GALLOTANNINS FROM QUERCUS ROBUR CULTIVATED IN EGYPT
Salwa
Farag
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
author
Nasr
El-Emary
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
author
Masatake
Niwa
Faculty of Pharmacy, Meijo University, Nagoya 468, Japan
author
text
article
1998
eng
Four gallotannins: 1,2,3-tri-O-galloyl-b-glucose; 1,2,3,6-tetra-O-galloyl-b-D-glucose; 1,2,3,4,6-penta-O-galloyl-b-D-glucose and 1,2,3,4,6-penta-O-galloyl-a-D-glucose, together with gallic acid and methoxy gallic acid have been isolated from the seeds of Quercus robur and their stuctures were elucidated on the basis of chemical and spectral evidence.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
1
6
https://bpsa.journals.ekb.eg/article_67765_000bff64943c0ed8e7dd44663aa35d55.pdf
dx.doi.org/10.21608/bfsa.1998.67765
MOLECULAR STRUCTURAL PARAMETERS IN TUBERCULOSTATIC ACTIVITY OF POLYHYDROXYXANTHONES
Hassan
Farag
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
author
Farghaly
Omar
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
author
Nadia
Mahfouz
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
author
text
article
1998
eng
This investigation was undertaken to test the correlation of the observed tuberculostatic activity of a series of 7(2)-polyhydroxyxanthones 1a-j with their lipophilic parameters (Rm) as well as molecular orbital descriptors such as; dipole moment (dp); electro density (D); heat of formation (hf), torsion angle (tor); van der Waal forces (vdw), bond length (str) and bond angle (bnd). The Rm-values were calculated from the corresponding Rf-values, determined using polyamide plates. The molecular orbital regressors were derived through semi-empirical calculations using MMX-computer program.
QSAR analysis of the activity parameters (Ka, Log Ka, Ka* and logKa*) as dependent variables and Rm or combination of Rm and dummy parameters representing the substitution pattern of hydroxyl groups on ring C of the xanthone nucleus demonstrated an increase in the lipophilic character by itself which did not correlate (r» -0.42) with increased potency against Mycobacterium lufu. Permeability study using standard cellophane membrane showed that, the synthesized compounds were poorly penetrating and may act directly on the cell wall. On the contrary higher correlation (r= 0.91) was observed between the activity parameter (log Ka*) and the electron density at C-4.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
7
14
https://bpsa.journals.ekb.eg/article_67766_8cba5ae25a8ac93be34b5427ff7f155a.pdf
dx.doi.org/10.21608/bfsa.1998.67766
DESIGN, SYNTHESIS AND ANTIDEPRESSANT ACTIVITY OF SOME N2-SUBSTITUTED NALIDIXIC ACID HYDRAZIDES AND THEIR CYCLIZED ANALOGUES
Adel
Youssef
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
author
Farghaly
Omar
Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
author
Hosney
Elsherief
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
author
Gamal El Din
Abuo-Rahma
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt
author
text
article
1998
eng
A series of N2-substituted nalidixic acid hydrazides 7-26 and some of their rigid analogues 29-31 in which the hydrazinocarbonyl moiety has been replaced by the corresponding 1,3,4-oxadiazole nucleus were synthesized as potential antidepressant agents. The preparation of the aforementioned compounds was achieved by reaction of nalidixic acid hydrazine 6 with the appropriate carbonyl compound or isothiocyanate derivative to afford the corresponding N-alkylidenes 7-11; N-arylidenes 12-26 or the thiocarbamoylhydrazinocarbonyl derivatives 27 and 28 respectively. Cyclodesulfurization of the latter derivatives yielded the corresponding 5-substituted amino-1,3,4-oxadiazoles 29 and 30. the unsubstituted 5-amino-1,3,4-oxadiazol-2-yl derivative 31 was synthesized by interaction of the hydrazide 6 with cyanogens bromide. The structures of the synthesized compounds were confirmed by IR; 1H-NMR and MS and their purity as assessed by TLC and elemental analyses.
Eleven of the synthesized compounds and isocarboxazide as a reference drug were tested at three dose levels (0.5; 1.0 and 1.5 mg/kg) for antidepressant activity in mice. Reduction in the duration of immobility in forced swimming test was taken as a measure for antidepressant activity. Seven of the tested substituted compounds and the unsubstituted hydrazide 6 exhibited highly significant difference from the control group at a dose level of 1.5 mg/kg. The acetophenonylidene derivative 18 showed antidepressant activity comparable to that of the reference drug. The rigid substituted hydrazide analogues represented by compound 29 were found to be inactive at the lower dose level and showed moderately significant difference than the control group at the higher dose level. This indicates that, cyclization of the hydrazide moiety to the corresponding 1,3,4-oxadiazole derivatives greatly reduced the antidepressant activity.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
15
26
https://bpsa.journals.ekb.eg/article_67767_238dd039e3932b1cc928aafdbb7f6233.pdf
dx.doi.org/10.21608/bfsa.1998.67767
TRITERPENOIDAL SAPONINS FROM KOCHIA INDICA WIGHT.
Khaled
Mohamed
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
author
Hashim
Hasanean
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt
author
Kazuhiro
Ohtani
Institute of Pharmaceutical Science, Hiroshima University School of Medicine, 1-2-3 Kasumi, Minami-Ku, Hiroshima 734, Japan
author
Kazuo
Yamasaki
Institute of Pharmaceutical Science, Hiroshima University School of Medicine, 1-2-3 Kasumi, Minami-Ku, Hiroshima 734, Japan
author
text
article
1998
eng
Seven oleanolic acid saponins (1-7) were isolated from the aerial parts of Kochia indica Wight. (Chenopodiaceae), of which saponins (4-7) are seco-glycosides containing acidic substituents at C-3 of glucuronic acid. Compounds (1-6) have been isolated for the first time from genus Kochia and compound (7) is first reported from family Chenopodiaceae. The structures of the isolated compounds were characterized by different spectroscopic methods and by comparison with previously reported data.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
27
36
https://bpsa.journals.ekb.eg/article_67832_c38fce996b070b4d661cf9cd1ef1e5a5.pdf
dx.doi.org/10.21608/bfsa.1998.67832
ANTIMICROBIAL ACTIVITY OF PYOVERDIN PIGMENT PRODUCED BY PSEUDOMONAS
A.
Al-Shibib
University of Philadelphia, College of Pharmacy
author
A.
Ebu-Talb
University of Philadelphia, College of Pharmacy
author
text
article
1998
eng
The main purpose of this paper is to focus light on the possibilities of presence of antimicrobial activity in pyoverdin pigment produced by Pseudomonas aeruginosa. The pyoverdin pigments were prepared form (1000) strains isolated from burns and chronic otitis media sources (Governmental and special Microbiological laboratories).
The inhibitory action were determined by both microdilution assay and minimum inhibitory concentration. Values were between 85-105 ml.
The stability of pyoverdin after extraction revealed that it is stable against different treatment of heat, pH and salt treatment.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
37
40
https://bpsa.journals.ekb.eg/article_67833_1fb9bac93cf6794911093d13ff122403.pdf
dx.doi.org/10.21608/bfsa.1998.67833
PART 1: DESIGN, SYNTHESIS AND EVALUATION OF NEW SITE-SPECIFIC MONOAMINE OXIDASE INHIBITORS
F.
Mohamed
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
N.
El-Rabbat
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
P.
Khashaba
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
H.
Farag
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt
author
N.
Bodor
Center for Drug Discovery, College of Pharmacy, University of Florida, Gainesville, Florida, USA
author
text
article
1998
eng
Certain new monoamine oxidase inhibitors (MAOIs) containing a pyridinium moiety as an integral part of their structures (Q) were designed. The quaternaries, their corresponding 1,4-dihydroxypyridine derivatives (CDS) and their parent pyridine compounds (P) were synthesized. A spectrofluorimetric method was used to test their in vitro monoamine oxidase inhibition. The compounds showed reasonable activities by the test performed.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
41
54
https://bpsa.journals.ekb.eg/article_67834_46e481835c47c59a5d3a84b84c5fbcc8.pdf
dx.doi.org/10.21608/bfsa.1998.67834
NEW ALKALOIDS FROM LUPINUS ALBUS L. SEEDS
M.
Mohamed
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, 71524 Assiut, Egypt
author
text
article
1998
eng
Two new lupin alkaloids, (+)-14-dehydro-10a-hydroxytermisine, (-)-13a-hydroxy-5,6-dehydromultiflorine N-oxide have been isolated from the ethanolic extract of Lupinus albus seeds together with (+)-13a-(2-methylbutyryl)-oxylupanine, (+)-a-isolupanine, (+)-ammodendrine and (-)-sparteine. The structure elucidation of these alkaloids is based on spectroscopic and semisynthetic methods.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
55
60
https://bpsa.journals.ekb.eg/article_67835_a348d5fcbdad4ba1bd7085bca66d0af9.pdf
dx.doi.org/10.21608/bfsa.1998.67835
MACRO- AND MICROMORPHOLOGICAL STUDY OF THE LEAVES AND STEMS OF CRYPTOSTEGIA GRANDIFLORA R.Br. CULTIVATED IN EGYPT
M.
Assaf
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, 71524 Assiut, Egypt
author
text
article
1998
eng
The macro- and micromorphological characters of the leaves and stems of Cryptostegia grandiflora R.Br. cultivated in Egypt are described. The diagnostic features by which the plant could be identified in both the entire and powdered forms are reported.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
61
74
https://bpsa.journals.ekb.eg/article_67836_d41d8cd98f00b204e9800998ecf8427e.pdf
dx.doi.org/10.21608/bfsa.1998.67836
PHYTOCHEMICAL STUDY FOR THE CONTENTS OF HIBISCUS SABDARIFFA L. SEEDS CULTIVATED IN EGYPT
M.
Assaf
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, 71524 Assiut, Egypt
author
text
article
1998
eng
A study of the protein, amino acids, minerals and lipids content for the seeds of Hibiscus sabdariffa L. was performed. Arginine, lysine, valine and phenylalanine were the major essential amino acids, besides glutamic, aspartic, glysine, serine and alanine. The seeds were found to be rich in magnesium (1.30%) and potassium contents (1.02%). Gossypol (polyphenolic bisesquiterpene) was detected in the pet. Ether and ether extracts of the seeds and estimated by HPLC (2.8x10-3 g.% w/w).
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
75
80
https://bpsa.journals.ekb.eg/article_67837_ef6cdc363faf634048e1c30d54299ac0.pdf
dx.doi.org/10.21608/bfsa.1998.67837
REVISED 13C-NMR ASSIGNMENTS OF KAURENOIDS FROM WEDELIA PROSTRATA HOOK et ARN (HEMSL)
S.
Farag
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, 71524 Assiut, Egypt
author
H.
Hassanean
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, 71524 Assiut, Egypt
author
M.
Makboul
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, 71524 Assiut, Egypt
author
N.
Emary
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, 71524 Assiut, Egypt
author
M.
Niwa
Faculty of Pharmacy, Meijo University, Tempaku, Nagoya, Japan
author
text
article
1998
eng
A sesquiterpene and nine known ent kaurenoids in addition to two flavonoids were isolated from Wedelia prostrate (Compositae) cultivated in Egypt for the first time. Their structures were elucidated on the basis of spectroscopic methods. The HH-COSY, CH-COSY, COLOC and/or HMBC studies led to revisement of the previously reported 13C-NMR resonances of some of them.
Bulletin of Pharmaceutical Sciences Assiut University
Assiut University, Faculty of Pharmacy
1110-0052
21
v.
1
no.
1998
81
87
https://bpsa.journals.ekb.eg/article_67842_d41d8cd98f00b204e9800998ecf8427e.pdf
dx.doi.org/10.21608/bfsa.1998.67842