Computational and biological efficacy of stigmasterol against HeLa cells and Vero cells- first time isolated from the ethanolic extract of Annonamuricata Linn leaves

The species Inga laurina is native to the Brazilian Cerrado. There are no studies about the chemical composition and biological activities of extracts of this endangered species. The ethanolic extract and its successive fractions are rich in phenolic compounds and presented good antifungal activities. HPLC/MS-MS/MS and H1/C13 analysis led to the identification of seventeen compounds, most of which are gallic acid derivatives, myricetin and quercetin glycosides. The ethyl acetate fraction (EAF) contained high levels of total phenolics, expressed in milligrams of gallic acid equivalents per gram of extract (475.3 ± 1.9 mg GAE gextract-1) and flavonoids expressed in milligrams of quercetin equivalents per gram of extract (359.3 ± 10.6 mg QE gextract-1). This fraction was active against fungi of the Candida genus. The EAF showed MIC value 11.7 μg mL−1 against C. glabrata and a selectivity index of 1.6 against Vero cells. The flavonol glycoside myricetin-3-O-rhamnoside was isolated for the first time from the Inga laurina. These results make I. laurina a promising plant as a source of pharmaceutical and biological active antifungal compounds.

Download Full-text

Heartwood of Secang (CAESALPINIA SAPPAN L.) Ethanolic Extract Show Selective Cytotoxic Activities on T47D and Widr Cells But Not on Hela Cells

Indonesian Journal of Cancer Chemoprevention ◽

10.14499/indonesianjcanchemoprev7iss2pp60-67 ◽

2017 ◽

Vol 7 (2) ◽

pp. 60

Author(s):

Erlina Rivanti ◽

Bani Adlina Shabrina ◽

Ika Nurzijah ◽

Cyndwika Ayu ◽

Adam Hermawan

Keyword(s):

Cancer Cells ◽

Hela Cells ◽

Breast Cancer Cells ◽

Ethanolic Extract ◽

Vero Cells ◽

Cytotoxic Activities ◽

Colon Cancer Cells ◽

Caesalpinia Sappan ◽

Ic50 Value ◽

Cervical Cancer Cells

The present study investigate the selectivity of heartwood of secang ethanolic extract (SEE) on T47D breast cancer cells, WiDr colon cancer cells, and HeLa cervical cancer cells, compared to Vero normal epithelial cells. The cytotoxic effect was evaluated by using MTT assay with 24-hour treatment to get IC50values. Selectivity was evaluated by using selectivity index (SI). SEE had a potent cytotoxic activity on T47D and WiDr cancer cells (IC50 <100 µg/ml). IC50 value of HeLa cancer cells was observed on moderate cytotoxic (100 <IC50 <1000 µg/ml). SEE demonstrated more selective to T47D and WiDr than Vero cells (SI > 3), while in HeLa cells is not selective (SI < 3). This result indicating its potential of Caesalpinia sappan as a chemopreventive agent in cancer therapy.Keywords: Cancer, selectivity, Secang, T47D, WiDr, HeLa, Vero

Download Full-text

Sequestration of Stigmasterol and β-Sitosterol from Ethanolic Extract of Kam Sabut (Croton caudatus Geiseler) Leaves

Asian Journal of Chemistry ◽

10.14233/ajchem.2021.23426 ◽

2021 ◽

Vol 33 (11) ◽

pp. 2851-2856

Author(s):

Longjam Shantabi ◽

Ganesh Chandra Jagetia ◽

Sharubam Victoria Devi ◽

H. Lalhenmawia ◽

Raghuvir H. Gaonkar

Keyword(s):

Anticancer Activity ◽

Mass Spectroscopy ◽

Column Chromatography ◽

Hela Cells ◽

Ethanolic Extract ◽

Reverse Phase Hplc ◽

Reverse Phase ◽

Northeastern India ◽

First Time

Croton caudatus (Kam sabut) has been traditionally used to treat cancer in northeastern India and earlier studies reported the anticancer activity of ethanolic extract of C. caudatus leaves in HeLa cells in vitro and Swiss albino mice transplanted with Dalton’s ascites lymphoma. Therefore, isolation of stigmasterol and β-sitosterol from the ethanolic extract of C. caudatus Geiseler leaves was carried out. Stigmasterol and β-sitosterol were isolated from the ethanolic extract of dried leaves of C. caudatus by column chromatography. The fractions were purified further on Sephadex® LH-20 column chromatography and reverse-phase HPLC. The isolated phytosterols were characterized and quantified by IR, 1H & 13 CNMR, mass spectroscopy and HPLC. This has led to the separation of 100 mg stigmasterol and 80 mg β-sitosterol. Stigmasterol and β-sitosterol have been isolated from the ethanolic extract of C. caudatus leaves for the first time.

Download Full-text

Bufadienolides from the Skin Secretions of the Neotropical Toad Rhinella alata (Anura: Bufonidae): Antiprotozoal Activity against Trypanosoma cruzi

Molecules ◽

10.3390/molecules26144217 ◽

2021 ◽

Vol 26 (14) ◽

pp. 4217

Author(s):

Candelario Rodriguez ◽

Roberto Ibáñez ◽

Luis Mojica ◽

Michelle Ng ◽

Carmenza Spadafora ◽

...

Keyword(s):

Vero Cells ◽

Chemical Diversity ◽

Hydroxyl Group ◽

Antitrypanosomal Activity ◽

The Family ◽

Toad Venom ◽

Skin Secretions ◽

Pharmacological Potential ◽

First Time ◽

Mcf 7

Toads in the family Bufonidae contain bufadienolides in their venom, which are characterized by their chemical diversity and high pharmacological potential. American trypanosomiasis is a neglected disease that affects an estimated 8 million people in tropical and subtropical countries. In this research, we investigated the chemical composition and antitrypanosomal activity of toad venom from Rhinella alata collected in Panama. Structural determination using mass spectrometry (MS) and nuclear magnetic resonance (NMR) spectroscopy led to the identification of 10 bufadienolides. Compounds identified include the following: 16β-hydroxy-desacetyl-bufotalin-3-adipoyl-arginine ester (1), bufotalin (2), 16β-hydroxy-desacetyl-bufotalin-3-pimeloyl-arginine ester (3), bufotalin-3-pimeloyl-arginine ester (4), 16β-hydroxy-desacetyl-bufotalin-3-suberoyl-arginine ester (5), bufotalin-3-suberoyl-arginine ester (6), cinobufagin-3-adipoyl-arginine ester (7), cinobufagin-3-pimeloyl-arginine ester (8), cinobufagin-3-suberoyl-arginine ester (9), and cinobufagin (10). Among these, three new natural products, 1, 3, and 5, are described, and compounds 1–10 are reported for the first time in R. alata. The antitrypanosomal activity assessed in this study revealed that the presence of an arginyl-diacid attached to C-3, and a hydroxyl group at C-14 in the structure of bufadienolides that is important for their biological activity. Bufadienolides showed cytotoxic activity against epithelial kidney Vero cells; however, bufagins (2 and 10) displayed low mammalian cytotoxicity. Compounds 2 and 10 showed activity against the cancer cell lines MCF-7, NCI-H460, and SF-268.

Download Full-text

Constituents of Chamaecrista diphylla (L.) Greene Leaves with Potent Antioxidant Capacity: A Feature-Based Molecular Network Dereplication Approach

Pharmaceutics ◽

10.3390/pharmaceutics13050681 ◽

2021 ◽

Vol 13 (5) ◽

pp. 681

Author(s):

Paulo Gomes ◽

Luis Quirós-Guerrero ◽

Abraão Muribeca ◽

José Reis ◽

Sônia Pamplona ◽

...

Keyword(s):

Antioxidant Capacity ◽

Ethanolic Extract ◽

Oxygen Radical ◽

Molecular Network ◽

Antioxidant Compounds ◽

Herbaceous Plant ◽

Network Approach ◽

Feature Based ◽

Promising Source ◽

First Time

Chamaecrista diphylla (L.) Greene (Fabaceae/Caesalpiniaceae) is a herbaceous plant that is widely distributed throughout the Americas. Plants from this genus have been used in traditional medicine as a laxative, to heal wounds, and to treat ulcers, snake and scorpion bites. In the present study, we investigated the chemical composition of Chamaecrista diphylla leaves through a mass spectrometry molecular network approach. The oxygen radical absorbance capacity (ORAC) for the ethanolic extract, enriched fractions and isolated compounds was assessed. Overall, thirty-five compounds were annotated for the first time in C. diphylla. Thirty-two of them were reported for the first time in the genus. The isolated compounds 9, 12, 24 and 33 showed an excellent antioxidant capacity, superior to the extract and enriched fractions. Bond dissociation energy calculations were performed to explain and sustain the antioxidant capacity found. According to our results, the leaves of C. diphylla represent a promising source of potent antioxidant compounds.

Download Full-text

PHYTOCHEMICAL CONSTITUENTS OF THE ROOT OF BERBERIS MICROPHYLLA

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i6.17803 ◽

2017 ◽

Vol 10 (6) ◽

pp. 225 ◽

Cited By ~ 1

Author(s):

María Cristina Furrianca ◽

Marysol Alvear ◽

Tomás Zambrano ◽

Víctor Fajardo ◽

Luis Salazar

Keyword(s):

Secondary Metabolites ◽

Cardiac Glycosides ◽

Methanolic Extract ◽

Ethanolic Extract ◽

Phytochemical Screening ◽

Qualitative And Quantitative ◽

Medicinal Properties ◽

Phytochemical Constituents ◽

First Time

Objective: To objective of this work was to perform phytochemical qualitative and quantitative analyzes of the main secondary metabolites in the root of Berberis microphylla.Methods: The extracts of B. microphylla root were tested through phytochemical screening and the quantification of the most important constituents was carried out using spectrophotometric and gravimetric techniques.Results: Phytochemical screening of both extracts showed the presence of alkaloids, flavonoids, glycosides, cardiac glycosides, saponins, terpenes,and tannins, which are pharmacologically important. Quantification of the major phytochemicals groups showed that the ethanolic extract contains 3.9% alkaloids, 0.46% flavonoids, 9.53% tannins, and 3.60% saponins. Similarly, the methanolic extract contains 6.61% alkaloids, 0.41% flavonoids, 7.40% tannins, and 1.43% saponins.Conclusion: This is the first time that the presence of tannins, flavonoids, and saponins in this plant has been reported. The medicinal properties of the root of B. microphylla may exist due to the presence secondary metabolites.

Download Full-text

Eﬀect of Zinc(II)-2,4,5-triphenyl-1H-imidazole Complex Against Replication DENV-2 in Vero Cell

Indonesian Journal of Tropical and Infectious Disease ◽

10.20473/ijtid.v8i3.11776 ◽

2020 ◽

Vol 8 (3) ◽

pp. 183

Author(s):

Teguh Hari Sucipto ◽

Aswandi Wibrianto ◽

Fahimah Martak ◽

Siti Churrotin ◽

Ilham Harlan Amarullah ◽

...

Keyword(s):

Dengue Virus ◽

Vero Cell ◽

Complex Compound ◽

Inhibitory Activity ◽

Vero Cells ◽

Inhibitory Effect ◽

Complex Compounds ◽

Antiviral Compound ◽

First Time

Dengue virus (DENV) is a significant pathogen emerging worldwide as a cause of infectious disease. DENVs are transmitted to humans through female mosquitoes from Aedes aegypti and Aedes albopictus species. Indonesia is one of the largest countries in the world in dengue endemic regions worldwide. Dengue fever was occurred for the first time as an outbreak in Surabaya and Jakarta in 1968. Many eﬀorts have been made to prevent and treat DENV infections, and clinical trials of a number of vaccines are currently underway. Antiviral testing of DENV is an important alternative for drug characterization and development. Complex compounds are formed as a result of metal and organic complex reactions. Complex compounds can be used as an anti-inflammatory, antimicrobial antifungal, antibacterial, antivirus. The Zn2+ ion can be used as an antiviral candidate. The purpose of this project was investigated Zinc(II)-2,4,5-triphenyl-1H-imidazole antiviral compound to be further tested for inhibitory eﬀect on the replication of DENV-2 in cell culture. DENV replication was measured by antiviral activity assay and cytotoxicity assay. The inhibitory activity of Zinc(II)-2,4,5-triphenyl-1H-imidazole complex compound was determined by Viral ToxGloTM Assay. The cytotoxicity of Zinc(II)-2,4,5-triphenyl-1H-imidazole complex compound was determined by CellTiter96® AQuoeus assay. The inhibitory concentration (IC50) of Zinc(II)-2,4,5-triphenyl- 1H-imidazole against dengue virus type-2 was 34.42 μg/ml. The cytotoxic concentration (CC50) of compound against Vero cell was <100 μg/ml. The results of this study demonstrate the antidengue serotype 2 inhibitory activity of investigated Zinc(II)-2,4,5-triphenyl-1H-imidazole complex and its high toxicity in Vero cells. Further studies are not required before investigated Zinc(II)-2,4,5-triphenylimidazole can be applied in the treatment of DENV-2 infections

Download Full-text

GC-MS Chemical Characterization of Main Components of Smilax Domingensis Wild. in Cuba

Journal of Agricultural Studies ◽

10.5296/jas.v6i2.13099 ◽

2018 ◽

Vol 5 (4) ◽

pp. 79 ◽

Cited By ~ 1

Author(s):

Pilar A. Soledispa ◽

José González ◽

Armando Cuéllar ◽

Julio Pérez ◽

Max Monan

Keyword(s):

Mass Spectra ◽

Chemical Constituents ◽

Chemical Characterization ◽

Ethanolic Extract ◽

Chemical Compounds ◽

Chemical Components ◽

Analytical Technique ◽

Main Components ◽

First Time

A preliminary chemical characterization of main components of ethanolic extract with dried rhizomes of Smilax domingensis Wid. that grow in Cuba was done using a GCMS-QP2010 Ultra Shimadzu and the mass spectra of the compounds found in the extract was matched with the National Institute of Standards and Technology (NIST) library. After sample derivatization 125 chemical compounds were registered by the equipment and from them, 35 different chemical components were characterized and reported for the first time from this part of the plant in our country. The results demonstrate the developed method could be employed as a rapid and versatile analytical technique for identification of chemical constituents and quality control of Smilax domingensis.

Download Full-text

Flavonoids from Milletia leucantha and Their Cytotoxicity

Natural Product Communications ◽

10.1177/1934578x1801300810 ◽

2018 ◽

Vol 13 (8) ◽

pp. 1934578X1801300

Author(s):

Uraiwan Sriphana ◽

Chavi Yenjai ◽

Siriporn Tungnoi ◽

Jongjai Srirapa ◽

Auemporn Junsongduang

Keyword(s):

Cytotoxic Activity ◽

Vero Cell ◽

Cell Line ◽

Vero Cells ◽

2D Nmr ◽

Nmr Techniques ◽

Vero Cell Lines ◽

First Time ◽

Flavonol Derivatives ◽

Mcf 7

Two known chalcones (1–2), five known flavonol derivatives (3 and 5–8) and one flavone (4) were isolated for the first time from fruits of Millettia leucantha Kurz. In addition, 5 was found for the first time from this genus. Their structures were elucidated on the basis of IR, MS, 1D and 2D NMR techniques. Chalcone 1 exhibited moderate cytotoxicity against the MCF-7 cell line with an IC50 value of 50.93 μM, whereas this compound showed inactive cytotoxicity against Vero cells. Compound 2 exhibited cytotoxicity against the KB, NCI-H187 and Vero cell lines with IC50 values of 63.64, 114.44 and 28.44 μM, respectively. Compound 8 only showed cytotoxic activity against the KB cell line with an IC50 value of 110.23 μM.

Download Full-text

Fluctuation in radioresponse of HeLa cells during the cell cycle evaluated based on micronucleus frequency

Scientific Reports ◽

10.1038/s41598-020-77969-0 ◽

2020 ◽

Vol 10 (1) ◽

Author(s):

Hiroaki Shimono ◽

Atsushi Kaida ◽

Hisao Homma ◽

Hitomi Nojima ◽

Yusuke Onozato ◽

...

Keyword(s):

Cell Cycle ◽

Hela Cells ◽

Time Lapse ◽

S Phase ◽

G1 Phase ◽

M Phase ◽

G2 Phase ◽

The Difference ◽

Time Lapse Imaging ◽

First Time

AbstractIn this study, we examined the fluctuation in radioresponse of HeLa cells during the cell cycle. For this purpose, we used HeLa cells expressing two types of fluorescent ubiquitination-based cell cycle indicators (Fucci), HeLa-Fucci (CA)2 and HeLa-Fucci (SA), and combined this approach with the micronucleus (MN) assay to assess radioresponse. The Fucci system distinguishes cell cycle phases based on the colour of fluorescence and cell morphology under live conditions. Time-lapse imaging allowed us to further identify sub-positions within the G1 and S phases at the time of irradiation by two independent means, and to quantitate the number of MNs by following each cell through M phase until the next G1 phase. Notably, we found that radioresponse was low in late G1 phase, but rapidly increased in early S phase. It then decreased until late S phase and increased in G2 phase. For the first time, we demonstrated the unique fluctuation of radioresponse by the MN assay during the cell cycle in HeLa cells. We discuss the difference between previous clonogenic experiments using M phase-synchronised cell populations and ours, as well as the clinical implications of the present findings.

Download Full-text