5-Fluorouracil And Curcumin With Pectin Coating As a Treatment Regimen For Titanium Dioxide Induced Colon Cancer Model

Objective: Induction of colorectal cancer in Wister rats using titanium dioxide and dimethylhydrazine and treatment using the physical conjugate of 5-Fluorouracil and Curcumin, with a synergistic approach.Methods: Compatibility studies are evaluated by using FT-IR,Vero cell lines, and HCT-116 cell lines are used for evaluating the synergistic approach. This followed by induction using titanium dioxide and dimethylhydrazine in Wister rats and treatment using 5-Fluorouracil and Curcumin with pectin coating. Result: The samples were found to be compatible. The synergistic effect was obtained at 1:1, 1:2, 1:4, and 2:1 ratio, where 1:4 ratio shows a CI50 value of 0.896, selected further for the animal studies when studied in HCT 116 cell lines and found to be safe with Vero cell lines. Colorectal cancer was shown to be induced within 70 days of administration of titanium dioxide and dimethylhydrazine.1:4 ratio of 5-Fluorouracil and Curcumin (50:200) shows effective for the treatment of colorectal cancer within 28 days, proven using histopathology report, bodyweight analysis, and hematological reports.Conclusion: 5-Fluorouracil and curcumin (1:4) ratio works with a synergistic approach and was proven effective for the treatment of colorectal cancer induced bythe titanium dioxide and dimethylhydrazine.

Antimicrobial and Antibiofilm Activities of 4,5-Dihydro-1H-pyrazole-1-carboximidamide Hydrochloride against Salmonella spp.

In the present study, the antimicrobial and antibiofilm activities of two 4,5-dihydro-1H-pyrazole-1-carboximidamide hydrochloride, (trifluoromethyl) phenyl-substituted (compound 1) and bromophenyl-substituted (compound 2), were evaluated against four Salmonella spp. serotypes through broth microdilution and biofilm-forming activity. Further, the cytotoxicity of the compounds was evaluated by cell viability assays using cultures of HeLa and Vero cell lines, and the mutagenic potential was assessed by the Ames test. In the broth microdilution test, compound 1 inhibited 90% of the strains tested at the minimum inhibitory concentration of 62.5 μg mL−1. Furthermore, both compounds prevented biofilm formation, with a reduction of up to 5.2 log10. HeLa and Vero cells exhibited 100% viability in the presence of compound 1. In contrast, low cell viability was observed in the presence of 15 µg mL−1 of compound 2. Furthermore, no mutagenic potential was detected at any of the tested concentrations of compound 1.

Antiproliferative effect of extracts and fractions of the root of Terminalia avicennioides (Combretaceae) Guill and Perr. on HepG2 and Vero cell lines

Background Terminalia avicennioides Guill and Perr (Combretaceae) is an important West African medicinal plant. The plant is used locally against microbes and parasites in both humans and animals and studies have demonstrated its cytotoxicity potential. Thus, this study was carried out to test the cytotoxic effect of the extracts and fractions of the root of the medicinal plant Terminalia avicennioides Guill and Perr (Combretaceae) in two different cell lines. Methods Methanol, ethanol, 30 % ethanol, hot water and cold water extracts and ethylacetate, hexane, chloroform, butanol and residual water fractions, were evaluated at 1000, 750, 500, 250, 100 and 50 µg/mL concentrations, with doxorubicin as positive control. The cells were incubated with the extracts for 48 h at 37 °C in a 5 % CO2 humidified incubator. The inhibition of cell viability, determined with the methyl blue thiazole tetrazolium bromide (MTT) assay, was used to assess the anti-proliferative effect of the extracts, in normal Vero Monkey kidney and human liver cancer (HepG2) cell lines. Results There was a concentration-dependent inhibition of cell viability in both the HepG2 and Vero cell lines. For HepG2 cells, antiproliferative effect was highest for the hexane fraction (viability ranged from 19.63 ± 1.10 % to 70.30 ± 1.78 % for 1000 and 50 µg/mL, respectively. For Vero cells, the highest antiproliferative effect, at 1000 µg/mL, was with hexane fraction (cell viability 21.37 ± 3.50 %), while at 50 µg/mL the chloroform fraction demonstrated the highest effect (viability of 86.10 ± 1.95 %). Conclusions The extracts and fractions from the root of Terminalia avicennioides have antiproliferative effect on the Vero and HepG2 cell lines tested. However, the extracts and fractions were not more toxic to the HepG2 than to the Vero cells. The cytotoxic effect of stem-bark and leaf extracts could be evaluated in the future to determine its anticancer potential.

Studies of Physico-chemical Properties and Cytotoxicity of Fruits of Syzygium jambos L. against HeLa and Vero Cell Lines

Syzygium jambos L. belonging to the family Myrtaceae has a long history of using as a dietary fruit and folklore medicine. Investigation of this fruit was carried out to evaluate the different chemical properties and biological activities. The moisture and ash content of the fruit sample were calculated as 86.88 ± 0.61% and 0.29±0.02%, respectively. Dried powder of the fruit was extracted successively with nhexane, dichloromethane (DCM) and methanol (MeOH). UV-Visible and FT-IR spectral analyses confirmed the presence of unsaturated carboxylic acid in n-hexane, unsaturated ester in DCM and a diketone in MeOH extracts. Cytotoxicity assay of different extracts was carried out against HeLa and Vero cell lines and no extract was found to be cytotoxic. Total phenolic contents of the n-hexane, DCM and MeOH extracts were 15.39 ± 0.24, 31.32 ± 0.25 and 42.19 ± 0.16 mg gallic acid equivalent per gram of dry extract, respectively and total flavonoid content of n-hexane, DCM and MeOH extracts were 6.52 ± 0.18, 15.55 ± 0.16 and 8.36 ± 0.16 mg quercetin equivalent per gram of dry extract, respectively. This study establishes that S. jambos fruit can be a potential source of natural antioxidants. Bangladesh Pharmaceutical Journal 24(2): 111-116, 2021

Green Synthesis of Chromium Oxide Nanoparticles for Antibacterial, Antioxidant Anticancer, and Biocompatibility Activities

This study deals with the green synthesis of chromium oxide (Cr2O3) nanoparticles using a leaf extract of Abutilon indicum (L.) Sweet as a reducing and capping agent. Different characterization techniques were used to characterize the synthesized nanoparticles such as X-ray diffraction (XRD), Scanning electron microscope (SEM), Transmission electron microscope (TEM), Energy-dispersive X-ray (EDX), Fourier transform infrared (FTIR), X-ray photoelectron spectroscopy (XPS), and ultraviolet-visible (UV-VIS) spectroscopy. The X-ray diffraction technique confirmed the purity and crystallinity of the Cr2O3 nanoparticles. The average size of the nanoparticles ranged from 17 to 42 nm. The antibacterial activity of the green synthesized nanoparticles was evaluated against four different bacterial strains, E. coli, S. aureus, B. bronchiseptica, and B. subtilis using agar well diffusion and a live/dead staining assay. The anticancer activities were determined against Michigan Cancer Foundation-7 (MCF-7) cancer cells using MTT and a live/dead staining assay. Antioxidant activity was investigated in the linoleic acid system. Moreover, the cytobiocompatibility was analyzed against the Vero cell lines using MTT and a live/dead staining assay. The results demonstrated that the green synthesized Cr2O3 nanoparticles exhibited superior antibacterial activity in terms of zones of inhibition (ZOIs) against Gram-positive and Gram-negative bacteria compared to plant extracts and chemically synthesized Cr2O3 nanoparticles (commercial), but comparable to the standard drug (Leflox). The green synthesized Cr2O3 nanoparticles exhibited significant anticancer and antioxidant activities against MCF-7 cancerous cells and the linoleic acid system, respectively, compared to chemically synthesized Cr2O3 nanoparticles. Moreover, cytobiocompatibility analysis displayed that they presented excellent biocompatibility with Vero cell lines than that of chemically synthesized Cr2O3 nanoparticles. These results suggest that the green synthesized Cr2O3 nanoparticles’ enhanced biological activities might be attributed to a synergetic effect. Hence, green synthesized Cr2O3 nanoparticles could prove to be promising candidates for future biomedical applications.

Phytochemical and Biological Activity Studies of Tinospora crispa Stem

Three compounds namely, tinosporol A, 8-methoxy palmatine and callecdysterol C were isolated from the methanol extract of the stem of Tinospora crispa. Biological activities of different partitionates of the parent extract was also evaluated. Antimicrobial screening of different partitionates was carried out against sixteen different microorganisms and only n-hexane fraction exhibited significant zone of inhibition against Staphylococcus aureus (9 mm), Shigella boydii (9 mm), Shigella dysenteriae (9 mm), Candida albicans (10 mm) and Aspergillus niger (10 mm).The crude methanol extract showed the highest general toxicity with LC50 values of 57.14 μg/mL against brine shrimp lethality bioassay.The total antioxidant capacity of aqueous fraction was found to be 61.61 mg as ascorbic acid equivalentper gram of plant extract.The antioxidant activity of DCM fraction revealed the highest activity having IC50 values 54.74 μg/mL. No significant cytotoxicity was observed on both HeLa and Vero cell lines. Dhaka Univ. J. Sci. 68(2): 167-170, 2020 (July)

Phytochemical characterization and cytotoxicity analysis of ayurvedic formulation of drug

The liver is a major endocrine organ which controls the significant metabolic activity in the human body. Treatment of several liver disorders with herbal based plant drugs is popularising nowadays due to their hepatoprotective and nontoxic effect. Livoral, a polyherbal Ayurvedic formulation is one such drug commonly recommended for liver disorders in India. The current work was aimed at studying the phytochemical characterisation and cytotoxic activity of livoral. Phytochemical analysis of extracts of livoral in methanol, hexane, acetone and petroleum ether was studied by TLC method. The cytotoxic activity of livoral was analysed by MTT assay in Vero cell lines at a concentration ranging from 10µg/ml to 500µg/ml. The phytochemical analysis revealed the presence of Phyto compound such as tannins, phenols, steroids, alkaloids, terpenes and carbohydrates in all the four types of livoral extracts. Phytochemicals such as phenols, terpenes and alkaloids were already known for their hepatoprotective activity. MTT assay revealed the nontoxic effect of livoral up to 300 µg/ml concentrations. Thus, based on the results of the phytochemical and cytotoxic analysis, the livoral was proven to be one of the best herbal drugs for liver disorders with hepatoprotective constituents and non-cytotoxic effect.

Antimalarial activity of Curcuma caesia against 3D7 and K1 strains of Plasmodium falciparum

Background: Malaria is one of the severe tropical disease and majority of deaths occurred due to Plasmodium falciparum. Lack of a vaccine and the widespread resistance to antimalarial drugs have resulted in emphasis on novel antimalarial drugs development. The purpose of the study was to evaluate in vitro and in-silico antiplasmodial potential of Curcuma caesia extracts against P. falciparum.Methods: Ethyl acetate and methanol extracts of C. caesia were prepared and analysed for their antiplasmodial activity against Chloroquine sensitive (3D7) and resistant (K1) strains of P. falciparum using fluorescence-based SYBR Green assay. The cytotoxicity tests were carried out using the vero cell lines by MTT assay. The phosphoethanolamine methyltransferase enzyme ((PfPMT) essential for growth of P. falciparum was used as protein target for in-silico study. Result: C. caesia ethyl acetate extracts showed the potent antiplasmodial activity with IC50 values of 3.37 µg/ml and 1.53 µg/ml against 3D7 and K1 strain respectively. The IC50 values of methanol extract were reported, 8.57 µg/ml against 3D7 and 18.29 µg/ml against K1 strains The cytotoxicity assay revealed that the extracts were not toxic against vero cell lines as the CC50 values were less than IC50. Docking results show that β-selinenol an oxygenized sesquiterpene present in C. caesia had the free binding energy of -6.76 Kcal/mol.Conclusion: The compounds β-selinenol, α-eudesmol, α –acorenol, boldione and xanthinin present in the C. caesia extract possess antimalarial potential being inhibitor of PfPMT. The present findings, however preliminary in nature. Further studies are needed to identify the active compounds and in vivo mechanism to prove the antimalarial efficacy of C. caesia in the development of antimalarial drugs.