In Vitro Screening for Cytotoxic, Anti-bacterial, Anti-HIV1-RT Activities and Chemical Constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii

2021 ◽  
Vol 11 ◽  
Author(s):  
Charina Worarat ◽  
Wilart Pompimon ◽  
Phansuang Udomputtimekakul ◽  
Sukee Sukdee ◽  
Punchavee Sombutsiri ◽  
...  

Background: Although the chemical constituents and biological activities of a large number of plants in the Croton genus have been studied, there are still recently discovered plants to be investigated. Objective: 1. To investigate the anti-bacterial, anti-HIV1-RT, and cytotoxicity activities of crude extracts from these plants. 2. To investigate the chemical constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii. Method: The anti-bacterial, anti-HIV1-RT, and cytotoxicity of the three plants were evaluated by standard techniques. Extraction, separation, and purification of extracts from the three plants were undertaken. Results: The ethyl acetate extract of C. fluviatilis showed low anti-bacterial activity against E. aerogenes, E. coli 0157: H7, and P. mirabilis, together with the ethyl acetate extract of C. acutifolius displayed low anti-bacterial activity against E. aerogenes, while all the crude extracts of C. thorelii were inactive. The ethyl acetate extracts of C. thorelii, and C. fluviatilis showed strong inhibited HIV1-RT, whereas the ethyl acetate extract of C. acutifolius, and the hexane extract of C. fluviatilis displayed moderate inhibited HIV1-RT. Cytotoxic properties of three Croton plants were specific to KKU-M213, MDA-MB-231, A-549, and MMNK-1. Especially, the ethyl acetate extract of C. acutifolius exhibited strong cytotoxic activities against MDA-MB-231, A-549, and MMNK-1. Furthermore, the ethyl acetate extract of C. thorelii showed high cytotoxic activities against KKU-M213, and MDA-MB-231. Compounds 1, and 4 were found in C. fluviatilis. Compounds 2 and 4 were also found in C. acutifolius. Moreover, compound 3 was only found in C. thorelii. Conclusion: The present study revealed that the three Croton species are good sources of flavonoid compounds and further investigation of the chemical constituents from these plants may prove to be fruitful to discover more active compounds to be tested as potential medicines.

2020 ◽  
Vol 10 ◽  
Author(s):  
Sakchai Chaibun ◽  
Wilart Pompimon ◽  
Chanika Tidchai ◽  
Noraset Chalaemwongwan ◽  
Jutarut Wongping ◽  
...  

Background: C. delpyi, C. decalvatus and C. caudatus are in the Euphorbiaceae family. The aerial parts; twigs, leaves and barks of these plants were used as traditional medicine such as anti-inflammatory, cytotoxicity, and antifungal properties. Objectives: The aims of this work were 1) to study the chemical composition of C. delpyi, C. decalvatus, and C. caudatus 2) to test their antibacterial, anti-HIV-1 RT, and cytotoxicity activities of crude extracts and pure compounds from these plants. Methods: Extraction, separation and purification of three plants were performed under chromatographic method. The biological activities including antibacterial, anti-HIV-1 RT and cytotoxicity assay of three plants were evaluated by the standard methods. Results: Phytochemical investigation of C. delpyi was founded a new clerodanes diterpenoids; crotondelpyitin A (1). The five known compounds, such as acetyl aleuritolic acid (2), 5-hydroxy-7,4- dimethoxyflavone (3), and pilloin (4) were founded in C. decalvatus and 3α-benzoyloxy-D:A-friedo-oleanan-27,16αlactone (5), and bergenin (6) were founded in C. caudatus. The compound 3 show the most effective antibacterial activities with MIC in range <0.16 -1.25 mg/mL, and MBC in range 0.6 - >5.0 mg/mL. The six compounds were inactive with antiHIV-1 RT. In addition, compound 4 was active for cytotoxic activities on FaDu and KKU-M213 at <4 µg/mL. Conclusion: The present study reveals that the Croton species are sources of diterpenoid-type compounds and significant guide for further research of the chemical constituents from these plants as potential medicines.


2019 ◽  
Vol 57 (3) ◽  
pp. 294
Author(s):  
Ho Dac Hung ◽  
Doan Huy Tien ◽  
Nguyen Thi Ngoan ◽  
Ba Thi Duong ◽  
Do Quoc Viet ◽  
...  

The first study on chemical constituents and biological activities of fruits of Dipterocarpus retusus Blume (Dipterocarpaceae.) growing in Vietnam was reported. Column chromatography of the ethyl acetate extract led to the isolation of five compounds: eleutherol (1), 3, 5, 4' - trihydroxy - trans - stilbene (2), polydatin (3) and β-sitosterol (4), β-sitosterol-3-O-β-D-glucopyranoside (5). Their structures were elucidated based on the NMR spectroscopic methods and comparison with literature date. The extracts from fruits of D. retusus Blume by n-hexane, ethyl acetate and butanol, consecutively, were evaluated for antioxidative and cytotoxic activities.


2018 ◽  
Vol 34 (11) ◽  
pp. 1586-1590 ◽  
Author(s):  
Wassila Benabderrahmane ◽  
Amel Amrani ◽  
Ouahiba Benaissa ◽  
Marta Lores ◽  
J. Pablo Lamas ◽  
...  

2015 ◽  
Vol 13 (1) ◽  
pp. 63-67
Author(s):  
Mozammel Haque ◽  
Mohammad Shoeb ◽  
Nilufar Nahar

Two compounds, ergosterol (1) and 4-hydroxy-hexadec-6-enoic acid methyl ester (2) were isolated from the ethyl acetate extract of the endophytic fungal strain labeled as MI-3, isolated from the leave of Magnifera indica L. The structures of the isolated compounds were elucidated by 1H NMR studies and comparing with published data. The crude ethyl acetate extract, three column fractions and ergosterol were tested for antimicrobial activity against five Gram-positive and eight Gram-negative bacteria and three fungi by disc diffusion method. The general toxicity and antioxidant activity of the parent extract, column fractions and ergosterol were also evaluated by using brine shrimp lethality assay and free radical scavenging assay, respectively. Low activities were observed in all cases. DOI: http://dx.doi.org/10.3329/dujps.v13i1.21862 Dhaka Univ. J. Pharm. Sci. 13(1): 63-67, 2014 (June)


2019 ◽  
Vol 8 (2) ◽  
pp. 103-111
Author(s):  
Jaqueline Scapinello ◽  
Monica S. Z. Schindler ◽  
Leila Zanatta ◽  
Laura Cassol Mohr ◽  
Ana Paula Capelezzo ◽  
...  

Many of the species used in popular medicine do not have their biological activities already proven by scientific studies. Among these species, the endemic South American Philodendron bipinnatifidum Schott ex Endl deserves special attention since it is already in use in popular medicine for inflammation cases, such as erysipelas, orchitis and ulcers. This study evaluated the antioxidant, antimicrobial and antidiabetic activities of extracts of the hastes de P. bipinnatifidum. The ethanolic extract showed a significant antioxidant potential. The ethyl acetate extract resulted in high antimicrobial activity against Streptococcus pyogenes. The most significant biological activity of ethyl acetate extract relates to its chemical composition when compared with ethanolic extract, which showed the highest concentration of bioactive compounds. In vitro antidiabetic activity was only evaluated for ethyl acetate extract, resulting in inhibition of intestinal disaccharidases (maltase and sucrase) at concentration of 500 μg/mL.


2018 ◽  
Vol 56 (4A) ◽  
pp. 246
Author(s):  
Quang Ngoc Dang

Five fungal secondary metabolites named 1,2,4,5-tetrachloro-3,6-dimethoxybenzene (1); ergosterol (2); ergosterol peroxide (3); (E)- 4-(3,4-dihydroxyphenyl)but-3-en-2-one (4) and [Bi-1,4-cyclohexandien-1-yl]-3,3’,6,6’-tetrone, 4, 4’-dihydroxyl-2,2’,5,5’-tetramethyl (5) were purified from ethyl acetate extract of the fruit bodies of Phellinus gilvus collected at Pu Mat national park, Nghe An province. Their structures were charaterized by 1D, 2D NMR and GC-MS spectroscopies. Especially, the structure of compound 1 was confirmed by X-ray crystallographic analysis. The antimicrobial and cytotoxicity activities of compounds 1 were also evaluated. This is the first report on the chemical constituents of Vietnamese Phellinus gilvus.


Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 4009
Author(s):  
Ahmed S. Abu Zaid ◽  
Ahmed E. Aleissawy ◽  
Ibrahim S. Yahia ◽  
Mahmoud A. Yassien ◽  
Nadia A. Hassouna ◽  
...  

Background: This study aimed to produce, purify, structurally elucidate, and explore the biological activities of metabolites produced by Streptomyces (S.) griseus isolate KJ623766, a recovered soil bacterium previously screened in our lab that showed promising cytotoxic activities against various cancer cell lines. Methods: Production of cytotoxic metabolites from S. griseus isolate KJ623766 was carried out in a 14L laboratory fermenter under specified optimum conditions. Using a 3-(4,5-dimethylthazol-2-yl)-2,5-diphenyl tetrazolium-bromide assay, the cytotoxic activity of the ethyl acetate extract against Caco2 and Hela cancer cell lines was determined. Bioassay-guided fractionation of the ethyl acetate extract using different chromatographic techniques was used for cytotoxic metabolite purification. Chemical structures of the purified metabolites were identified using mass, 1D, and 2D NMR spectroscopic analysis. Results: Bioassay-guided fractionation of the ethyl acetate extract led to the purification of two cytotoxic metabolites, R1 and R2, of reproducible amounts of 5 and 1.5 mg/L, respectively. The structures of R1 and R2 metabolites were identified as β- and γ-rhodomycinone with CD50 of 6.3, 9.45, 64.8 and 9.11, 9.35, 67.3 µg/mL against Caco2, Hela and Vero cell lines, respectively. Values were comparable to those of the positive control doxorubicin. Conclusions: This is the first report about the production of β- and γ-rhodomycinone, two important scaffolds for synthesis of anticancer drugs, from S. griseus.


2021 ◽  
pp. 17-17
Author(s):  
Janpen Tangjitjaroenkun ◽  
Wanchai Pluempanupat ◽  
Rungnapa Tangchitcharoenkhul ◽  
Waraporn Yahayo ◽  
Roongtawan Supabphol

The in vitro biological activities of the ethyl acetate extract of the culture filtrate from Streptomyces achromogenes TCH4 (TCH4 extract) were evaluated. The ethyl acetate extract of TCH4 produced a bacteriostatic effect against Enterobacter cloacae, Staphylococcus aureus, Staphylococcus saprophyticus, Bacillus subtilis, methicillin-resistant S. aureus (MRSA) and Klebsiella pneumoniae. The extract had bactericidal activity against S. aureus, S. saprophyticus, S. aureus (MRSA) and K. pneumoniae with minimum bactericidal concentration (MBC) values in the range of 500-1000 ?g/mL. The total phenolic and flavonoid contents in TCH4 were 107.20?2.57 mg gallic acid equivalent (GAE)/g and 44.91?0.84 mg quercetin equivalent (QE)/g of dry extract. Antioxidant activity was determined by DPPH radical (IC50 299.64?6.83 ?g/mL) and ABTS radical scavenging (IC50 65.53?0.95 ?g/mL), and the ferric-reducing antioxidant power (FRAP) (822.76?9.12 mM FeSO4.7H2O/g dry extract) assays. TCH4 exhibited cytotoxic activity in the DU-145 cell line (IC50 9.36?0.37 ?g/mL). Analysis of extract constituents by GC-MS revealed pyrrolo[1,2-a]pyrazine-1,4-dione, hexahydro-3-(2-methylpropyl) (36.85%), benzeneacetamide (23.76%), and deferoxamine (12.85%) as the major compounds, which have been reported to possess pharmaceutical properties. S. achromogenes TCH4 could be a potential source of bioactive metabolites with antibacterial, antioxidant and anticancer activities for pharmaceutical applications.


Author(s):  
Ni Wayan Rika Kumara Dewi ◽  
I Wayan Gunawan ◽  
Ni Made Puspawati

ABSTRAK: Penelitian ini bertujuan untuk menentukan aktivitas antioksidan dan mengidentifikasi senyawa golongan flavonoid yang terkandung dalam ekstrak etil asetat daun pranajiwa (Euchresta horsfieldii Lesch Benn.). Uji aktivitas antioksidan dilakukan secara invitro dengan metode DPPH (1,1-diphenyl-2-pycrylhidrazyl). Teknik pemisahan dilakukan dengan kromatografi kolom dan diidentifikasi dengan spektrofotometer FTIR dan UV-Vis. Hasil penelitian menunjukkan bahwa ekstrak etil asetat memiliki aktivitas antioksidan dengan nilai IC50 sebesar 393,95 µg/mL dan kadar total flavonoid sebesar 6619,72 mg QE/100g atau 6,62 % QE. Pemisahan dan pemurnian ekstrak etil asetat menggunakan fase diam silika gel 60 dan fase gerak n-heksana:kloroform: etanol (20:1:1) yang menghasilkan isolat aktif yang positif flavonoid (isolat FE) yang diduga merupakan senyawa flavonoid golongan flavonol yaitu 3,5,7,3’,4’-pentahidroksi flavonol.   ABSTRACT: The present study was conducted to determine antioxidant activity and to identify the flavonoid active compounds from ethyl acetate extracts of Pranajiwa leaves. In vitro antioxidant activity was carried out using DPPH (1,1-diphenyl-2-pycrylhidrazyl) method. The separation of the ethyl acetate extracts was conducted by column chromatography and the identification by using FTIR and UV-Vis spectrophotometer. The results showed that ethyl acetate extract has antioxidant activity with IC50 value of 393,95 µg/mL and the total flavonoid of 6619,72 mg QE /100g or 6,62% QE. The separation and purification of  ethyl acetate extract was chromatography column on silica gel 60 and the solvent n-hexane:chloroform:ethanol (20:1:1) based on UV-Vis and Infrared spectra positive flavonoid isolate (isolates FE) was tentaviely identified as 3,5,7,3',4'-pentadihydroxy flavonols.    


2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Rotimi Larayetan ◽  
Zacchaeus S. Ololade ◽  
Oluranti O. Ogunmola ◽  
Ayodele Ladokun

Plants are reservoir for potentially useful bioactive compounds, and owing to the rising occurrences of drug resistance to malaria parasites, there is a need to discover and develop new phytochemicals in plant that can be used as antimalarial agents. In this study, we gave a detailed description of the phytochemicals present in both ethyl acetate and methanolic extracts of Callistemon citrinus (C. citrinus) using Gas Chromatography-Mass Spectrometry (GC-MS) analysis; both extracts were also evaluated for their in vitro antimalarial, antitrypanosomal, and cytotoxicity activities against Trypanosoma brucei brucei (T. b brucei) parasites, Plasmodium falciparum (P. falciparum) malaria parasites 3D7 strain, and human cervix adenocarcinoma cells (HeLa cells); in addition, the antimicrobial and antioxidant efficacies were determined using standard methods. Both extracts were characterized by a high amount of fatty acids (52.88 and 62.48%). The ethyl acetate extract exhibited a greater activity with minimum inhibitory concentration (MIC) values ranging from 0.025 to 0.10 mg/mL while the methanol extract ranged from 0.025 to 0.15 mg/mL. Both extracts were bactericidal to Escherichia coli ATCC 35150 (E. coli) and Pseudomonas aeruginosa ACC (P. aeruginosa). Qualitative and quantitative phytochemical screenings conducted for both extracts revealed the presence of alkaloids, glycosides, saponins, steroids, and triterpenoids, fat and oils, flavonoids, phenols, and tannins in varying amounts. Both crude extracts exhibited antitrypanosomal potentials with an IC50 of 6.6/9.7 μg/mL and antiplasmodial activities with an IC50 of 8.4/13.0 μg/mL. Conclusion from this study indicates that apart from the folkloric uses of this plant in traditional settings, the extracts possess a broad spectrum of antimicrobial, antitrypanosomal, and antimalarial activities and some pharmaceutically essential bioactive components with remarkable antioxidant capacities that may be used in the synthesis of novel drugs for the management of different varieties of ailments.


Sign in / Sign up

Export Citation Format

Share Document