In vitro Biomedical Application of Endophytic Aspergillus melleus Isolated from Leaves of Premna serratifolia L.

Some microorganisms known as endophytes live in symbiotic relationships in the living tissues of plants without posing a health risk. As a result, they synthesize many metabolites which are helpful for the plants in many ways. So, these metabolites are known to exhibit many biological properties like antioxidant, antidiabetic anti-inflammatory, etc. Currently, many drugs are used to control inflammatory diseases like arthritis and, irritable bowel disease; however, they pose a lot of side effects. The present study was taken up to explore the anti-inflammatory properties along with the phytochemicals present, its quantification, and other in vitro biological activities of the less reported Aspergillus melleus, an endophytic fungus, isolated from Premna serratifolia L., a medicinal plant. The results of the investigation demonstrated the presence of alkaloids, phenols, terpenoids, flavonoids, tannins, cardiac glycosides and amino acids in the methanolic extract of endophytic fungus. It yielded 25.28 µg GAE/g and 19.465 µg GAE/g of total phenolic and flavonoid content, respectively. The results of anti-inflammatory activity showed 84.69+0.82% protein inhibition by BSA and also showed IC50 values of 68.53 µg/mL and 43.34 µg/mL for COX1 and COX 2, respectively. It exhibited 63.91+0.08% of radical scavenging activity by DPPH. The IC50 values of 181.41 µg/mL and 190.62 µg/mL were found for the in vitro antidiabetic activity. This study shows that the endophytic fungus A. melleus has exhibited considerably good results with respect to its in vitro biological activities. Yet, there is a scope for future researchers to isolate the bioactive metabolites to explore for future needs

GC-MS Analysis and In-vitro Apoptosis Induction and Anticancer Activity of Methanol Extract of Aspergillus terreusagainst Lung Cancer

The present study was focusing on qualitative and quantification of bioactive compounds present in Aspergillus terreus and evaluating its anticancer activity and apoptosis detection against lung cancer. Methods: A. terreus was sequentially extracted using the Soxhlet extraction technique with hexane, ethyl acetate, methanol and distilled water. Detection of bioactive compounds was done using Standard biochemical tests and GC-MS analysis was performed with NIST database to identify the bioactive compounds. The toxicity and anticancer activity of crude extract was investigated using MTT assay on L929 cells and lung cancer A549 cells whereas apoptosis study was conducted through Flowcytometry-based surface marker study on the A549 cancer cell line. Results: secondary metabolites analysis showed the presence of phenols and terpenoids as major constituents in the methanol extract whereas other solvent extracts have shown the absence of major bioactive compounds. Quantification studies showed that methanol extract has shown the phenolic content 179 µg/g of Gallic acid equivalent. The GC-MS analysis showed the presence of 1-Flurodecane, Methyl palmitate, Ethyl palmitate, 9, 12-Octadecanopic acid, 10-Octadecanoic acid, Methyl stearate, Octadecadeoinoate, Ethyl 9-hexadecanoate and 1-Monoarachidin as major bioactive compounds. Further, MTT based toxicity study on the L929 cell line revealed that methanol extract at lower concentrations like 50µg, 100µg and150µg shown more than 50% of cell viability and at higher concentration between 200µg-250 µg it was showing toxic nature with 47.89±0.01% viability. In case of anticancer activity against lung cancer A549 cell line the methanol extract have shown the dose dependent activity i.e the percentage of cell viability was decreased with increase in the concentration of methanol extract at 250µg the cell viability was found to be 35.12±0.005%. Flow cytometry based apoptosis study revealed that methanol extract has shown the inducing apoptosis in treated lung cancer A549 cells with percentage of 10.84. Conclusion: overall the present study shown that A. terreus possess different class of bioactive compounds and it has higher phenolic content. Toxicity study showed that methanol extract exhibited toxic nature at higher concentration on tested cell line and Anticancer and Apoptosis study revealed that methanol extract has shown the prominent with inhibiting the growth of lung cancer A549 cells through inducing apoptosis. Further, A. terreus would be a promising natural microorganism that has to be further researched in order to discover and isolate potent drug to treat cancer. Future studies will be on study of in-vivo animal studies and study of molecular mechanism of drug action on particular with anticancer study

Synthesis, in vitro biological evaluation and molecular docking study of coumarin-1,4-dihydropyridine derivatives as potent anti-inflammatory agents

The green chemistry approach provides for the synthesis of coumarin-1,4-dihydropyridine scaffolds 6a-o via sequential multicomponent reaction using catalytic amount of triethylamine (TEA). These new coumarin scaffolds have been successfully explored for the effective inflammatory as well as microbial infection inhibitors. The antimicrobial activity results of the title compounds have shown potent activity against both gram positive and gram negative bacterial, and fungal stains. Additionally, anti-inflammatory activity of all the compounds has been found to be quite promising in comparison with standard Diclofenac sodium. Furthermore, the in silico docking study has been performed for all the compounds with S. aureus DNA gyrase and cyclooxygenase-2 (PDB ID 4PH9). The computational results are in good agreement with the in vitro antibacterial and anti-inflammatory experimental results.

Synthesis, in vitro biological evaluation and molecular docking study of coumarin-1,4-dihydropyridine derivatives as potent anti-inflammatory agents

418-432The green chemistry approach provides for the synthesis of coumarin-1,4-dihydropyridine scaffolds 6a-o via sequential multicomponent reaction using catalytic amount of triethylamine (TEA). These new coumarin scaffolds have been successfully explored for the effective inflammatory as well as microbial infection inhibitors. The antimicrobial activity results of the title compounds have shown potent activity against both gram positive and gram negative bacterial, and fungal stains. Additionally, anti-inflammatory activity of all the compounds has been found to be quite promising in comparison with standard Diclofenac sodium. Furthermore, the in silico docking study has been performed for all the compounds with S. aureus DNA gyrase and cyclooxygenase-2 (PDB ID 4PH9). The computational results are in good agreement with the in vitro antibacterial and anti-inflammatory experimental results

Physicochemical properties, antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids

Objective: To study physicochemical properties, antioxidant and anti-inflammatory activities of coumarin-carbonodithioate hybrids. Methods: The substituted 4-bromomethyl coumarins were synthesized in first step by the cyclization. Then the reaction of substituted coumarins (a-e) with potassium O-ethyl/methyl carbonodithioate (1) by using absolute ethanol as solvent, afforded coumarin-carbonodithioate (1a-1j) derivatives under microwave irradiation and the conventional method. The spectroscopic analysis was used for the characterization of coumarin derivatives. The title (1a-1j) compounds were confirmed by spectroscopic methods. Antioxidant property was evaluated by using DPPH free radical-scavenging ability assay method and anti-inflammatory activity was evaluated by protein denaturation procedure using diclofenac sodium as a standard. Drug-likeness. In-silico toxicity was predicted with LD50 value and bioactivity score was also calculated for all the compounds. Results: All coumarin (1a-1j) compounds exhibited promising in-vitro antioxidant and anti-inflammatory properties in comparison to standard drugs. All tested compounds were used for evaluating their physicochemical properties as set by Lipinski rule. It was observed that the synthesized compounds followed rule of five, indicating more ‘drug-like’ nature. Conclusions: All the screened coumarin-carbonodithioates display promising in vitro antioxidant and anti-inflammatory activities. From the physicochemical properties of coumarin derivatives, it is found that none of the compounds violate the Lipinski rule and they fall well in the range of rule of five. It is concluded that the coumarin-carbonodithioate hybrids act with more ‘drug-like’ nature

GCMS-based phytochemical profiling and in vitro pharmacological activities of plant Alangium salviifolium (L.f) Wang

Abstract Background There is an urge for traditional herbal remedies as an alternative to modern medicine in treating several diseases. A significant number of modern pharmaceutical drugs are based on or derived from medicinal plants or their extracts. These drugs derived from the plant origin have various antimicrobial, antioxidant, anticancer, anti-inflammatory activities. Alangium salviifolium belongs to Cornaceae family and is well known for its medicinal properties. The present study was carried out to evaluate the antibacterial, antioxidant effect and possible bioactive components present in the chloroform, acetone, ethanol, methanol and aqueous extract of Alangium salviifolium leaves. Methodology Dried leaves of Alangium salviifolium were subjected to serial solvent extraction using increasing polarity of solvents, i.e., chloroform, acetone, methanol, ethanol, and distilled water. Crude extracts were further tested for qualitative analysis of phytochemicals using standard procedure, while GCMS analysis was performed to identify the probable phytocompounds. Antibacterial activity was performed against bacterial pathogens using agar well method, whereas antioxidant activity was performed using in vitro PM, DPPH and FRAP assays. Results Phytochemical analysis of the extracts revealed the presence of key phytochemical classes. Using gas chromatography-mass spectrometry, several high and low molecular weight chemical compound kinds were discovered. These chemical substances are regarded as having significant biological and pharmacological effects. All crude extracts had considerable and comparable in vitro antioxidant and antibacterial properties. Conclusions According to the findings of this study, Alangium salviifolium leaves are a rich source of phytoconstituents that are crucial in stopping the advancement of numerous disorders

A pilot study: Changes of MDAMB-231 cancer cell line response to synthesized oleic acid – coated MgFe2O4 nano ferrite compound and its cytotoxic effects on L929 cell line

In this investigation, we synthesized MgFe2O4 nano ferrite compounds using the sol-gel method and coated them with oleic acid. The synthesized compounds were evaluated for cytotoxicity study on the L929 cell line and the anticancer activity against the breastcancer-MDAMB-231 cellline using in vitro approach. The physical structure of the compounds was confirmed to have a cubic spinel structure and Fd3m space group using X-ray diffraction (XRD). Scherrer's formula revealed crystallite sizes of 11 nm for MgFe2O4and 33 nm for oleic acid-coated MgFe2O4 nanoferrites. Fourier transform infrared (FTIR) spectroscopy confirmed the existence of MgFe2O4 inuncoated and coated compounds. Scanning electron microscopy (SEM) was used to examine the surface structure and morphology of the synthesized compounds. The compounds show a grain-like structure with a little agglomeration. With the help of histogram graph average size of the particles are determined, where the MgFe2O4 and coated MgFe2O4 have 17.2 and 20 nm average particle sizes. Testing of magnetic properties was done with a vibrating sample magnetometer (VSM), demonstrating ferromagnetic properties for the samples. Cytotoxicity tests revealed that MgFe2O4 exhibited higher cytotoxicity compared to oleic acid-coated MgFe2O4 nanoferrite on L929 cells. MgFe2O4 & oleic acid-coated MgFe2O4 compounds were tested on the MDAMB-231 breast cancer cell line, with the uncoated sample displaying significantly greater anticancer activity, as evidenced by a higher percentage of cell viability and a lower IC50 value of 55.67 µg compared to 65.97 µg for the coated sample

Additional file 1 of GCMS-based phytochemical profiling and in vitro pharmacological activities of plant Alangium salviifolium (L.f) Wang

Additional file 1: Figure S1. Alangium salviifolium mature plant. Figure S2. FTIR Spectra of Leaf Chloroform extract of A. salviifolium. Figure S3. FTIR Spectra of Leaf Acetone extract of A. salviifolium. Figure S4. FTIR Spectra of Leaf Ethanol extract of A. salviifolium. Figure S5. FTIR Spectra of Leaf Methanol extract of A. salviifolium. Figure S6. FTIR Spectra of Leaf Aqueous extract of A. salviifolium. Figure S7. GC-MS chromatogram of Chloroform extract of A. salviifolium leaves. Figure S8. GC-MS chromatogram of Acetone extract of A. salviifolium leaves. Figure S9. GC-MS chromatogram of Ethanol extract of A. salviifolium leaves. Figure S10. GC-MS chromatogram of Methanol extract of A. salviifolium leaves. Figure S11. GC-MS chromatogram of Aqueous extract of A. salviifolium leaves. Figure S12. Graph for Phosphomolybdenum (PM) assay for A. salviifolium leaf extract. Figure 13. Graph for FRAP assay for A. salviifolium leaf extract. Figure S14. Anti-bacterial activity of Leaf extract of A. salviifolium against S. aureus; A: Chloroform extract; B: Acetone extract; C: Ethanol extract; D: Methanol extract; E: Aqueous extract; F: Control. Figure S15. Anti-bacterial activity of Leaf extract of A. salviifolium against P. aeroginosa; A: Chloroform extract; B: Acetone extract; C: Ethanol extract; D: Methanol extract; E: Aqueous extract; F: Control

Green Synthesis and Characterization of Iron Nanoparticles Synthesized from Aqueous Leaf Extract of Vitex leucoxylon and Its Biomedical Applications

The cold extraction method was used to obtain the aqueous extract of Vitex leucoxylon leaves in a ratio of 1:10. Iron nanoparticles (FeNPs) were synthesized using aqueous leaf extract of V. leucoxylon as a reducing agent. The phytoreducing approach was used to make FeNPs by mixing 1 mL of plant extract with 1 mM of ferric sulfate. Scanning electron microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), Ultraviolet–visible spectroscopy (UV-Vis), and energy-dispersive X-ray spectroscopy were used to examine the synthesized FeNPs. The reducing reaction was shown by a change in the color of the solution, and the formation of black color confirms that FeNPs have been formed. The greatest absorption peak (max) was found at 395 nm in UV-Vis spectral analysis. The FTIR spectra of V. leucoxylon aqueous leaf extract showed shifts in some peaks, namely 923.96 cm−1 and 1709.89 cm−1, with functional groups carboxylic acids, unsaturated aldehydes, and ketones, which were lacking in the FTIR spectra of FeNPs and are responsible for FeNPs formation. FeNPs with diameters between 45 and 100 nm were observed in SEM images. The creation of FeNPs was confirmed by EDX, which shows a strong signal in the metallic iron region at 6–8 Kev. XRD revealed a crystalline nature and an average diameter of 136.43 nm. Antioxidant, anti-inflammatory, cytotoxic, and wound healing in vitro tests reported significant activity of the FeNPs. The cumulative findings of the present study indicate that the green synthesis of FeNPs boosts its biological activity and may serve as a possible dermal wound-healing agent and cytotoxic agent against cancer. Future study is needed on the identification of mechanisms involved in the synthesis of FeNPs by V. leucoxylon and its biomedical applications

Synthesis and Characterization of Silver Nanoparticles from Rhizophora apiculata and Studies on Their Wound Healing, Antioxidant, Anti-Inflammatory, and Cytotoxic Activity

Silver nanoparticles (AgNPs) have recently gained interest in the medical field because of their biological features. The present study aimed at screening Rhizophora apiculata secondary metabolites, quantifying their flavonoids and total phenolics content, green synthesis and characterization of R. apiculata silver nanoparticles. In addition, an assessment of in vitro cytotoxic, antioxidant, anti-inflammatory and wound healing activity of R. apiculata and its synthesized AgNPs was carried out. The powdered plant material (leaves) was subjected to Soxhlet extraction to obtain R. apiculata aqueous extract. The R. apiculata extract was used as a reducing agent in synthesizing AgNPs from silver nitrate. The synthesized AgNPs were characterized by UV-Vis, SEM-EDX, XRD, FTIR, particle size analyzer and zeta potential. Further aqueous leaf extract of R. apiculata and AgNPs was subjected for in vitro antioxidant, anti-inflammatory, wound healing and cytotoxic activity against A375 (Skin cancer), A549 (Lung cancer), and KB-3-1 (Oral cancer) cell lines. All experiments were repeated three times (n = 3), and the results were given as the mean ± SEM. The flavonoids and total phenolics content in R. apiculata extract were 44.18 ± 0.086 mg/g of quercetin and 53.24 ± 0.028 mg/g of gallic acid, respectively. SEM analysis revealed R. apiculata AgNPs with diameters ranging from 35 to 100 nm. XRD confirmed that the synthesized silver nanoparticles were crystalline in nature. The cytotoxicity cell viability assay revealed that the AgNPs were less toxic (IC50 105.5 µg/mL) compared to the R. apiculata extract (IC50 47.47 µg/mL) against the non-cancerous fibroblast L929 cell line. Antioxidant, anti-inflammatory, and cytotoxicity tests revealed that AgNPs had significantly more activity than the plant extract. The AgNPs inhibited protein denaturation by a mean percentage of 71.65%, which was equivalent to the standard anti-inflammatory medication diclofenac (94.24%). The AgNPs showed considerable cytotoxic effect, and the percentage of cell viability against skin cancer, lung cancer, and oral cancer cell lines was 31.84%, 56.09% and 22.59%, respectively. R. apiculata AgNPs demonstrated stronger cell migration and percentage of wound closure (82.79%) compared to the plant extract (75.23%). The overall results revealed that R. apiculata AgNPs exhibited potential antioxidant, anti-inflammatory, wound healing, and cytotoxic properties. In future, R. apiculata should be further explored to unmask its therapeutic potential and the mechanistic pathways of AgNPs should be studied in detail in in vivo animal models