Metabolism by Schistosoma mansoni of a new schistosomicide: 2-[(1-methylpropyl)amino]-1-octanethiosulphuric acid

Parasitology ◽  
1995 ◽  
Vol 111 (2) ◽  
pp. 177-185 ◽  
Author(s):  
M. L. O. Penido ◽  
D. L. Nelson ◽  
L. Q. Vieira ◽  
D. G. Watson ◽  
J. R. Kusel
Keyword(s):  
Oral Dose ◽  
Thin Layer ◽  
Schistosoma Mansoni ◽  
Mass Spectroscopy ◽  
Female Adult ◽  
Male And Female ◽  
New Class ◽  
Organic Extracts ◽  
Layer Chromatography

SUMMARYIn order to investigate the mode of action of a new class of schistosomicides, the N-alkylaminoalkanethiosulphuric acids, the ‘outer 35S] 2-[(1-methylpropyl)amino]-1-octanethiosulphuric acid was synthesized. Labelling studies of adult Schistosoma mansoni were performed in infected mice and in in vitro incubations. After a single oral dose of the drug to infected mice, 5 metabolites were detected by thin-layer chromatography in organic extracts of male and female adult schistosomes. In vitro studies showed that the same compounds were present in organic extracts obtained from adult male and female worms. One of these metabolites was identified by mass spectroscopy as being the dimeric disulphide derivative of the parent labelled thiosulphuric acid.

scholarly journals A Comparative Proteomic Analysis of Praziquantel-Susceptible and Praziquantel-Resistant Schistosoma mansoni Reveals Distinct Response Between Male and Female Animals

2021 ◽  
Vol 2 ◽  
Author(s):  
António Pinto-Almeida ◽  
Tiago M. F. Mendes ◽  
Pedro Ferreira ◽  
Ana B. Abecasis ◽  
Silvana Belo ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Schistosoma Mansoni ◽  
Rural Areas ◽  
Neglected Tropical Disease ◽  
Female Adult ◽  
Male And Female ◽  
Comparative Proteomic Analysis ◽  
The World ◽  
And Control

Schistosomiasis is a chronic neglected tropical disease saddling millions of people in the world, mainly children living in poor rural areas. Praziquantel (PZQ) is currently the only drug used for the treatment and control of this disease. However, the extensive use of this drug has brought concern about the emergence of PZQ-resistance/tolerance by Schistosoma mansoni. Studies of Schistosoma spp. genome, transcriptome, and proteome are crucial to better understand this situation. In this in vitro study, we compare the proteomes of a S. mansoni variant strain stably resistant to PZQ and isogenic to its fully susceptible parental counterpart, identifying proteins from male and female adult parasites of PZQ-resistant and PZQ-susceptible strains, exposed and not exposed to PZQ. A total of 60 Schistosoma spp. proteins were identified, some of which present or absent in either strain, which may putatively be involved in the PZQ-resistance phenomenon. These proteins were present in adult parasites not exposed to PZQ, but some of them disappeared when these adult parasites were exposed to the drug. Understanding the development of PZQ-resistance in S. mansoni is crucial to prolong the efficacy of the current drug and develop markers for monitoring the potential emergence of drug resistance.

Phytochemical, Analytical and Medicinal Studies of Holoptelea integrifolia Roxb. Planch - A Review

2019 ◽  
Vol 5 (4) ◽  
pp. 270-277 ◽  
Author(s):  
Vijay Kumar ◽  
Simranjeet Singh ◽  
Ragini Bhadouria ◽  
Ravindra Singh ◽  
Om Prakash
Keyword(s):  
Liquid Chromatography ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
High Performance ◽  
Biologically Active ◽  
Toxicological Studies ◽  
Wide Range ◽  
Layer Chromatography

Holoptelea integrifolia Roxb. Planch (HI) has been used to treat various ailments including obesity, osteoarthritis, arthritis, inflammation, anemia, diabetes etc. To review the major phytochemicals and medicinal properties of HI, exhaustive bibliographic research was designed by means of various scientific search engines and databases. Only 12 phytochemicals have been reported including biologically active compounds like betulin, betulinic acid, epifriedlin, octacosanol, Friedlin, Holoptelin-A and Holoptelin-B. Analytical methods including the Thin Layer Chromatography (TLC), High-Performance Thin Layer Chromatography (HPTLC), High-Performance Liquid Chromatography (HPLC) and Liquid Chromatography With Mass Spectral (LC-MS) analysis have been used to analyze the HI. From medicinal potency point of view, these phytochemicals have a wide range of pharmacological activities such as antioxidant, antibacterial, anti-inflammatory, and anti-tumor. In the current review, it has been noticed that the mechanism of action of HI with biomolecules has not been fully explored. Pharmacology and toxicological studies are very few. This seems a huge literature gap to be fulfilled through the detailed in-vivo and in-vitro studies.

scholarly journals In vitro effects of artesunate on the survival of worm pairs and egg production of Schistosoma mansoni

2009 ◽  
Vol 83 (1) ◽  
pp. 7-11 ◽  
Author(s):  
Y. Mitsui ◽  
M. Miura ◽  
Y. Aoki
Keyword(s):  
Schistosoma Mansoni ◽  
Adult Worm ◽  
Survival Time ◽  
Egg Production ◽  
Inhibitory Effect ◽  
Male And Female ◽  
Paired Male ◽  
In Vitro Effects ◽  
Paired Female

AbstractThe effect of artesunate (ART) on the survival time of adult worm pairs of Schistosoma mansoni and on their egg output during in vitro culture was assessed. ART significantly decreased the survival time of both paired male and female worms at concentrations of 5, 10, 20 and 40 mg l− 1 during in vitro cultivation. An inhibitory effect of ART on the daily egg output of paired female worms during in vitro cultivation was also observed.

STEROID EXCRETION AND BIOSYNTHESIS, WITH SPECIAL REFERENCE TO ANDROST-16-ENES, IN A WOMAN WITH A VIRILISING ADRENOCORTICAL CARCINOMA

1969 ◽  
Vol 60 (2) ◽  
pp. 265-275 ◽  
Author(s):  
D. B. Gower ◽  
Margaret I. Stern
Keyword(s):  
Liquid Chromatography ◽  
Thin Layer ◽  
Adrenocortical Carcinoma ◽  
Gas Liquid Chromatography ◽  
Adrenal Carcinoma ◽  
Peripheral Plasma ◽  
Steroid Excretion ◽  
Layer Chromatography ◽  
Free Steroid

ABSTRACT The level of 3α-hydroxy-5α-androst-16-ene (Δ16-androstenol) excreted as glucuronide in the urine of a woman with virilising adrenal carcinoma was measured by gas-liquid chromatography (GLC) of the free steroid and its chloromethyl dimethyl silyl (CMDS) ether and found to be 1.46 mg/day. On the basis of thin-layer chromatography (TLC) and GLC of free steroid and derivatives, Δ16-androstenol has also been tentatively identified in the urinary sulphate fraction and in peripheral plasma. The values were approx. 0.6 mg/d and 2.8 μg/100 ml respectively. After operation, the amount of urinary Δ16-androstenol (as glucuronide) fell to a low level; none was detected in plasma or in urine (as sulphate). Levels of other steroids in the urine and plasma were consistent with the clinical diagnosis of virilising adrenal carcinoma. After operation, the excretion of most of these steroids had reverted to values which were normal or lower. In vitro, the cancerous adrenal tissue metabolised 4-14C-pregnenolone to 3β-hydroxy-androsta-5,16-diene (0.2 %) and 4-14C-progesterone to a small quantity (< 0.03 %) of androsta-4,16-dien-3-one. No androst-16-enes were formed from radioactive dehydroepiandrosterone (DHA) or testosterone. The formation of other labelled metabolites confirmed studies by earlier workers.

THE ACTION OF DIBUTYRYL CYCLIC 3′,5′-ADENOSINE MONOPHOSPHATE ON THE MOUSE THYROID GLAND IN VITRO

1970 ◽  
Vol 47 (3) ◽  
pp. 333-338 ◽  
Author(s):  
PAT KENDALL-TAYLOR ◽  
D. S. MUNRO
Keyword(s):  
Thyroid Gland ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Adenosine Monophosphate ◽  
Thyroid Stimulating Hormone ◽  
In Vitro Assay ◽  
Vitro Assay ◽  
Layer Chromatography ◽  
Mouse Thyroid

SUMMARY The effects of dibutyryl cyclic 3′,5′-adenosine monophosphate (DBc-AMP) on the mouse thyroid gland have been investigated in the in-vitro assay of Brown & Munro (1967). The distribution of 131I-labelled compounds in the glands and the supporting medium have been analysed by thin-layer chromatography and the changes induced by cyclic 3′,5′-adenosine monophosphate (c-AMP), DBc-AMP or thyroid-stimulating hormone (TSH) compared. The release of 131I was increased when the glands were incubated with DBc-AMP, c-AMP or TSH. The potency of DBc-AMP was approximately 50 times that of c-AMP on a basis of molarity. Like TSH, DBc-AMP increased the proportion of iodothyronines in the system as a whole, whereas c-AMP had little effect. The possible explanations for this are discussed.

Sign in / Sign up

Export Citation Format

Share Document