases, which are crucial markers of tumor invasiveness.

Preliminary Study to Assess the Antioxidant and Antibacterial Activity of Extracts from the Leaves of Morelia Senegalensis (A Rich)

frican populations rely heavily on traditional medicine, which uses plants to treat human and animal diseases. However, scientific validation of this empirical knowledge concerning the efficacy, toxicity and dosage of the proposed treatments is urgently needed. The aim of this study was to evaluate the antioxidant and antibacterial activity of Morelia senegalensis leaf extracts on the 2,2-diphenyl-1-picrylhydrawyl (DPPH) radical and the (2,2’-azino-bis-(3-ethylbenzothiazoline-6-sulfonic) acid) ABTS cation radical and on four reference bacterial strains (E. coli 25922, E. coli 35218, E. faecalis 29212 and S. aureus 29213) using protocols already described in the literature. The phytochemical screening test revealed the presence of flavonoids, alkaloids, tannins, saponins, reducing compounds and sterols in Morelia senegalensis leaves. All the extracts showed antioxidant activity to varying degrees. The most active ethyl acetate (AE) extract had half-maximum inhibition concentration (IC50 )of 0.33 and 0.62 mg/mL for the ABTS and DPPH tests respectively, followed by DCM and EB extracts with IC50 of 0.86 and 0.88 mg/mL for the ABTS test respectively, while the vitamin C used as a reference was more active with IC50 of 0.04 and 0.06 mg/mL. Antibacterial activity showed inhibition diameters ranging from 7 to 16 mm depending on the concentration and strain considered. The ethyl acetate fraction was the most active on S aureus 29213 with an inhibition diameter of 16 mm at 50 mg/mL. These interesting results were confirmed by the Minimal Inhibitory Concentration inhibitory (MIC) and Minimal Bacterial Concentration (MBC) studies, which showed that all the extracts had a bactericidal effect on all the studied strains. Morelia senegalensis plant has shown promising preliminary results in the treatment of bacterial infections. Further studies are needed to isolate and characterize the secondary metabolites contained in the leaves of this plant.

In-Vitro Cytotoxic and Anti-Inflammatory Potential of Asparagus Densiflorus Meyeri and its Phytochemical Investigation.

Genus Asparagus is well known for its pharmacological activities and ethnopharmacological applications. In folk medicine, it is used in the management of several diseases such as diabetes, inflammations, and rheumatism. This work aimed to investigate the potential of Asparagus densiflorus meyeri root & aerial parts extracts as cytotoxic and anti-inflammatory and the investigation of their chemical profile. GC analysis & Folin-Ciocalteu and gravimetric methods were used respectively to estimate the lipoidal, phenolic, and saponin contents. MTT assay was conducted using two cell lines (MCF-7 & HepG2) to investigate the cytotoxic and anti-inflammatory activity using TNF-α stimulated MCF-7 cells through monitoring the level of nitric oxide release and NF-κB gene expression. Preliminary phytochemical investigation indicated that both extracted parts are equally rich in saponins, flavonoids, carbohydrates and/or glycosides, and sterols and/or triterpenes. Palmitic acid and β sitosterol represented the major saturated fatty acids and sterol, respectively. A significant cytotoxic activity against MCF-7 cells was recorded for DCM extract (IC50 26.13 μg/ml). All tested extracts showed a significant decrease in NO release and NF-κB gene expression thus it possesses a potential anti-inflammatory activity. A. densiflorus meyeri is considered a good candidate as a food supplement for protection from malignancy.

Integrative approach to the biochemical, and toxicological fingerprinting of Polygonum glabrum.: A computational and experimental synergy for a medicinal food plant

In this work, the biological and chemical fingerprints of methanol and DCM extracts from an important Polygonum species (Polygonum glabrum) was investigated. The biological fingerprint was assessed for its antioxidant, enzyme inhibitory, and cytotoxic effects. For the chemical characterization, total bioactive components, and individual secondary metabolites were determined using photometric, HPLC-PDA polyphenolic quantification, and UHPLC-MS methods. The main identified compounds were belonging to flavonoid and phenolic classes of phytochemicals. Methanol extracts contained the highest total phenolic (54.66 mg GAE/g extract) and flavonoid (27.85 mg GAE/g extract) content. The results of antioxidant assays showed that methanol extract displayed higher antioxidant (for DPPH, ABTS, FRAP, CUPRAC) activity compared to the DCM extract (which was most active for metal chelation assay). For the enzyme inhibition activity, the DCM extract was found to be active against cholinesterases, while the methanol extract exhibited the higher inhibition potential for tyrosinase, amylase, and glucosidase enzymes. Generally, the methanol extract exhibited higher biological activities which might be correlated with higher levels of the bioactive components. Moreover, three flavonoids (citrusin B, robinetin 3-rutinoside, and demethyltexasin) were selected for molecular docking studies against the tested enzymes. Furthermore, the utilization of Swiss ADME, pkCSM, and DFT computational analysis has enhanced our comprehension of the pharmacokinetic characteristics and electronic factors of the identified phytochemicals, hence advancing the possibility for drug discovery. To conclude, the results suggest that the P. glabrum extracts could be further studied as a potential candidate for developing new phyto-pharmaceuticals and functional ingredients.

Limonoids from the fruits of Chisocheton erythrocarpus and their mosquito larvicidal activities

Phytochemical study of the fruits of Chisocheton erythrocarpus (Hiern) allowed the identification of eight undescribed limonoids, namely erythrocarpines O – V (1–6, 7a and 7b), along with seven known compounds. The structures of these compounds were elucidated based on spectroscopic and HRMS data, along with electronic circular dichroism to configure the absolute configuration. Erythrocarpines O and P are γ-hydroxybutenolide analogs of mexicanolide-type limonoids while erythrocarpine Q – V are phragmalin-type limonoids possessing a 1,29-oxymethylene bridge with either benzoyl or cinnamoyl moiety in their structures. Mosquito larvicidal activity revealed that crude DCM extract of C. erythrocarpus possessed a good larvicidal effect against Aedes aegypti larvae in 48 h (LC50 = 153.0 ppm). Subsequent larvicidal activity of isolated compounds indicated that erythrocarpine G (10) and 14-deoxyxyloccensin K (11) were responsible for the enhanced larvicidal effect of the extract, reporting LC50 values of 18.55 ppm and 41.16 ppm, respectively. Moreover, residual activity testing of the crude DCM extract revealed that the duration of its larvicidal effects is up to 14 days, where it maintained a 98 % larval mortality throughout the test period, under laboratory conditions.

Tropical mobola plum (Parinari Curatellifolia): a full characterization of wood and bark within the scope of biorefineries

Parinari curatellifolia is the main species used to produce charcoal in Angola. Its chemical, anatomical, and thermal properties were analyzed. The bark is dark grey, rough, and corky, and the wood is brown to yellow-red. Compared to wood, bark fibers presented lower length, lumen, and wall thickness. There is not much difference between height and cell numbers of rays. Sieve tube elements appear solitary or in small groups (2–3 cells), and vessels were of two diameter classes but diffuse-porous. Bark basic density was lower than wood (505 kg.m− 3vs. 580 kg.m− 3). The mean chemical composition from bark vs. wood of P. curatellifolia was ash (3.2% vs. 1.6%), total extractives (12.2% vs. 10.0%), total lignin (42.4% vs. 28.4%), and suberin 5.4%. Families identified by GC-MS from DCM extracts were predominated by fatty acids in wood and triterpenoid contents in bark. Bark and wood had higher antioxidant activity in FRAP and DPPH methods. The bark had a monomeric lignin composition richer in guaiacyl-units (25.9% vs. 22.5%) and lower syringyl-units (5.7% vs. 8.5%). Potassium was the most abundant mineral, while the least was cadmium found in wood and bark. Regarding thermal properties, bark presented higher moisture content (9.0% vs. 8.0%), ash (3.33% vs. 1.61%), total volatiles (27.5% vs. 20.7%), lower fixed carbon (69.1% vs. 77.7%) and higher heating value (20.9 MJ/kg vs. 19.1 MJ/kg). According to these characteristics, both biomasses are interesting for developing more value-added products (e.g., charcoal, bio-chemicals with phytochemistry and pharmacology activities) besides burning under the context of biorefineries.

Antinociceptive and anti-inflammatory activity of extracts and α-pyrones isolated from Cantinoa stricta.

This study evaluated the composition and the antinociceptive and anti-inflammatory activity of the crude extracts and two isolated compounds, anamarine (ANA) and 10-epi-olguine (eOL), obtained from the leaves of Cantinoa stricta (Lamiaceae). Crude ethanolic extract (EEt) and dichloromethane extract (DCM), selected based on NMR data, were submitted to pharmacological tests in male Swiss mice. The oral administration of EEt and DCM significantly reduced the second phase of formalin-induced nociception (60%), lipopolysaccharide (LPS)-induced mechanical hyperalgesia (90%), and carrageenan (Cg)-induced edema (25%). ANA and eOL, the major compounds in EEt and DCM extracts, administered orally or locally (in the paw), also reduced the LPS-induced mechanical hyperalgesia (Oral ID50 1.9 and 3.9mg/kg; Local ID50 93.4 and 677.3ng, respectively) without changing the thermal acute nociception or the motor performance of the animals. Local administration of ANA and eOL also reduced Cg-induced edema (40 and 23%, respectively). These isolated compounds did not change the mechanical hyperalgesia induced by tumor necrosis factor-α, interleukin-1β, prostaglandin E2, dibutyryl cyclic AMP, or forskolin but reversed the hyperalgesia induced by dopamine, epinephrine, and phorbol 12-myristate 13-acetate. The hyperalgesia induced by epinephrine was reversed in male but not in female mice, in which this response is not dependent on protein kinase C (PKC). These results suggest thatC. strictaextracts possess antinociceptive and anti-inflammatory activity which is related to the presence of ANA and eOL. Differently from the known analgesics, these substances seem to exert their action mainly interfering with the sympathetic component of pain, possibly with PKC.

Bacteriostatic and antidiabetic activities of various extracts from the mixture leaves and stems of Suaeda marimita

Humans were always in need of new medications to fight the many developing diseases that they face. In recent years, the race to develop new medicines has increased caused for new diseases to occur by bacteria and viruses developed causing accumulation, local damage, and inflammation or irritation. Suaeda maritima (S. maritima) is a plant that was used in the past to treat illness and the plant extracts showed several biological activities especially hepatoprotective, antimicrobial, and antidiabetic activities. The present goal of this work is to prepare plant extracts with varied polarities from the mixture of leaves and stems of S. maritima and examine their bacteriostatic and antidiabetic activities by in vitro methods. The crude extract was prepared from the mixture of leaves and stems powder samples by methanol using the maceration method for 36 h. The methanol was removed from the extract by the usual method and then fractionated methanol extract with different polarities solvents. The bacteriostatic and antidiabetic activities of plant extracts were determined by using disc diffusion and enzyme methods. The prepared varied polarities extract at four different concentrations (2000, 1000, 500, and 250 µg/mL) were used to evaluate their bacteriostatic activity against the Gram (+ and −) bacterial strains. Among the six plant extracts, ethyl acetate extract showed the highest bacterial activity, and the lowest activity was in DCM extract. However, at low concentrations, almost all plant extracts of the selected plant didn’t show any bacteriostatic activity. The antidiabetic activity of plant varied extracts was assessed by using an α-glucosidase bioassay and the highest IC50 was obtained in methanol extract and the lowest was in hexane extract from this bioassay. The other plant crude extracts also showed promising activity against the α-glucosidase bioassay. The plant extracts with significant activity from the selected plant could be used as natural medication to treat diabetes.

Green synthesis of Iron oxide and Iron dioxide nanoparticles using Euphorbia tirucalli: characterization and antiproliferative evaluation against three breast cancer cell lines

Researchers have become increasingly interested in nanoparticles made from plants because of their stability and large surface area. In the current study, iron oxide and iron dioxide nanoparticles were synthesized using aerial parts of the E. tirucalli as a reducing agent. The nanoparticles were analyzed using various techniques, including Ultraviolet-visible spectroscopy, Fourier Transform Infrared spectroscopy, X-ray diffractometer, X-ray photoelectron spectroscopy, X-ray energy dispersive spectroscopy, Scanning electron Microscopy, and Transmission Electron Microscopy. The nanoparticles were then investigated for their antiproliferative effect against MCF-7, SK-BR-3, MDA-MB231, and Vero cell lines. The results confirmed the formation of FeO and FeO2 nanoparticles by color change and a UV absorbance peak between 220–390 nm. EDS analysis showed traces of Fe and O, while TEM confirmed the nanoparticle size of 100 nm. FTIR showed a peak at 514 nm. The FeO-RT NPs demonstrated over 80% antiproliferative activity against the MCF-7 cell line at a concentration of 10 μg/mL. while doxorubicin, FeO-RT NPs, and DCM extract showed similar activity against the MDA-MB231 cell line at 10 and 1 g/mL concentrations. However, Vero and SK-BR-3 cell lines showed decreased antiproliferative activity. This study highlights the environmentally friendly use and safe application of iron oxide NPs in cancer therapy.

Green Extraction, Phytochemical Profiling, and Biological Evaluation of Dysphania ambrosioides: An In Silico and In Vitro Medicinal Investigation

ABSTRACT Parasitic and microbial infections present substantial health risks, requiring effective treatments amidst growing antibiotic resistance. This study delves into Dysphania ambrosioides medicinal properties, utilizing hydro distillation and ultrasonic methods for extraction, followed by GC-MS analysis. Assessments revealed potent anti-diabetic effects in the methanol extract, significant antioxidant activity in the DCM extract and oil, and resistance against Escherichia coli. This research underscores the potential of local flora for novel treatments, particularly in underdeveloped regions. It emphasizes the value of plant screening in bioprospecting efforts, suggesting further investigations into specific bioactive compounds for pharmaceutical applications.

Evaluation of the Antibacterial Activity and Toxicity Properties of Funtumia elastica (Preuss) Stapf. (TSN 30176), Used in Traditional Medicine in Nigeria

Background: The urgent need for new and novel antibacterial chemotherapy to combat the worrisome emergence of antimicrobial resistance necessitated the exploration of medicinal plants such as Funtumia elastica. This study was designed to evaluate the antibacterial activity, acute and sub-acute toxicity studies of Funtumia elastica which is used in the ethnomedical treatment of infections.
 Methods: The leaves and stem bark of F. elastica were collected, pulverized, extracted using soxhlet extractor and evaluated phytochemically. Antibacterial activities and Minimum Inhibitory Concentrations (MIC) of the crude extracts were investigated on clinical isolates using agar well diffusion. Bioactive fractions of the dichloromethane extract were obtained through column chromatography and thin layer chromatography. Acute and subacute toxicity studies were evaluated on the dichloromethane extract (DCM) using female Swiss albino mice.
 Results: The leaves contain tannins, flavonoids, alkaloids, steroids, saponins, and glycosides while the stem contains tannins and steroids. The hexane extracts lack activities while DCM and ethylacetate extracts of F. elastica were found to have some degree of activities on tested clinical isolates. Bioactivity guided fractionation of the DCM extract yielded only fraction 2 been active on the clinical isolates at 3.5625mg/mL. There were no signs of acute toxicity at the maximum dose of 5000mg/kg body weight. Biochemical parameters showed no significant changes in the liver enzymes. This infers that the extract might not have any negative impact on the liver with regards to metabolism.
 Conclusion: The moderate antibacterial activities of Funtumia elastica extracts justified its ethnomedicinal uses and potential to furnish new antimicrobials.

In vitro Evaluation of Sersia Lancea Root Extract for the treatment of Common Microbial Infections

Searsia lancea (SL) has been exploited by native healers in the Southern African region for the treatment of various bacterial and fungal infections. This study was aimed to analyze the antimicrobial activity and the minimum inhibitory concentration of SL root extract against Candida albicans, Candida glabrata, E.coli and Staph aureus. The maceration technique was used as the extraction method. The antifungal and antibacterial activity was determined by the agar well diffusion method. The agar dilution method was used for estimating the minimum inhibitory concentration (MIC). The biological investigations in this study clearly demonstrate the antibacterial and antifungal potential of SL aqueous and organic extract. The aqueous and organic Sersia Lancea root extract achieved zone of inhibition from 17.1-40.2mm against the tested organisms. The order of susceptibility of the pathogens to the tested extracts was found to be S.aureus>Candida Albicans>E.coli>Candida Glabrata. The results of the MIC experiment demonstrate that Candida Albicans and E.Coli were susceptible to the MIC of 3.12mg/mL for the SL distilled water root extract . The MIC of the aqueous extract against Candida glabrata and Staph Aureus were 6.25 and 12.5mg/mL respectively. All the microrgaisms were susceptible to MIC 6.25mg/mL for the DCM extract except for Candida Glabrata with MIC of 12.5mg/mL. The current work has not performed any isolation or structural elucidation studies for the potential compounds responsible for the antimicrobial activity. This is the first report to demonstrate the antibacterial and antifungal property of SL root extract. The results in this work provide scope for future studies to elucidate the structure of potential actives in SL root extract and to test their potential as possible antibacterial and antifungals.

A multidirectional phytochemical profiling, antimicrobial, antioxidant and toxicity studies of Neurada procumbens L.: A desert medicinal plant

ObjectivesNeurada procumbens L. (Neuradaceae) is a Cholistani desert plant traditionally employed in fever, inflammations, diabetes and hepatitis. The purpose of this study was to determine the chemical composition, anti-bacterial, antibiofilm and antioxidant activities of various extracts of this important medicinal plant; separately for its aerial and floral parts. MethodsThe phytochemical screening (by HPLC analysis), antioxidant (by DPPH assay), antibacterial (by disc diffusion test and MIC) and anti-biofilm potential against seven bacterial strains (E. coli, K. pneumoniae, S. aureus, S. aureus MDR, P. aeruginosa, P. aeruginosa MDR and P. vulgaris) were determined by aqueous, methanol, n-butanol, ethyl acetate, n-hexane and dichloromethane extracts of floral and aerial parts of N. procumbens. ResultsThe floral MetOH and DCM extracts were found to contain higher polyphenolic contents including 2,3-di methoxy benzoic acid (38.21 µg/mg), chlorogenic acid (26.59 µg/mg) and catechin (14.24 µg/mg) and exhibited a comparatively higher antioxidant (IC50 < 100 μg/ml) potential in DPPH assay. Moreover, these floral MetOH and DCM extracts were found to be most active (>13.5 mm zone of inhibition and MICs 62.5–125 µg/ml) against P. aeruginosa MDR and S. aureus in anti-bacterial activity. In an anti-biofilm assay, MetOH and DCM floral extracts showed a promising potential (>85 % biofilm inhibition) with IC50 < 150 μg/ml against P. aeruginosa MDR and S. aureus MDR better than moxifloxacin and was further confirmed by light and scanning electron microscopy. Moreover, the floral-MetOH extract of N. procumbens has been found to be safe up to 2 g/kg BW with its lethal dose (LD50) as 3872.98 mg/kg BW in rats. ConclusionHence, due to presence of essential medicinal compounds with low toxicity effects, the plant is recommended to be safely employed in various pharmaceutical preparations.

Antioxidant and anti-inflammatory potentials of aerial and floral parts of Neurada procumbens extracts: In vitro and in vivo studies

Neurada procumbens (Neuradaceae) is an importent plant of the Cholistan desert and is traditionally been used for the treatment and control of diabetes, fever, inflammations and jaundice. The aim of the current project is to investigate the bioactive compounds, free radical scavenging capacity and the anti-inflammatory potential of Neurada procumbens separately for its aerial and floral parts in six different extracts. The phytochemical profile (total bioactive contents, HPLC polyphenolic quantification), anti-oxidant (DPPH and FRAP assays), anti-inflammatory (HRBC stabilization) activities of the Aqu, MetOH, n-But, EtAc, n-Hex, and DCM extracts from the aerial and floral parts of Neurada procumbens were quantified. Based on the current results, the aerial and floral parts of N. procumbens extracts have found to contain a significant amount of active metabolites including polyphenolic compounds such as 2,3 di MeO benzoic acid, p-coumaric acid, chlorogenic acid, quercetin dihydrate and t-ferrulic acid. The total phenolic and total flavonoid contents of the plant were found to range from 28.13 to 78.9 GAE mg/g of plant and 17.23 to 68.23 RE mg/g of plant, respectively. DCM and n-But extracts of floral part exhibited comparatively higher antioxidant potential in DPPH (IC50 < 100 μg/ml) and FRAP (IC50 < 55 μg/ml) assays compared to aerial part. The dichloromethane floral extract demonstrated impressive anti-inflammatory activity in the hemolytic red blood cell lysis assay, with 83 % protection of HRBC lysis at an IC50 of 469.6 µg/ml (p < 0.01). In vivo, a 300 mg/kg body weight of DCM floral extract reduced carrageenan-induced paw oedema by 8.51 ± 0.35 mm to 7.65 ± 0.38 mm, a highly significant difference (p < 0.001).The toxicity studies revealed that the floral-DCM dose extract was found to be safe up to 2000 mg/kg BW, while its lethal dose (LD50) was found to be 4472.13 mg/kg BW in rats. Due to quite low toxicity effects, the floral part of the plant could be recommended as a safe pharmacological agent for various therapeutic applications.

Bioactivity Assays of Eryngium thyrsoideum; Focusing on Cytotoxic Effects, Antioxidant Activity, and Antimalarial Properties

Background: The genus Eryngium, Apiaceae is widely distributed in the world and used in traditional medicine for different therapeutic purposes. Eryngium thyrsoideum was investigated due to a lack of phytochemical studies on the probable bioactivities of its compounds. Methods: The aerial parts of the plant were extracted using n-hexane, dichloromethane, and methanol (MeOH) by the soxhlet method. The MeOH extract was exposed to C18 Sep-Pak fractionation by a step gradient of MeOH-H2 O. The essential oil was obtained by the Clevenger apparatus. Free-radical scavenging activity of the extracts and fractions was assessed using the DPPH-scavenging activity method. Total flavonoid content was determined by Aluminum chloride colorimetric and phenolic content was determined by using the Folin-Ciocalteu reagent method. α-Glucosidase inhibitory and antimalarial activity of extracts and essential oil and cytotoxic activity of essential oils was also established in this study. Results: The 20% solid phase extraction fraction demonstrated high antioxidant activity (0.13±0.01 mg/mL) and also indicated the most total flavonoid and total phenolic contents (474.20±23.11 and 27.90±0.55 mg/100 g) respectively, in comparison to other fractions. We observed a moderate β-Hematin Formation Assay inhibitory effect of the essential oil (10.37±0.02 mg/mL) and DCM extract (7.64±0.01 mg/mL). Low levels of α-glucosidase inhibition were observed in n-hexane extract (9.78±1.1%) and essential oil of aerial parts (2.7±1.1%). Cytotoxic activity for the essential oils is confirmed by representing respectively IC50 with 2.51 mcg/mL and 1.07 mcg/mL in 24 and 48 hours in MCF-7 cell lines. Conclusion: The presence of phenolic compounds and flavonoids in MeOH extract and fractions is effective on the antioxidant potency of E. thyrsoideum. Essential oil of this plant presented noticeable effects on human breast cancer cell lines.

Bioactive profiling and evaluation of anti-proliferative and anti-cancerous properties of Shivagutika, an Indian polyherbal formulation synchronizing in vitro and in silico approaches.

Shivagutika is a polyherbal formulation mentioned in Ayurveda, the oldest system of medicine. The aim of this study was to investigate the anti-breast cancer potential of DCM extract of Shivagutika using MCF-7, MDA-MB-231, and MDA-MB-468. Primarily, various extracts of Shivagutika were prepared and subjected to primary in vitro analysis-total protein, phenolic acid content, and flavonoid content. DCM extract among all the extracts showed the promising results hence, it was subjected to LC-MS/MS analysis to identify the phytochemicals. The same extract was subjected to anti-proliferation assay and anti-cancer assay. It inhibited all the 3cell lines and increased the activity of Caspase 3, pro-apoptotic protein. Further, to find the potent molecule(s) in silico analysis (molecular docking and molecular dynamics simulation studies) was performed. Sciadopitysin was identified as a potent molecule among all phytochemicals as it interacted with Caspase 3 with a binding energy of -7.2kcal/mol. MD simulation studies also revealed that Sciadopitysin was stable inside the binding pocket of Caspase 3 by interacting with the amino acids in the catalytic site thereby activating the Caspase 3 levels. By all the above results, Shivagutika could be used as a potent anti-breast cancer agent (specifically DCM extract of Shivagutika) which could decrease the cases of breast cancer in future.

Isolation of bioactive natural products from Rumex dentatus and their antimicrobial evaluation: A comparative study against various pathogenic bacteria

Rumex dentatus is traditionally used to treat different ailments including bacterial and fungal infections. The presented study disclosed isolation of five bioactive molecules from Rumex dentatus. All the isolates were evaluated for antimicrobial activities. In this protocol the comparative study has been made on various extracts and isolated compounds in order to identify the lead molecule. Thus the activity carried, resulted, compound X2 with strong anti-microbial potential and exhibiting IC50 value between 14–32 μM. While rest of isolates showed moderate antibacterial potential. Further, the investigation of antimicrobial activity on various plant extracts against six human pathogens (five bacteria and a fungal pathogen), most of the extracts showed strong to moderate antimicrobial activity with IC50 ranging from 24–35 μM. Out of all the extracts which were evaluated for antimicrobial activities, the hexane and methanol: DCM (1:1) extracts were found to have good antibacterial potential in microtiter plate assay. The IC50 value of compound X2 was found to be favorable and presented a strong antimicrobial potential. Thus the results inferred that the plant has strong antibacterial value and hence can be used in medication for the treatment of various bacterial infections.

Staphylococcus aureus antibiofilm agents from Combretum species (Combretaceae) by metabolomics profiling

About 80 % of all chronic bacterial infections are related to biofilms. Among several bacteria capable of developing biofilms, Staphylococcus aureus and Pseudomonas aeruginosa are recognized as two major opportunistic pathogens associated with biofilm infections, especially those related to medical devices. In light of the exciting progress of metabolomics within the field of natural products, and given the pressing need for new alternatives to control bacterial pathogens, this study applied metabolomic profiling and statistical analyses to identify S. aureus or P. aeruginosa biofilm inhibitors from three Brazilian Combretum species. The extracts were obtained from leaves and bark of C. leprosum, C. laxum, and C. lanceolatum, by solvent extraction with hexane (Hx), dichloromethane (Dcm), and hydromethanolic (Me70). Me70 extracts from leaves of all tested species were active against S. aureus biofilm formation (inhibition rate of 92 % for C. lanceolatum, 80 % for C. leprosum, and 65 % for C. laxum), but they did not inhibit bacterial growth. Other extracts from C. leprosum also presented similar results, decreasing S. aureus biofilm formation without affecting cell growth (inhibition of 90 % for bark Me70 extract, 72 % for bark Dcm extract, and 69 % for leaf Hx extract). Dcm extract from C. leprosum leaves decreased biofilm formation in 69 % while having antibacterial activity (85 % inhibition of bacterial growth). None of the extracts were active against P. aeruginosa. Metabolomic analysis by LC-MS followed by statistical evaluation clearly evidenced chemical differences associated with the activity level of the extracts. Univariate analysis by Pearson's r correlation suggested thirty-five metabolites with positive correlation with S. aureus antibiofilm activity, including alkaloids, tannins, phenolic acids, sugars, and glycosylated and non-glycosylated flavonoids. We obtained in vitro confirmation that ellagic acid is a key component for antibiofilm activity by Combretum extracts against S. aureus, showing circa 70% inhibition. It is likely that ellagic acid prevents bacterial-material surfaces interaction, since it led to increased hydrophobicity in S. aureus surface at the same concentrations that affected biofilm formation (up to 0.1563 µM). Importantly, ellagic acid, and the 4 most active Combretum crude extracts, are not toxic as determined using Galleria mellonella larvae model. The lower selective pressure toward bacterial resistance is an attractive feature of antibiofilm agents compared with antibiotics. Their identification will contribute to the development of novel anti-infective strategies, including less prone adherent surfaces, with a direct impact on the reduction of infections associated with medical devices.

Antitumoral Activity of Leptocarpha rivularis Flower Extracts against Gastric Cancer Cells.

Leptocarpha rivularis is a native South American plant used ancestrally by Mapuche people to treat gastrointestinal ailments. L. rivularis flower extracts are rich in molecules with therapeutic potential, including the sesquiterpene lactone leptocarpin, which displays cytotoxic effects against various cancer types in vitro. However, the combination of active molecules in these extracts could offer a hitherto unexplored potential for targeting cancer. In this study, we investigated the effect of L. rivularis flower extracts on the proliferation, survival, and spread parameters of gastric cancer cells in vitro. Gastric cancer (AGS and MKN-45) and normal immortalized (GES-1) cell lines were treated with different concentrations of L. rivularis flower extracts (DCM, Hex, EtOAc, and EtOH) and we determined the changes in proliferation (MTS assay, cell cycle analysis), cell viability/cytotoxicity (trypan blue exclusion assay, DEVDase activity, mitochondrial membrane potential MMP, and clonogenic ability), senescence (β-galactosidase activity) and spread potential (invasion and migration assays using the Boyden chamber approach) in all these cells. The results showed that the DCM, EtOAc, and Hex extracts display a selective antitumoral effect in gastric cancer cells by affecting all the cancer parameters tested. These findings reveal an attractive antitumoral potential of L. rivularis flower extracts by targeting several acquired capabilities of cancer cells.

Antifungal Activity of Certain Plants of Benin on Fusarium graminearum Cereals Pathogene

Phytopathogenic fungi decrease crop yield and quality and cause crop damage. The present work aims to study the effectiveness of certain extracts of medicinal and food plants (EtOH, DCM) that are present in the Republic of Benin on the mycelial growth of toxigenic molds responsible for the degradation of cereals.&#x0D; Ethanol, dichloromethane and aqueous extracts were studied in vitro for their antifungal activities against Fusarium graminearum using microdilution methods. The results show that the minimum inhibitory concentration (MIC) of Ocimum gratissimum essential oil is 2.5μl/ml. Regarding the essential oils of Cymbopogon citractus and Eucalyptus globulus they have a complete inhibition at 0.3μl / ml which is the most concentration tested. &#x0D; Ethanolic and dichloromethane extracts from different plants showed relative growth of about 77.54% for trunk bark and 41.7% for root bark of Anogeisus leiocarpus. The DCM extract of Momordica charantia showed an inhibition of approximately 59.675% at 800μg/ml. The essential oils Cymbopogon citractus, Eucalyptus globulus, Ocimum gratissimum and trunk bark of Anogeissus leiocarpus show promise as an antifungal agent.