The Pharmaceutical and Chemical Journal

1-5

Authors: Rodriguez L, Raffaelli S, Abreo E, Altier N, Vazquez A

In spite of the great advances in chemotherapeutics, infectious diseases are still one of the leading causes of death in the world. Thus, development of new antimicrobial compounds against different microorganisms and with new mechanisms of action is becoming critically important. In our continuous search for new antimicrobial molecules we screened the culture broth of several soil microorganisms. A Beauveria isolate showed promising activity and we isolated and determined the structure of a phenolic glycoside (6-Methyl-1,2,4-trihydroxybenzene-1-O-β-D-4´-methyl-glucopyranoside)never before reported in this species.

13-20

Authors: Harrizul Rivai, Susi Yulianti, Boy Chandra

Research on the qualitative and quantitative analysis of bay leaves (Syzygium polyanthum (WIGHT) Walp) has been carried out from hexane, acetone, ethanol and water extracts. This study aims to analyze the chemical compounds contained in each extract of hexane, acetone, ethanol, and water from bay leaves, and determine the secondary metabolic content contained in each extract of the bay leaf. The extraction method used was maceration for hexane, acetone and ethanol solvents, infusions for water solvents. The results obtained from phytochemical screening and assay showed that bay leaf acetone extract contained phenol 0.1202% and tannin 0.1452%. Ethanol extract of bay leaves contains 0.34% alkaloids, 0.59% flavonoids, 0.1258% phenols, and 0.1688% tannins. Bay leaf water extract contains 0.486% flavonoids, phenol 0.2248% and tannin 0.1622%. The hexane extract of bay leaves was not detected to contain secondary metabolites.

31-36

Authors: Barikpoa Uedeme-Naa, Awoteinm D.I. George

The effect of Moringa oleifera leaf powder on the organosomatic index (gill, kidney, liver, heart and spleen), condition factor and glucose profile was carefully examined in this study. It was observed that the responses of Clarias gariepinus juveniles (mean length, 29.8±1.40cm SD; mean weight, 203.3± 5.11g SD g) exposed to 0.05, 0.10, 0.15 and 0.20g/l of Moringa Oleifera leaf powder for 15 days was concentration dependent. Fish gill recorded the highest index at 0.20g/l (24.55%) and least at 0.05g/l (17.42%) when compared with control (19.57%). Gill, kidney and spleen indices at 0.05, 0.10, 0.15 and 0.20g/l and condition factor were not significantly impacted (P>0.05) while liver and heart were significantly impacted (P<0.05) with increase in M. oleifera leaf concentration when compared with control. Glucose level was significantly (P<0.05) impacted at all the treatment levels when compared with control. The study indicated that the phytochemicals in Moringa oleifera leaf could improve the health status or well being and influence positively on the utilization of energy derived from glucose for other necessary use in fish body.

53-62

Authors: Okafor, C. Sandra, Onukwuli, O. Dominic, Anadebe, V. Chikaodili

This work is on optimization and impedance study of inhibition efficiency of moringa leaf extract as corrosion inhibitor of aluminum in alkaline solution. Gravimetric method, polarization study and impedance measurement was employed in the corrosion inhibition study. Response surface methodology (RSM) was applied in the optimization process. Central composite design tool of design expert software version 9 was used to evaluate the effects and interactions of four variables of acid concentration (AC), inhibitor concentration (IC), temperature (T) and time (t) on the inhibition efficiency of the extract. Analysis of variance (ANOVA) was used to study the data generated. Moringa leaf extract exhibited optimum inhibition efficiency of 96.65 % at optimum inhibitor concentration of 1.5 g/L-1. The electrochemical impedance spectra revealed that moringa leaf extract acted as a mixed-type inhibitor. The extract is highly efficient in surface treatment of aluminum in alkaline environment.

69-76

Authors: M.K. Haruna, C.U. Aguoru, C.C. Iheukwumere, C.I.C. Ogbonna, Jose Addy

This work was carried out at Jigawa Research Institute Biotechnology Laboratory Kazaure to determine callus induction potentials of 30 wheat genotypes using matured embryo as ex-plant source under different 2,4-Dichlorophenoxyacetic Acid (2,4-D) levels. The experiment had six treatments (control, 1mgl1 2,4-D, 2mgl1 2,4-D, 3mgl1 2,4-D, 4mgl1 2,4-D, and 5mgl1 2,4-D,) including control with each replicated three times and the percentage taken with callus induction frequency which ranged from 32% to 80%. Meanwhile maximum callus among the genotypes were noticed in varieties 8 followed by varieties 27, 28 and 7 with respective callus induction percentages of 79.99%, 79.99% and 77.33%, with minimum callus frequency of 32% was recorded by varieties 19, while 13 had callus induction potential of 36%. The best callus production was recorded at the treatment levels of 5mgl-1 (78.878%), callus recorded at 5mgl-1 were more granular and morphogenic in nature. However higher mean values for days to callus were at varieties 5 (6.60), 4 (6.40), 21 (6.40) and 26 (6.40), with the least mean values for days to callus at varieties 8 (5.40) and 7 (5.60), while the least mean values for days to callus was recorded at 5mgl-1 (4.69) and levels of 2, 4-D, while the higher mean values for days to callus was scored at 2mgl-1 (7.06) levels of 2, 4-D. The weight ranged from 62.24mg mean value to 85.14mg mean values. Genotype 8 had the maximum mean weight across treatments (85.14mg) followed by genotypes 7 (82.5mg), 28 (81.56mg) and 2 (81.46mg) respectively while the minimum weight values were noticed in genotypes 3 (62.24mg), 26 (64.48mg) and (64.9mg). However the maximum weight of callus according to treatments was observed at the level of 5mgl-1 of 2, 4-D with mean value 105.7mg f. while the minimum mean weight values were recorded at 1mgl-1 (31.1mg) 2, 4-D.

83-92

Authors: Valantina Al Bitar, Shaza Al Laham, Rana Attieh

Methylsulfonylmethane (MSM) is an organic sulfur-containing natural compound without any toxicity. MSM may have anti-inflammatory and free radical scavenging activity. The present work was done to investigate the possible protective effects of methylsulfonylmethane on acetic acid-induced colitis in rats. Colitis was induced by intracolonic injection of 5% acetic acid. Several parameters including macroscopic score, histopathological and biochemical parameters such as myeloperoxidase activity and glutathione levels were measured following standard assay procedures. Results showed that MSM decreased macroscopic and microscopic colonic damage scores caused by administration of acetic acid. MSM also significantly reduced colonic levels of MPO and increased the levels of GSH compared to acetic acid-induced colitis group. It seems that MSM as a natural product was able to give a nearly complete protection against acetic acid-induced colitis.

99-111

Authors: Komsok T. Joël, Chelea Matchawe, Kouamouo Jonas, Sipowo T. V. Raissa, Fekam Fabrice, Ngoupayo Joseph

For decades, plants have been a source of inspiration for new drugs. Almost all ancient civilisations and cultures depended entirely or partially on phytotherapy because of its effectiveness, accessibility, availability and dose-related low toxicity. Thus, the know-how of traditional healers is a starting point for phytochemical and pharmacological investigation of these natural medicines. Therefore, the present study was aimed at studying phytochemical, cytotoxic, anti-haemolytic and antioxidant activities of leaf and bark extracts of Azadirachta indica. The leaves and bark of A. indica were harvested, dried and reduced to powder. Then the powder was extracted in different solvents (distilled water, ethanol and ethanol/water 70% (v / v)). The resulting extracts were subjected to phytochemical analysis by colorimetric reactions followed by the cytotoxicity test on the Vero cell line using colorimetric method at MTT. The antihemolytic activity of the promising extracts was performed on the red blood cells and the antioxidant properties of the extracts were evaluated by the DPPH radical scavenging method and Ferric ion reduction. The results show that the extraction yields ranged from 5.02 to 20.7%. The phytochemical screening revealed the presence of alkaloids, polyphenols, saponosides and steroids. All the extracts were non-cytotoxic with CC50 values ranging from 169.73 to greater than 1000 μg/ml and two of these exhibited antihemolytic activities with 62% and 57% protection percentages. The extracts had DPPH IC50 values ranging from 14.933 to 95.360 μg/mL. The ferric ions reducing power (OD) of the different extracts ranged from 0.15805 to 3.40545. The activities of Azadirachta indica extracts indicate that this plant is a potential source of active compounds.

116-124

Authors: Kelechi E. Onwuka, Kalu S. Eze, Christopher U. Aghalibe, Igwe J.C., Ezeaku I.I.

The effect of temperature on the equilibrium adsorption of Malachite green dye from aqueous solution using rectorite was studied. The equilibrium adsorption data were analyzed using three widely applied isotherms; Langmuir, Freundlich, and Redlich-Peterson isotherm. A nonlinear method was used for comparing the best fitting of the isotherms. Best fits were found to be Redlich-Peterson isotherm. Thermodynamic parameters, such as ΔG°, ΔH°, and ΔS°, were calculated using adsorption equilibrium constant obtained from the Langmuir isotherm. Results suggested that the Malachite green adsorption on rectorite was an endothermic and spontaneous process.

1-10

Authors: Abdel Karim, M., Mawahib, A., Salah, H.

Eucalyptus oil has been used traditionally for bronchitis and asthma. The oil which is plentiful in leaves has also been used against diabetes, cystitis, malaria, kidney disorders, leucorrhoea and laryngitis. The anticancer activity of this oil has been studied in vivo. The GC-MS analysis revealed the presence of 42 components. Major constituents are: eucalyptol (21.24%), decahydro-1,1,7-trimethyl-4-methylene - 1H-cycloprop[e]azulen-7-ol (12.59 %) , p-cymene (12.11 %), decahydro-1,1,4,7-tetramethyl-1H-cycloprop[e]azulen-4-ol (11.64 %) and β-phellandrene (8.59%). The oil was evaluated for antibacterial activity via the agar diffusion bioassay against: Gram positive: Staphylococcus aureus and Gram negative: Escherichia coli using ampicillin and gentamicin as positive controls. At a concentration of 100mg/ml the oil showed moderate activity against Escherichia coli and Staphylococcus aureus.

17-19

Authors: L. Kh. Sharipova, M. S. Orzieva, R.A. Amonov, F. R. Juraeva

The article reveals the cardiovascular system in healthy and visually impaired children. The main types of adaptation are analyzed.

25-38

Authors: Omyma K. Radwan, Salwa K. El-Nabarawy,Rasha A. El-Sayed.,Suzan F. El-Sisi, Fatma F. Abd El-Salam

The liver is one of the most important organs in the body, performing a fundamental role in the regulation of diverse processes, among which the metabolism, secretion, storage, and detoxification of endogenous and exogenous substances are prominent. Due to these functions, hepatic diseases continue to be among the main threats to public health. Glucocorticoids are among the most utilized medications around the world, dexamethasone (DEX) is one of the most potent synthetic glucocorticoid that associated with several side effects especially on the liver. Many natural products and plant extracts become a new trend in the traditional and complementary medicines. Bee Venom (BV) and Echinacea Purpurea (EP) were used for their chemo-protective and immunomodulatory activities. Aims and Objectives: To study the protective effect of BV and EP and their combination on the liver status and liver cell energy against DEX treatment in adult female albino rats. Method: For performing the present work fifty-six adult female albino (150 ± 20 gm) were randomly divided into 7 groups (n=8). G1: control group; G2: treated with DEX (5mg i.p /kg BW/day) for three days; G3: orally treated with BV (150 µg/kg BW/day) for 28 days; G4: orally treated with EP (30 mg /kg B.W/day) for 28 days; G5: treated with both DEX+BV; G6: treated with both DEX+EP; G7: treated with DEX+BV+EP, all with the same aforementioned doses and durations. Liver injury was assessed biochemically and histologically. Results: Administration of DEX (5mg i.p /kg BW/day) for three days resulted in elevated liver enzymes, protein synthesis and reduction in liver cell energy. On the other hand oral administration of BVfor 28 days (150 µg/kg B.W/day) and EP (30 mg /kg B.W/day) for 28 days with DEX resulted in a great normalization in the levels of liver’s protein and significantly decreased ALT and AST serum levels as compared to DEX group. In addition, both BV and EP resulted in ameliorated effect on liver cell energy by increasing their levels in comparing with DEX group. Conclusion: The current findings suggested that both BV and EP or their combination, may exert beneficial protective effects against the negative deteriorative influences during DEX treatment through ameliorating liver status and liver cell energy prominence. In conclusion, treatment with DEX resulted in mild liver injuriousness, whose certain manifestations were alleviated on co-treatment with BV and EP biochemically and histologically. Based on these results, patients should be monitored periodically liver functions during DEX therapy.

44-46

Authors: L. Kh. Sharipova, G. G., Yuldasheva, M. S. Orzieva, F. R. Juraeva

The article reveals the influence of biological, social and hygienic factors on the formation of visual pathology in children.

53-55

Authors: Z. A. Akhmedova, Kh. P. Kenjaeva

The article reveals the importance of Ibn Sina's medical heritage. The main aspects of the revival of methods of Oriental medicine are analyzed

62-70

Authors: Loveth N. Emembolu, Dominic O. Onukwuli

Newbouldia leavis (NL) and Pepper fruit (PF) leaf extracts were investigated for their ability to impede corrosion of zinc in 0.5 M HCl by gravimetric and thermometric techniques. The results obtained showed that different concentrations of the (NL and PF) extracts hinder the corrosion of zinc in 0.5 M HCl. Inhibition efficiency of each extract varies with concentration, time of immersion and temperature. The values of activated energies were higher in the suppressed corrosion reaction of zinc than the values calculated for the blank. The thermodynamic study shows that the NL and PF leaf extracts adsorbed on the surface of zinc was spontaneous and follows Frumkin adsorption isotherm. Physical adsorption mechanism has been proposed for adsorption of these inhibitors on the surface of zinc metal.

81-83

Authors: O. I. Jabbarova

Cellular and humoral immunity on antigene Hyal is studied at mice-hybrids. Hyal possessed low immunogenic properties.Use DS,PO as immunoadjuvant towards Hyal raised it immunogenic the activity expressed in strengthening humoral of the immune response on Hyal at mice.DS also was capable to activate specific cellular reactions DTH on Hyal.

91-102

Authors: Hülya Akgün, Betül Kaya, Yusuf Mulazim, Banu Kesanli, Hande Sipahi, Beril Kadıoğlu, Barkın Berk, Sevde Nur Biltekin

In this study, ten substituted N - ([1,3-dioxoindolin-2-yl] phenyl] sulfonyl) structures (compound 1-10), which seven of them were original synthesized using conventional and microwave synthesis methods. In the first method the cis-1,2-cyclohexanecarboxylic anhydride and sulfa derivatives reacted under reflux for 2-3 hours in acetic acid. In the second method the cis-1,2-cyclohexanecarboxylic anhydride and sulfa derivatives were dissolved in DMF and radiated by microwave. Structure elucidation of the synthesized compounds were confirmed by UV, IR 1H-NMR, 13C-NMR with mass spectral methods and elemental analysis method. Anticancer activities of the compounds were studied by MTT assay. Synthesized compounds generally showed moderate or no cytotoxic activity against MCF7 (human breast cancer cell line). Among them, N-([1,3-Dioxoindolin-2-yl)phenyl]sulfonyl)6-amino-4,5-dimethoxypyrimidine (7), N-([1,3-Dioxoindolin-2-yl)phenyl]sulfonyl)-2-aminothiazole (3) and N-([1,3-Dioxoindolin-2-yl)phenyl]sulfonyl)aminopyrimidine (10) presented activity against MCF7 cancer cell lines with IC50 values of 71.5  3.01μM, 87.9  2.34and 89.3  2.05 μM, respectively. Anti-inflammatory activity of the compounds were tested against LPS-induced nitrite production in RAW 264.7cell line. The compounds4-(1,3-dioxohexahydro-2H-isoindol-2-yl)-N-(5-methyl-1,2-oxazol-3-yl) benzenesulfonamide(1), 4-(1,3-dioxohexahydro-2H-isoindol-2-yl)-N-(6-methoxypyridazin-3-yl)benzenesulfonamide (4) and 4-(1,3-Dioxohexahydro-2H-isoindol-2-yl)benzenesulfonamide (9) showed nitrite production inhibitory activity 24.43 ± 3.16, 9.73 ± 1.04, and 6.44 ± 2.48 µM, respectively. Compound 4 exhibited the highest anti-inflammatory activity by suppressing the NO production. These compounds might be candidate to inflammatory therapy for further development.

112-122

Authors: Mohammad T. Hossain, Md. Asadujjaman, Md. Imran N. Manik, Md A. Matin, Reefat Z. Chowdhury, Md H. Rashid

Bioactive alkaloids, glycosides and saponins are phytoconstituents and belong to the secondary metabolites of plants kingdom. These constituents possesses many pharmacological properties such as antioxidant activity, antimicrobial effect, modulation of detoxification of enzymes and hormone metabolism, stimulation of the immune system, decrease of platelet aggregation procedure, possess antidiabetic, antihypertensive, antidepressants, analgesics and anticancer etc. properties. Now a days these compounds have received great attention worldwide as the sources of novel agents, important pharmaceutical intermediates and significant starting materials for a lot of synthetics or semi synthetics drugs due to potent pharmacological activities, higher safety profile, low toxicity and cost effectiveness. So the current study is designed to focus on the accumulation of sufficient information’s about the above mentioned phytoconstituents regarding their pharmacological effects and mechanisms of action along with other significant properties.

128-130

Authors: N. N. Kazakova

The article reveals the presence of the features of the child's body according to the medical heritage of Ibn Sina. The features of women's milk in the “Canon of medical science” Abu Ali Ibn Sina”are analyzed.

1-10

Authors: Benson Muriuki Githaiga, Eliud Mugu Gathuru, Paul Njenga Waithaka, Mercy Maloba

Mangoes are an important source of vitamins all over the world. However, their production has been endangered by Colletotrichum gloeosporioides that causes anthracnose of mangoes. This study was aimed at isolating the fungus from infected mangoes followed by testing the sensitivity of the fungus to essential oils from eucalyptus, sage and rosemary plant. Infected mango fruits were acquired from Njokerio Market near Egerton University. Fungal pathogens were isolated from the infected fruits using potato dextrose agar. Essential oils were extracted from eucalyptus, sage and rosemary plant using distillation method. Sensitivity of Colletotrichum gloeosporioides to the extracted essential oils was carried out using agar well technique. The colonies of Colletotrichum gloeosporioides had dense whitish mycelium with black and orange color fruiting bodies. The spores were smooth, hyaline and sub cylindrical with round end spores. The conidia were cylindrical in shape, hyaline in colour and the size was 13.4 – 24 x 4.0 – 5.9µm. The appresoria were obovate to clavate in shape, brown in colour and 6.7 – 19.8 x 3.8 – 11.9µm in size.There was a relationship between heating time and yield of essential oils in rosemary (r=0.99) and leaves (r=0.99). Conversely, there was no significant difference in the percentage yield of essential oils from eucalyptus, sage and rosemary (P=0.057). There was no significant difference in the percentage composition of the different compounds in the essential oils extract from eucalyptus, sage and rosemary (F=0.48 P=0.62). The zone of inhibition of essential oils obtained from eucalyptus against Colletotrichum gloeosporioides varied from 19±3mm to 21±1mm, sage (18±1mm-19±2mm) and rosemary (17±1mm-19±1mm). The minimum inhibition of essential oils from eucalyptus leaves was120±0.01mg/ml, sage (241±0.00mg/ml) and rosemary (230±0.02mg/ml). The minimum fungicidal concentration of essential oils from eucalyptus was (120±0.01mg/ml), sage (241±0.00) and rosemary (230±0.02). The essential oils from eucalyptus, sage and rosemary have bioactive compounds that have antifungal properties againstColletotrichum gloeosporioides.

19-23

Authors: Khalid Salem Baayou, Mohammed Hussain Patel, Osama Al Okabi, Bashier Ali Alhanash

To evaluate the value of using trans- oral rigid endoscopic examination of nasopharynx after conventional curettage adenoidectomy for complete removal and prevention of recurrence. A Prospective study of 50 children with adenoid hypertrophy was done at Misurata Central Hospital. They presented clinically with symptoms of nasal obstruction, mouth breathing and snoring confirmed radiologically with plan x ray nasopharynx lateral view, of both sex ageing from 1.5 years to 15 years, with mean age of 6.9 years and S.D± 3.44, carried out in a period of 6months from January 2015 Patients were divided into two groups. Group A underwent conventional curettage adenoidectomy only, while group B underwent a conventional curettage adenoidectomy and at the end trans-oral endoscopic visualization of nasopharynx done, using 70 degree rigid endoscope to detect and subsequently to remove any residual adenoid tissue transorally by curettage. In group B, at the end of conventional curettage adenoidectomy, endoscopic examination of nasopharynx detected the remnant of adenoid tissue in 13 patients, 8 patients(61.54%) in roof, 2 patients(15.38%) at Eustachian tube opening, 2patients(15.38%) over posterior wall, and 1 patient(7.70%) posterior wall+ roof indicate that conventional curettage used alone failed to remove the adenoid tissue completely. There was a significant difference in rate of adenoid recurrence between both groups was statistically significant (P =0.04) (6months postoperatively).At the end of 6 months postoperatively 16 patients (64%) in group A and 23 patients (92%) in group B were symptoms free. Examination of nasopharynx of patients with persistence of symptoms of nasal obstruction, 9 patients (36%) in Group A showed the adenoid recurrence, 7patients (78%) in roof and 2 patients (22%) in posterior wall. While 2 patients (8%) in group B with persistence of symptoms of nasal obstruction did not revealed any recurrence of adenoid tissue but showed hypertrophied inferior turbinate. Conventional curettage adenoidectomy missed the residual adenoid tissue, Rigid endoscopic examination of nasopharynx is necessary after conventional adenoidectomy for detecting any residual adenoid tissue to remove subsequently thus reducing the recurrence.

27-36

Authors: Enenche, E. Daniel, Ogo, A. Ogo, Obochi, O. Godwin, Afolayan S. Sunday, Idoko O. Blessing

Natural and biosynthesized phytocompounds have gained significant attention in the food industry because of their non-controversial health and safety benefits as compared with chemically synthesized antioxidants. However, no natural biosynthesized phyto-compounds has been commercially available and used in routine food processing. This study evaluates the antioxidant property of Sidaacuta plant commonly used by many locals in storing cooking oils. The ethanolic leaf extract of this plant was evaluated for its antioxidant potential, total phenolic (TP) and total flavonoid (TF) contents using standard procedures. The extract was added to groundnut oil at four different concentrations of 100 mg/L, 200 mg/L, 400 mg/L and 800 mg/L and stored over a six-month period, while chemical properties of oil including peroxide value (PV), anisidine value (AnV), acid value (AV) and iodine value (IV) were checked on a monthly basis. The results showed that the extract had significant antioxidant effect for DPPH radical scavenging activity (27.4800±0.0173 IC50 % inhibition), β-carotene linoleic antioxidant activity (29.7267±0.0251 IC50 % inhibition), ORAC (6.1067±0.0115 µ Mol TE/g) and FRAP (291.0367±0.0305 µ Mol Fe2+/L). Total phenolic content expressed in tannic acid equivalents was 27102.365±10.189 µg/ml, while total flavanoid content expressed in quercetine equivalents was 1024.783±5.569 µg/ml. The addition of the leaf extract to oils showed significant retardation of oxidation compared to samples without the extract. The findings reveal that the use of Sidaacuta as a natural antioxidant to prevent vegetable oils oxidation if properly harnessed can be a good alternative to synthetic antioxidants.

46-48

Authors: A.N. Zulfikorov, N.I. Khudoykulova, Sh.R. Davronova, B.S. Shakirov, D.B. Sultanova

The article analyzes the process of restoration of reproductive function during breastfeeding.

53-56

Authors: Derouicha Matmour, Elhachemi Medjadji, Mohammed Bousselham, Toumi Houari

Chlorobutanol is an active pharmaceutical ingredient used in therapeutic for many years as an antiseptic, analgesic and local anesthetic. It has other properties: hypnotic, anti-inflammatory and anti-emetic. It’s used as conservative in some pharmaceutical preparations because it has antibacterial and antifungal properties. We synthesized this active pharmaceutical ingredient in Therapeutic laboratory of pharmacy department of Sidi Bel-Abbes by Referenced method based on the addition of chloroform with acetone under the influence of chemical catalyst (potassium hydroxide) using the distillation assembly. The second synthesis using the optimized method improves the yield of 20 %. The synthesized product was controlled according to the requirements of the European Pharmacopoeia 8th edition: the organoleptic characteristics, solubility, colorimetric reactions and the degree of coloring were positive; its melting point is 78 °C; its water content is estimated to 4.66% and its purity is equal to 98.27%.

60-68

Authors: Abdel Karim, M., Mawahib, A., Salah, H.

Eucalyptus oil has been used traditionally for bronchitis and asthma. The oil which is plentiful in leaves has also been used against diabetes, cystitis, malaria, kidney disorders, leucorrhoea and laryngitis. The anticancer activity of this oil has been studied in vivo. The GC-MS analysis revealed the presence of 42 components. Major constituents are : eucalyptol (21.24%), decahydro-1,1,7-trimethyl-4-methylene - 1H-cycloprop[e]azulen-7-ol (12.59 %), p-cymene (12.11 %), decahydro-1,1,4,7-tetramethyl- 1H-cycloprop[e]azulen-4-ol (11.64 %) and β-phellanderene (8.59%). The oil was evaluated for antibacterial activity via the agar diffusion bioassay against: Gram positive: Staphylococcus aureus and Gram negative: Esherichia coli using ampicilin and gentamycin as positive controls. At a concentration of 100mg/ml the oil showed moderate activity against Escherichia coli and Staphylococcus aureus.

72-83

Authors: Yaprak Yıldız, HülyaAkgün, Hande Sipahi, İnci Deniz, Barkın Berk

A series of N1,N2-bis [(2-substitutedphenyl)ethyl]phthalamide (compounds 1-10) and 3-nitro-N1, N2-bis [(2-substitutedphenyl)ethyl]phthalamide (compounds 11-20) were synthesized. Their structures and purity were analyzed by IR, 1H-NMR spectra and elemental analysis. The compounds were evaluated for their in vitro cytotoxicity against the MCF7 and Hep3B cancer cell lines. Cytotoxicity screening revealed that N1,N2-bis[2-(2,4-dichlorophenyl)ethyl]phthalamide (compound 5), 3-nitro-N1,N2-bis[2-(2,4-dichlorophenyl) ethyl]phthalamide (compound 15) and 3-nitro-N1,N2-bis[2-(2-fluorophenyl)ethyl]phthalamide (compound 16) had the highest activity. The synthesized compounds were also screened for their antimicrobial activity against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. Among the compounds, N, N’-bis[2-(4-chlorophenyl)ethyl]phthalamide (compound 4), 3-Nitro-N,N’-bis[2-(2-chlorophenyl) ethyl]phthalamide (compound 12), 3-Nitro-N,N’-bis[2-(4-chlorophenyl)ethyl] phthalamide (compound 14), and 3-Nitro-N,N’-bis[2-(2,4-dichlorophenyl)ethyl]phthalamide (compound 15) exhibited good activity. The prediction of drug-likeness, molecular and ADME properties of the compounds were also examined during the study.

90-97

Authors: Emmanuel Enyi1, Peter M. Eze, Uchenna C. Ogwaluonye, Ezinne S. Iloh, Ogechukwu L. Nwankwo, Festus B. C. Okoye, Charles O. Esimone

This study was undertaken to investigate the biological properties of secondary metabolites of two endophytic fungi (code names: GA and GC) isolated from Psidium guajava leaves. Isolation of the endophytic fungi, fermentation and extraction of fungal secondary metabolites was carried out using standard procedures. The fungal extracts were screened for antimicrobial, antioxidant and cytotoxic activities using the agar well diffusion, DPPH and MTT assay methods respectively. Also, the extracts were subjected to high performance liquid chromatography (HPLC) analysis for the identification of the constituents. Result of the antimicrobial assay revealed that at 1 mg/mL, the crude extract of GA displayed broad spectrum antibacterial activity against all the test bacteria - E. coli, S. aureus, B. subtilis and S. typhi with inhibition zone diameter (IZD) of 5, 6, 5 and 4 mm respectively. Extract of GC showed antibacterial activity only against S. aureus, with IZD of 7 mm. In the DPPH antioxidant assay, GA and GC extracts at 100 µg/mL displayed average antioxidant activity with inhibitions of 56.7 and 55.2% respectively, which is comparable to the 63.7% inhibition recorded for the positive control ascorbic acid. At 10 µg/mL, GA and GC extracts showed poor cytotoxic activities against mouse lymphoma cells L5178Y, with inhibitions of 38.5 and 12.4% respectively. HPLC analysis of GA extract revealed the presence of citreoisocoumarinol, while acropyrone and citreoisocoumarin were detected in the extract of GC. The results of this study indicate that endophytic fungi isolated from leaves of P. guajava produced secondary metabolites that can play vital role in the development of drugs for effective treatment of diseases.

103-110

Authors: Alice Piperea-Șianu, Dan Piperea-Șianu, Alexandru G. Croitoru, Adela-Maria Ceau

Tobacco smoke contains a complex mixture of over 5000 toxic substances, of which at least 69 are carcinogenic, being also involved in other pathologies such as cardiovascular and pulmonary diseases. The purpose of this review is to highlight the toxicological profile of some of the most harmful xenobiotics in tobacco smoke: NNK (tobacco-specific nitrosamine - Nicotine-derived nitrosamine ketone), benzo[a]pyrene and carbon monoxide.