Bioactive cubitane diterpenoids from a Colombian gorgonian species of the genus Eunicea

2012 ◽  
Vol 84 (9) ◽  
pp. 1847-1855 ◽  
Author(s):  
Xiaomei Wei ◽  
Karinel Nieves ◽  
Abimael D. Rodríguez
Keyword(s):  
Plasmodium Falciparum ◽  
Mycobacterium Tuberculosis ◽  
Cytotoxic Activity ◽  
National Cancer Institute ◽  
Spectroscopic Analysis ◽  
Gorgonian Coral ◽  
Gorgonian Species ◽  
Pathogenic Microbes ◽  
New Metabolites

Two new diterpenes having the rare cubitane skeleton were isolated from a southwestern Caribbean gorgonian coral of the genus Eunicea. The structures of the new metabolites, as well as those of three known cubitanes were elucidated by extensive spectroscopic analysis. One compound showed significant in vitro cytotoxic activity against a National Cancer Institute (NCI) panel of cancer cell lines, whereas the remaining metabolites were shown to exert mild antitubercular and antimalarial activities against the pathogenic microbes Mycobacterium tuberculosis and Plasmodium falciparum.

scholarly journals New Quinolone-Based Thiosemicarbazones Showing Activity Against Plasmodium falciparum and Mycobacterium tuberculosis

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1740 ◽  
Author(s):  
Richard M. Beteck ◽  
Ronnett Seldon ◽  
Audrey Jordaan ◽  
Digby F. Warner ◽  
Heinrich C. Hoppe ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Mycobacterium Tuberculosis ◽  
Drug Interactions ◽  
Hela Cells ◽  
African Region ◽  
H37rv Strain

Co-infection of malaria and tuberculosis, although not thoroughly investigated, has been noted. With the increasing prevalence of tuberculosis in the African region, wherein malaria is endemic, it is intuitive to suggest that the probability of co-infection with these diseases is likely to increase. To avoid the issue of drug-drug interactions when managing co-infections, it is imperative to investigate new molecules with dual activities against the causal agents of these diseases. To this effect, a small library of quinolone-thiosemicarbazones was synthesised and evaluated in vitro against Plasmodium falciparum and Mycobacterium tuberculosis, the causal agents of malaria and tuberculosis, respectively. The compounds were also evaluated against HeLa cells for overt cytotoxicity. Most compounds in this series exhibited activities against both organisms, with compound 10, emerging as the hit; with an MIC90 of 2 µM against H37Rv strain of M. tuberculosis and an IC50 of 1 µM against the 3D7 strain of P. falciparum. This study highlights quinolone-thiosemicarabazones as a class of compounds that can be exploited further in search of novel, safe agents with potent activities against both the causal agents of malaria and tuberculosis.

scholarly journals Antibacterial and Antifungal Sesquiterpenoids from Aerial Parts of Anvillea garcinii

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1730 ◽  
Author(s):  
Shagufta Perveen ◽  
Jawaher Alqahtani ◽  
Raha Orfali ◽  
Hanan Y. Aati ◽  
Areej M. Al-Taweel ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Spectroscopic Analysis ◽  
Antimicrobial Properties ◽  
Ionization Mass ◽  
Two Dimensional ◽  
One Dimensional ◽  
Aerial Parts ◽  
Pathogenic Microbes ◽  
Antibacterial And Antifungal ◽  
New Metabolites

Two new sesquiterpenoids belonging to the guaiane, 4α,9α,10α-trihydroxyguaia-11(13)en-12,6α-olide (1), and germacrane, 9β-hydroxyparthenolide-9-O-β-D-glucopyranoside (2), classes have been isolated from the leaves of the Saudi medicinal plant Anvillea garcinii along with seven known compounds (3–9). The structures of the new metabolites were elucidated by spectroscopic analysis, including one-dimensional (1D) and two-dimensional (2D) Nuclear Magnetic Resonance (NMR) and high-resolution electrospray ionization mass spectrometry (HR-ESIMS). The antimicrobial properties of 1–9 were screened against seven different pathogenic microbes, and compounds 1–3 showed a potent antifungal activity.

Salaterpene E, a eudesmane-type sesquiterpene from Salacia longipes var. camerunensis

2016 ◽  
Vol 71 (2) ◽  
pp. 87-93 ◽  
Author(s):  
Brice Mittérant Mba’ning ◽  
Bruno Lenta Ndjakou ◽  
Ferdinand Mouafo Talontsi ◽  
Alain Meli Lannang ◽  
Birger Dittrich ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Absolute Configuration ◽  
Previous Investigation ◽  
Spectroscopic Analysis ◽  
Inhibitory Concentration ◽  
Anomalous Scattering ◽  
X Ray Diffraction ◽  
Meoh Extract ◽  
X Ray

AbstractA mixture of two compounds with potent antiplasmodial activity in vitro against the W2 strain of Plasmodium falciparum (half maximal inhibitory concentration, 1.12 μg/mL) was obtained in a previous investigation of the CH2Cl2-MeOH extract of the seeds of Salacia longipes var. camerunensis. Separation by column chromatography led now to the isolation of salaterpene E (1) and (1R,2R,4S,5S,6R,7R,9S,10R)-2-acetoxy-1,6,9-tribenzoyloxy-4-hydroxy-dihydro-β-agarofuran (2). The structure of 1 was elucidated by spectroscopic analysis, and its absolute configuration was established unambiguously by means of single-crystal X-ray diffraction. Also the absolute configurations of the recently described salaterpenes A (2a) and D (2b) were determined by this method using the anomalous scattering of the oxygen atoms only.

Ultrastructural observations on the in vitro cytoadherence of Plasmodium falciparum infected red blood cells

1990 ◽  
Vol 48 (3) ◽  
pp. 914-915
Author(s):  
D.J.P. Ferguson ◽  
A.R. Berendt ◽  
J. Tansey ◽  
K. Marsh ◽  
C.I. Newbold
Keyword(s):  
Plasmodium Falciparum ◽  
Red Blood Cells ◽  
Blood Cells ◽  
Umbilical Vein ◽  
Cell Types ◽  
Amelanotic Melanoma ◽  
Cytoplasmic Process ◽  
Umbilical Vein Endothelial Cells

In human malaria, the most serious clinical manifestation is cerebral malaria (CM) due to infection with Plasmodium falciparum. The pathology of CM is thought to relate to the fact that red blood cells containing mature forms of the parasite (PRBC) cytoadhere or sequester to post capillary venules of various tissues including the brain. This in vivo phenomenon has been studied in vitro by examining the cytoadherence of PRBCs to various cell types and purified proteins. To date, three Ijiost receptor molecules have been identified; CD36, ICAM-1 and thrombospondin. The specific changes in the PRBC membrane which mediate cytoadherence are less well understood, but they include the sub-membranous deposition of electron-dense material resulting in surface deformations called knobs. Knobs were thought to be essential for cytoadherence, lput recent work has shown that certain knob-negative (K-) lines can cytoadhere. In the present study, we have used electron microscopy to re-examine the interactions between K+ PRBCs and both C32 amelanotic melanoma cells and human umbilical vein endothelial cells (HUVEC).We confirm previous data demonstrating that C32 cells possess numerous microvilli which adhere to the PRBC, mainly via the knobs (Fig. 1). In contrast, the HUVEC were relatively smooth and the PRBCs appeared partially flattened onto the cell surface (Fig. 2). Furthermore, many of the PRBCs exhibited an invagination of the limiting membrane in the attachment zone, often containing a cytoplasmic process from the endothelial cell (Fig. 2).

Tuberkulose - Screening

2011 ◽  
Vol 68 (7) ◽  
pp. 381-387
Author(s):  
Otto Schoch
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Interferon Gamma ◽  
Wird Eine ◽  
Interferon Gamma Release Assays

Das primäre Ziel der Aktivitäten zur bevölkerungsbezogenen Tuberkulosekontrolle ist die Identifizierung von Patienten mit sputummikroskopisch positiver Lungentuberkulose. Wenn diese Patienten umgehend therapiert werden, haben sie nicht nur eine optimale Heilungschance, sondern übertragen auch den Krankheitserreger nicht weiter auf andere Personen. Das Screening, die systematische Suche nach Tuberkulose, erfolgt in der Regel radiologisch bei der Suche nach Erkrankten, während immunologische Teste bei der Suche nach einer Infektion mit Mycobacterium tuberculosis zur Anwendung kommen. Diese Infektion, die ein erhöhtes Risiko für die Entwicklung einer Tuberkulose-Erkrankung mit sich bringt, wird im Rahmen der Umgebungsuntersuchungen oder bei Hochrisikogruppen gesucht. Neben dem traditionellen in vivo Mantoux Hauttest stehen heute die neueren in vitro Blutteste, die sogenannten Interferon Gamma Release Assays (IGRA) zur Verfügung, die unter anderem den Vorteil einer höheren Spezifität mit sich bringen, weil die verwendeten Antigene der Mykobakterien-Wand beim Impfstamm Bacille Calmitte Guerin (BCG) und bei den meisten atypischen Mykobakterien nicht vorhanden sind. Zudem kann bei Immunsupprimierten dank einer mitgeführten Positivkontrolle eine Aussage über die Wahrscheinlichkeit eines falsch negativen Testresultates gemacht werden. Bei neu diagnostizierter Infektion mit Mycobacterium tuberculosis wird eine präventive Chemotherapie mit Isoniazid während 9 Monaten durchgeführt.

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