New Adenosine Derivatives from Aizoon canariense L.: In Vitro Anticholinesterase, Antimicrobial, and Cytotoxic Evaluation of Its Extracts

Aizoaceae is a large succulent family characterized by many psychoactive species. Aizoon canariense L., a wild neglected plant traditionally used in gastrointestinal ailments, has been the subject of a limited number of phytochemical and biological studies. Therefore, herein, we investigated the in vitro cytotoxic, antimicrobial, and anticholinesteraseactivity of the aerial parts of A. canariense L. and analyzed the phytochemical compositions of the lipoidal and alkaloidal fractions. Petroleum ether extract showed the presence of behenic and tricosylic acid, while an in-depth investigation of the alkaloidal fraction revealed the identification of new adenine based alkaloids (1–5), which were isolated and identified for the first time from Aizoon canariense L. Their structures were elucidated based on extensive spectroscopic analyses. The alkaloidal extract showed a powerful cytotoxic effect (IC50 14–28 μg/mL), with the best effect against colon carcinoma, followed by liver and breast carcinomas. The alkaloidal extract also had a potent effect against Candida albicans and Escherichia coli, with minimum inhibitory concentrations (MIC) values of 312.5 and 625 µg/mL. The in vitro anticholinesterase activity was potent, with IC50 < 200 ng/mL for the tested extracts compared with 27.29 ± 0.49 ng/mL for tacrine.

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α-Glucosidase Inhibition and Docking Studies of 5-Deoxyflavonols and Dihydroflavonols Isolated from Abutilon pakistanicum

Current Organic Chemistry ◽

10.2174/1385272823666191001224741 ◽

2019 ◽

Vol 23 (17) ◽

pp. 1857-1866

Author(s):

Munawar Hussain ◽

Zaheer Ahmed ◽

Shamsun N. Khan ◽

Syed A. A. Shah ◽

Rizwana Razi ◽

...

Keyword(s):

Methanolic Extract ◽

Docking Studies ◽

Hydroxyl Group ◽

Coumaric Acid ◽

In Vitro Activity ◽

Aerial Parts ◽

First Time ◽

Acid Esters ◽

Phenol Moiety

Three new 5-deoxyflavonoid and dihydroflavonoids 2, 3 and 4 have been isolated from the methanolic extract of Abutioln pakistanicum aerial parts, for which structures were elucidated explicitly by extensive MS- and NMR-experiments. In addition to these, 3,7,4′-trihydroxy-3′-methoxy flavonol (1) is reported for the first time from Abutioln pakistanicum. Compound 2 and 4 are p-coumaric acid esters while compounds 2–4 exhibited α-glucosidase inhibitory activity. Docking studies indicated that the ability of flavonoids 2, 3 and 4 to form multiple hydrogen bonds with catalytically important residues is decisive hence is responsible for the inhibition activity. The docking results signified the observed in-vitro activity quite well which is in accordance with previously obtained conclusion that phenol moiety and hydroxyl group are critical for the inhibition of α-glucosidase enzyme.

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Six New 3,5-Dimethylcoumarins from Chelonopsis praecox, Chelonopsis odontochila and Chelonopsis pseudobracteata

Natural Products and Bioprospecting ◽

10.1007/s13659-021-00318-9 ◽

2021 ◽

Author(s):

Chang-An Geng ◽

Zhen-Tao Deng ◽

Qian Huang ◽

Chun-Lei Xiang ◽

Ji-Jun Chen

Keyword(s):

Protein Tyrosine Phosphatase ◽

Tyrosine Phosphatase ◽

2D Nmr ◽

Cell Protein ◽

Protein Tyrosine Phosphatase 1B ◽

Protein Tyrosine ◽

Aerial Parts ◽

Spectroscopic Analyses ◽

New Compounds

AbstractTen 3,5-dimethylcoumarins (1–6 and 8‒11) involving six new ones (1–6), together with a known 3-methylcoumarin (7), were isolated from the aerial parts of three Chelonopsis plants, C. praecox, C. odontochila, and C. pseudobracteata. The structures of the new compounds were determined by extensive HRESIMS, 1D and 2D NMR spectroscopic analyses. According to the substitution at C-5, these coumarins were classified into 5-methyl, 5-hydroxymethyl, 5-formyl, and 5-nor types. All the isolates were assayed for their inhibition on α-glucosidase, protein tyrosine phosphatase 1B, and T-cell protein tyrosine phosphatase in vitro. Graphic Abstract

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GC-MS Investigation of Amaryllidaceae Alkaloids in Galanthus xvalentinei nothosubsp. subplicatus

Natural Product Communications ◽

10.1177/1934578x1300800312 ◽

2013 ◽

Vol 8 (3) ◽

pp. 1934578X1300800

Author(s):

Buket Bozkurt Sarikaya ◽

Strahil Berkov ◽

Jaume Bastida ◽

Gulen Irem Kaya ◽

Mustafa Ali Onur ◽

...

Keyword(s):

Inhibitory Activity ◽

Anticholinesterase Activity ◽

Amaryllidaceae Alkaloids ◽

Acetylcholinesterase Inhibitory Activity ◽

Aerial Parts ◽

Ms Analysis ◽

Ellman’S Method ◽

First Time

A GC-MS analysis of alkaloids in the aerial parts and bulbs of Galanthus x valentinei nothosubsp. subplicatus was performed for the first time. Totally, twenty-six alkaloids were identified, of which tazettine and galanthindole were the major ones. Acetylcholinesterase inhibitory activity of the alkaloidal extracts was determined using modified in vitro Ellman's method. Significant anticholinesterase activity was observed in the tested samples (bulbs: IC50 = 21.3 μg/mL, aerial parts: IC50 = 16.3 μg/mL).

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In Vitro Bioactivity of Methanolic Extracts from Amphipterygium adstringens (Schltdl.) Schiede ex Standl., Chenopodium ambrosioides L., Cirsium mexicanum DC., Eryngium carlinae F. Delaroche, and Pithecellobium dulce (Roxb.) Benth. Used in Traditional Medicine in Mexico

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2018/3610364 ◽

2018 ◽

Vol 2018 ◽

pp. 1-11

Author(s):

Peter Knauth ◽

Gustavo J. Acevedo-Hernández ◽

M. Eduardo Cano ◽

Melesio Gutiérrez-Lomelí ◽

Zaira López

Keyword(s):

Bark Extract ◽

Phytochemical Analysis ◽

Potential Candidate ◽

Chenopodium Ambrosioides ◽

Bacterial Strains ◽

Fruit Extract ◽

Methanolic Extracts ◽

Biological Studies ◽

First Time

Seven out of eight methanolic extracts from five plants native to Mexico were inactive against ten bacterial strains of clinical interest. The fruit extract of Chenopodium ambrosioides inhibited the bacteria Enterococcus faecalis (MIC = 4375 μg/ml), Escherichia coli (MIC = 1094 μg/ml), and Salmonella typhimurium (MIC = 137 μg/ml). The fruit extract of C. ambrosioides was with CC50 = 45 μg/ml most cytotoxic against the cell-line Caco-2, followed by the leaf extract from Pithecellobium dulce (CC50 = 126 μg/ml); interestingly, leaves of C. ambrosioides (CC50 = 563 μg/ml) and bark of P. dulce (CC50 = 347 μg/ml) extracts were much less cytotoxic. We describe for the first time the cytotoxic effect from extracts of the aerial parts and the flowers of Cirsium mexicanum (CC50 = 323 μg/ml and CC50 = 250 μg/ml, resp.). Phytochemical analysis demonstrated for both extracts high tannin and saponin and low flavonoid content, while terpenoids were found in the flowers. For the first time we report a cytotoxicological study on an extract of Eryngium carlinae (CC50 = 356 μg/ml) and likewise the bark extract from Amphipterygium adstringens (CC50 = 342 μg/ml). In conclusion the fruit extract of C. ambrosioides is a potential candidate for further biological studies.

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Chemical Constituents From the Aerial Part of Tiliacora triandra (Colebr.) Diels and Their α-Glucosidase and α-Amylase Inhibitory Activity

Natural Product Communications ◽

10.1177/1934578x19899595 ◽

2020 ◽

Vol 15 (1) ◽

pp. 1934578X1989959

Author(s):

Emmanuel Ayobami Makinde ◽

Chitchamai Ovatlarnporn ◽

Chonlatid Sontimuang ◽

Gaëtan Herbette ◽

Opeyemi Joshua Olatunji

Keyword(s):

Inhibitory Activity ◽

Chemical Constituents ◽

Ethyl Linoleate ◽

Resonance Spectroscopy ◽

Ionization Mass ◽

Pheophorbide A ◽

Aerial Parts ◽

Fatty Acid Derivatives ◽

First Time

Two new fatty acid derivatives identified as 5,7-dihydroxy-6-oxoheptadecanoic acid (1) and ethyl-5,7-dihydroxy-6-oxooctadecanoate (2) together with four known compounds, ethyl linolenate (3), ethyl linoleate (4), ethyl pheophorbide A (5), and pheophorbide A (6), were isolated from the aerial parts of Tiliacora triandra. All the compounds were isolated from T. triandra for the first time. The structures of the compounds were elucidated using high-resolution electrospray ionization mass spectrometry, 1-dimensional and 2-dimensional nuclear magnetic resonance spectroscopy, and comparison with literature data. All the isolated compounds were evaluated for their in vitro inhibitory activity against α-glucosidase and α-amylase. Compounds 1-6 exhibited α-glucosidase inhibitory activity with half-maximal inhibitory concentration values (IC50) values in the range of 11.58-424.06 μM, while only compound 1 displayed inhibitory activity against α-amylase at an IC50 value of 26.27 μM.

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UPLC-ESI-MS/MS Profile and Antioxidant, Cytotoxic, Antidiabetic, and Antiobesity Activities of the Aqueous Extracts of Three Different Hibiscus Species

Journal of Chemistry ◽

10.1155/2020/6749176 ◽

2020 ◽

Vol 2020 ◽

pp. 1-17

Author(s):

Hanan M. Al-Yousef ◽

Wafaa H. B. Hassan ◽

Sahar Abdelaziz ◽

Musarat Amina ◽

Rasha Adel ◽

...

Keyword(s):

Cytotoxic Activity ◽

Aqueous Extract ◽

Biological Activities ◽

Biological Effects ◽

Aqueous Extracts ◽

Potent Effect ◽

Esi Ms ◽

Biological Studies ◽

Hct 116

The aqueous extracts of Hibiscus calyphyllus (HcA), Hibiscus micranthus (HmA), and Hibiscus deflersii (HdA) growing in Saudi Arabia did not receive enough attention in phytochemical and biological studies. This inspired the authors to investigate the phytochemicals of these extracts for the first time using UPLC-ESI-MS/MS in negative and positive ionization modes. The analysis afforded the tentative identification of 103 compounds including phenolic compounds, flavonoids, and anthocyanins. Moreover, in vitro evaluations of their cytotoxic, antioxidant, antidiabetic, and antiobesity activities were carried out. The results showed that aqueous extract of Hibiscus calyphyllus had the highest activity as an antioxidant agent (SC50 = 111 ± 1.5 μg/mL) compared with ascorbic acid (SC50 = 14.2 ± 0.5 μg/mL). MTT assay was used to evaluate cytotoxic activity compared to cisplatin. Hibiscus deflersii showed the most potent cytotoxic effect against A-549 (human lung carcinoma) with IC50 = 50 ± 5.1 μg/mL, and Hibiscus micranthus showed a close effect with IC50 = 60.4 ± 1.7 μg/mL. Hibiscus micranthus showed the most potent effect on HCT-116 (human colon carcinoma) with IC50 = 56 ± 1.9 μg/mL compared with cisplatin (IC50 = 7.53 ± 3.8 μg/mL). HcA and HdA extracts showed weak cytotoxic activity against A-549 and HCT-116 cell lines compared to the other extracts. Eventually, Hibiscus deflersii showed astonishing antidiabetic (IC50 = 56 ± 1.9 μg/mL) and antiobesity (IC50 = 95.45 ± 1.9 μg/mL) activities using in vitro α-amylase inhibitory assay (compared with acarbose (IC50 = 34.71 ± 0.7 μg/mL)) and pancreatic lipase inhibitory assay (compared with orlistat (IC50 = 23.8 ± 0.7 μg/mL)), respectively. In conclusion, these findings are regarded as the first vision of the phytochemical constituents and biological activities of different Hibiscus aqueous extracts. Hibiscus deflersii aqueous extract might be a hopeful origin of functional constituents with anticancer (on A-549 cell line), antidiabetic, and antiobesity activities. It might be a natural alternative remedy and nutritional policy for diabetes and obesity treatment without negative side effects. Isolation of the bioactive phytochemicals from the aqueous extracts of aerial parts of Hibiscus calyphyllus, Hibiscus micranthus, and Hibiscus deflersii and estimation of their biological effects are recommended in further studies.

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Sugar Containing Compounds and Biological Activities of Lagochilus setulosus

Molecules ◽

10.3390/molecules26061755 ◽

2021 ◽

Vol 26 (6) ◽

pp. 1755

Author(s):

Davlat Kh. Akramov ◽

Nilufar Z. Mamadalieva ◽

Andrea Porzel ◽

Hidayat Hussain ◽

Mthandazo Dube ◽

...

Keyword(s):

Methanolic Extract ◽

Biological Activities ◽

2D Nmr ◽

Septoria Tritici ◽

2D Nmr Spectroscopy ◽

Aerial Parts ◽

Spectroscopic Analyses ◽

Phytochemical Investigation ◽

Diphenyl Tetrazolium Bromide

Phytochemical investigation of the methanolic extract obtained from the aerial parts of Lagochilus setulosus (Lamiaceae) afforded the new compound 1-methoxy-3-O-β-glucopyranosyl-α-l-oliose (1) together with five known glycosides, namely sitosterol-3-O-β-glucoside (2), stigmasterol-3-O-β-glucoside (3), pinitol (4), 6β-hydroxyl-7-epi-loganin (5), and chlorotuberoside (6). The structures of these compounds were elucidated by extensive spectroscopic analyses, especially HR-MS, 1D and 2D NMR spectroscopy. The in vitro cytotoxic activity of the methanolic extract and the isolated compounds was assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and crystal violet (CV) staining assays. In addition, the antifungal activities of the components were evaluated against Botrytis cinerea, Septoria tritici, and Phytophthora infestans. The anthelmintic potential was determined against Caenorhabditis elegans nematodes. Neither the extract nor the isolated compounds showed promising activity in all the bioassays.

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Feline Morbillivirus Infection in Domestic Cats: What Have We Learned So Far?

Viruses ◽

10.3390/v13040683 ◽

2021 ◽

Vol 13 (4) ◽

pp. 683

Author(s):

Eliana De Luca ◽

Giuseppe Andrea Sautto ◽

Paolo Emidio Crisi ◽

Alessio Lorusso

Keyword(s):

Current Knowledge ◽

Domestic Cats ◽

Stray Cats ◽

Potential Association ◽

Clinicopathological Findings ◽

A Cell ◽

The Subject ◽

First Time

Feline morbillivirus (FeMV) was identified for the first time in stray cats in 2012 in Hong Kong and, since its discovery, it was reported in domestic cats worldwide. Although a potential association between FeMV infection and tubulointerstitial nephritis (TIN) has been suggested, this has not been proven, and the subject remains controversial. TIN is the most frequent histopathological finding in the context of feline chronic kidney disease (CKD), which is one of the major clinical pathologies in feline medicine. FeMV research has mainly focused on defining the epidemiology, the role of FeMV in the development of CKD, and its in vitro tropism, but the pathogenicity of FeMV is still not clear, partly due to its distinctive biological characteristics, as well as to a lack of a cell culture system for its rapid isolation. In this review, we summarize the current knowledge of FeMV infection, including genetic diversity of FeMV strains, epidemiology, pathogenicity, and clinicopathological findings observed in naturally infected cats.

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Relationship between Dyskerin Expression and Telomerase Activity in Human Breast Cancer

Analytical Cellular Pathology ◽

10.1155/2008/830562 ◽

2008 ◽

Vol 30 (6) ◽

pp. 483-490

Author(s):

Lorenzo Montanaro ◽

Maria Calienni ◽

Claudio Ceccarelli ◽

Donatella Santini ◽

Mario Taffurelli ◽

...

Keyword(s):

Ribosome Biogenesis ◽

Telomerase Activity ◽

Breast Carcinomas ◽

Over Expression ◽

Small Nuclear Rnas ◽

Tumour Pathology ◽

First Time ◽

The Relationship ◽

Tert Expression

The nucleolar protein dyskerin is involved in the modification of specific uridine residues to pseudouridine on ribosomal and small nuclear RNAs and in the stabilization of the telomerase RNA component (TERC). In this study we investigated for the first time the relationship between dyskerin expression and telomerase activity in a series of 61 primary breast carcinomas. We found that when dyskerin mRNA values were very low the telomerase activity was markedly reduced, independently of the expression of other important components of the telomerase complex such as telomerase reverse transcriptase (TERT). In vitro experiments showed that reduction of dyskerin expression affect telomerase activity through the reduction of TERC. Only when TERC levels were strongly reduced telomerase activity was hindered. Retroviral mediated over-expression of TERC abolished the telomerase impairment due to dyskerin knock down. In conclusion, our results indicated that, beside its effect on ribosome biogenesis, the levels of dyskerin in cancer cells modulate telomerase activity through the regulation of TERC levels, independently of TERT expression. This should be taken into consideration when utilizing TERT expression as a surrogate indicator of telomerase activity in tumour pathology.

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Comparative Antimicrobial Study of Different Parts of Ocimum americanum L., O. basilicum L. and O. sanctum L. in Comparison to Standard Antibiotics Collected from Dibrugarh, Assam

Journal of Scientific Research ◽

10.3329/jsr.v13i1.47322 ◽

2021 ◽

Vol 13 (1) ◽

pp. 195-208

Author(s):

J. Chetia ◽

L. R. Saikia ◽

S. Upadhyaya ◽

E. Khatiwora ◽

A. Bawri

Keyword(s):

Petroleum Ether Extract ◽

Ether Extract ◽

E Coli ◽

Aerial Parts ◽

Whole Plant ◽

Young Leaves ◽

Antibacterial And Antifungal ◽

Different Parts ◽

Ocimum Americanum

Lamiaceae members are commonly used in ethno-medicinal practices of our country. The in vitro antibacterial and antifungal activity of various solvents extracts of different aerial parts of Ocimum americanum L., O. basilicum L. and O. sanctum L. wereassessed on standard bacterial and fungal strains using standard laboratory methods. Extracts from O. americanum have inhibitory activity against B. subtilis, B. cereus and S. aureus.Acetone extracts of O. basilicum and O. sanctum were found to be more potent being capable of exerting significant inhibitory activities against majority of the bacteria investigated. Acetone extract of young inflorescence of O. americanum showed highest antibacterial activity against B. cereus (14±1mm) which was also higher (10±1mm) than the inhibition of standard Clotrimazole (10mcg). Hot petroleum ether extract of mature leaves of O. basilicum showed highest activity against E. coli (16±2mm) which was also higher than the inhibition ofAmpicillin, Streptomycitin, Erythromycin.Petroleum ether extract of young leaves of O. sanctum recorded highest inhibition against P. vulgaris (20±2mm). Presence of tannins, flavonoids, saponins, phenols in all the parts of the plants. Use of different parts instead of using whole plant will help in sustainable management of these medicinal plants.

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