title: Anti-leishmanial activities of extracts and isolated compounds from Drechslera rostrata and Eurotium tonpholium.
abstract: 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.
authors.affiliation: Chemistry Department, King Saud University, Riyadh, KSA.
authors.forename: Amani S
authors.initials: AS
authors.lastname: Awaad
authors.forename: Haifa M
authors.initials: HM
authors.lastname: Al-Zaylaee
authors.forename: Saleh I
authors.initials: SI
authors.lastname: Alqasoumi
authors.forename: Mohamed E
authors.initials: ME
authors.lastname: Zain
authors.forename: Ebtesam M
authors.initials: EM
authors.lastname: Aloyan
authors.forename: Ahmed M
authors.initials: AM
authors.lastname: Alafeefy
authors.forename: Elham S H
authors.initials: ES
authors.lastname: Awad
authors.forename: Reham M
authors.initials: RM
authors.lastname: El-Meligy
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001203:Ascomycota / Q000737:chemistry*; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology; D006224:Cricetinae; D055325:Eurotium / Q000737:chemistry*; D005260:Female; D006168:Guinea Pigs; D018320:Leishmania major / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy*; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D017208:Rats, Wistar; D023382:Toxicity Tests, Acute; D059550:Toxicity Tests, Subchronic
chemical_list: D000981:Antiprotozoal Agents; D001688:Biological Products
keywords: 1, 8-dihydroxy-3-methoxy-6-methyl-anthraquinone; 8-peroxide, diisooctyl phthalate; Drechslera rostrata; Eurotium tonpholium; Leishmania major; anti-leishmanial activity; ergosterol-5; mannitol