Synthesis and antileishmaniasis activity of 2-[2′-chlorostyryl]-4-[δ-diethyl-amino-α-methylbutylamino]-7-chloroquinazoline diphosphate

Yakhontov, L. N.; Zhikhareva, G. P.; Mastafanova, L. I.; Евстратова, М. И.; Pershin, G. N.; Moskalenko, N. Yu.; Pushkina, T. V.; Kutchak, S. N.; Fadeeva, N. I.; Sokolova, N. D.; Gus'kova, T. A.; Chicherina, L. A.; Sharova, S. A.

doi:10.1007/bf00764884

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“… Sub‐chronic toxicity before inducing Leishmanias :Oral administration of the alcohol extract of D. rostrata and E. tonpholium at the tested dose didn't disturb liver and kidney functions (Table ). Interestingly, the obtained results revealed that these extracts are safer than standard drug which causes negative side effects on liver and kidney function (Meinecke et al ., ; Yakhontov et al ., ).…”

Section: Resultsmentioning

confidence: 99%

“…Oral administration of the alcohol extract of D. rostrata and E. tonpholium at the tested dose didn't disturb liver and kidney functions (Table 2). Interestingly, the obtained results revealed that these extracts are safer Eurotium tonpholium H6 1,8-dihydroxy-3-methoxy-6-methyl-anthraquinone H7 1,4,5-trihydroxy-7-methoxy-2-methyl-anthraquinone 777 ANTI-LEISHMANIAL ACTIVITIES than standard drug which causes negative side effects on liver and kidney function (Meinecke et al, 1999;Yakhontov et al, 1987).…”

Section: Sub-chronic Toxicity Before Inducing Leishmaniasmentioning

confidence: 97%

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Anti-leishmanial Activities of Extracts and Isolated Compounds fromDrechslera rostrataandEurotium tonpholium

et al. 2013

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The fungal extract of Drechslera rostrata and Eurotium tonpholium showed a significant anti-leishmanial activity against Leishmania major; IC50 was 28.8 and 28.2 μg/mL, respectively. Seven compounds, five from D. rostrata (H1-H5) and two from E. tonpholium (H6 and H7), were isolated and identified using different spectroscopic analysis including (1) HNMR, (13) CNMR, Hetero-nuclear multiple bond connectivity (HMBC), Hetero-nuclear Multiple Quantum Correlation (HMQC), and EI-MS. The isolated compounds are: di-2-ethylhexyl phthalate (1), (22E)-5α,8α-epidioxyergosta-6,22-diene-3β-ol (2),1,3,8-trihydroxy-6-methyl-nthraquinone (3), aloe-emodine 8-O-glucopyranoside(4), 2R, 3R,4R,5R hexane 1, 2, 3, 4, 5, 6 hexole (Mannitol) (5), 1,8-dihydroxy-3-methoxy-6-methyl-anthraquinone (6) and 1, 4, 5-trihydroxy-7-methoxy-2-methyl-anthraquinone (7). However, compounds (1) and (6) showed activity against L. major with IC50 of 3.2 and 10.38 µg/mL, respectively. On the other hand, oral administration of the two extracts (100 mg/kg) and compounds 1 and 6 (50 mg/kg) showed very good activity when compared with the anti-leishmanial drug Pentostam (125 mg/kg). Interestingly, the complete heeling activity of the extracts and compounds (1) and (6) was obtained after 13-17 days of treatment, while complete healing activity of Pentostam was obtained after 28 days. No alteration on liver and kidney functions was recorded on animals treated with the two extracts for 15 consecutive days.

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Section: Resultsmentioning

confidence: 99%

Section: Sub-chronic Toxicity Before Inducing Leishmaniasmentioning

confidence: 97%