Muhammad Taher

Antimicrobial activity and essential oils of Curcuma aeruginosa, Curcuma mangga, and Zingiber cassumunar from Malaysia

OBJECTIVE To analyze the chemical composition of the essential oils of Curcuma aeruginosa (C. aeruginosa), Curcuma mangga (C. mangga), and Zingiber cassumunar (Z. cassumunar), and study their antimicrobial activity. METHODS Essential oils obtained by steam distillation were analyzed by gas chromatography-mass spectrometry (GC-MS). The antimicrobial activity of the essential oils was evaluated against four bacteria: Bacillus cereus (B. cereus), Staphylococcus aureus (S. aureus), Escherichia coli (E. coli), and Pseudomonas aeruginosa (P. aeruginosa); and two fungi: Candida albicans (C. albicans) and Cyptococcus neoformans (C. neoformans), using disc-diffusion and broth microdilution methods. RESULTS Cycloisolongifolene, 8,9-dehydro formyl (35.29%) and dihydrocostunolide (22.51%) were the major compounds in C. aeruginosa oil; whereas caryophyllene oxide (18.71%) and caryophyllene (12.69%) were the major compounds in C. mangga oil; and 2,6,9,9-tetramethyl-2,6,10-cycloundecatrien-1-one (60.77%) and α-caryophyllene (23.92%) were abundant in Z. cassumunar oil. The essential oils displayed varying degrees of antimicrobial activity against all tested microorganisms. C. mangga oil had the highest and most broad-spectrum activity by inhibiting all microorganisms tested, with C. neoformans being the most sensitive microorganism by having the lowest minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) values of 0.1 μL/mL. C. aeruginosa oil showed mild antimicrobial activity, whereas Z. cassumunar had very low or weak activity against the tested microorganisms. CONCLUSIONS The preliminary results suggest promising antimicrobial properties of C. mangga and C. aeruginosa, which may be useful for food preservation, pharmaceutical treatment and natural therapies.

Antimicrobial activity of mangrove plant (Lumnitzera littorea).

OBJECTIVE To investigate the antimicrobial activities of n-hexane, ethyl acetate and methanol extracts of the leaves of Lumnitzera littorea (L. littorea) against six human pathogenic microbes. METHODS The antimicrobial activity was evaluated using disc diffusion and microdilution methods. RESULTS The antimicrobial activities of the crude extracts were increased with increasing the concentration. It is clear that n-hexane extract was the most effective extract. Additionally, Gram positive Bacillus cereus (B. cereus) appear to be the most sensitive strain while Pseudomonas aeruginosa (P. aeruginosa) and the yeast strains (Candida albicans (C. albicans) and Cryptococcus neoformans (C. neoformans)) appear to be resistance to the tested concentrations since no inhibition zone was observed. The inhibition of microbial growth at concentration as low as 0.04 mg/mL indicated the potent antimicrobial activity of L. littorea extracts. CONCLUSIONS The obtained results are considered sufficient for further study to isolate the compounds responsible for the activity and suggesting the possibility of finding potent antibacterial agents from L. littorea extracts.

In vitro antimicrobial activity of mangrove plant Sonneratia alba

OBJECTIVE To investigate the antimicrobial property of mangrove plant Sonneratia alba (S. alba). METHODS The antimicrobial activity was evaluated using disc diffusion and microdilution methods against six microorganisms. Soxhlet apparatus was used for extraction with a series of solvents, n-hexane, ethyl acetate and methanol in sequence of increasing polarity. RESULTS Methanol extract appeared to be the most effective extract while n-hexane extract showed no activity. The antimicrobial activities were observed against the gram positive bacteria Staphylococcus aureus (S. aureus) and Bacillus cereus (B. cereus), the gram negative Escherichia coli (E. coli) and the yeast Cryptococcus neoformans. Pseudomonas aeruginosa and Candida albicans appeared to be not sensitive to the concentrations tested since no inhibition zone was observed. E. coli (17.5 mm) appeared to be the most sensitive strain followed by S. aureus (12.5 mm) and B. cereus (12.5 mm). CONCLUSIONS From this study, it can be concluded that S. alba exhibits antimicrobial activities against certain microorganisms.

Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer and osteoporosis in post-menopausal women, shows poor oral bioavailability of 2%. The aim of this study was to develop, statistically optimize, and characterize raloxifene hydrochloride-loaded transfersomes for transdermal delivery, in order to overcome the poor bioavailability issue with the drug. A response surface methodology experimental design was applied for the optimization of transfersomes, using Box-Behnken experimental design. Phospholipon® 90G, sodium deoxycholate, and sonication time, each at three levels, were selected as independent variables, while entrapment efficiency, vesicle size, and transdermal flux were identified as dependent variables. The formulation was characterized by surface morphology and shape, particle size, and zeta potential. Ex vivo transdermal flux was determined using a Hanson diffusion cell assembly, with rat skin as a barrier medium. Transfersomes from the optimized formulation were found to have spherical, unilamellar structures, with a homogeneous distribution and low polydispersity index (0.08). They had a particle size of 134±9 nM, with an entrapment efficiency of 91.00%±4.90%, and transdermal flux of 6.5±1.1 μg/cm2/hour. Raloxifene hydrochloride-loaded transfersomes proved significantly superior in terms of amount of drug permeated and deposited in the skin, with enhancement ratios of 6.25±1.50 and 9.25±2.40, respectively, when compared with drug-loaded conventional liposomes, and an ethanolic phosphate buffer saline. Differential scanning calorimetry study revealed a greater change in skin structure, compared with a control sample, during the ex vivo drug diffusion study. Further, confocal laser scanning microscopy proved an enhanced permeation of coumarin-6-loaded transfersomes, to a depth of approximately160 μM, as compared with rigid liposomes. These ex vivo findings proved that a raloxifene hydrochloride-loaded transfersome formulation could be a superior alternative to oral delivery of the drug.

Antioxidant and cytotoxic properties of two sea cucumbers, Holothuria edulis Lesson and Stichopus horrens Selenka

Sea cucumbers are marine invertebrates of the phylum of Echinodermata that have been used in Asian traditional medicine since ancient times. This study was conducted to investigate the antioxidant and cytotoxic properties of aqueous and organic extracts from two sea cucumber species, Holothuria edulis Lesson (Holothuriidae) and Stichopus horrens Selenka (Stichopodidae). Antioxidant activities of the extracts were evaluated by DPPH· and β-carotene bleaching assays, while MTT and trypan blue exclusion assays were used to demonstrate the cytotoxic effects of the extracts against two human cancer cell lines, non-small cell lung cancer cells (A549) and esophageal cancer cells (TE1). The results showed that both aqueous and organic extracts of H. edulis were able to scavenge DPH radical (IC50 at 2.04 mg/ml and 8.73 mg/ml, respectively). Aqueous and organic extracts of S. horrens inhibited 79.62% and 46.66% of β-carotene oxidation by linoleate free radical. On the other hand, the organic extract of S. horrens exhibited the highest cytotoxic effects against A549 and TE1 cancer cells giving IC50 at 15.5 and 4.0 μg/ml, respectively. In conclusion, the present study revealed that H. edulis and S. horrens contain promising levels of antioxidant and cytotoxic natural products that might be used for cancer prevention and treatment.

Apoptosis, antimicrobial and antioxidant activities of phytochemicals from Garcinia malaccensis Hk.f

OBJECTIVE To study the chemical constituents of stembark of Garcinia malaccensis (G. malaccensis) together with apoptotic, antimicrobial and antioxidant activities. METHODS Purification and structure elucidation were carried out by chromatographic and spectroscopic techniques, respectively. MTT and trypan blue exclusion methods were performed to study the cytotoxic activity. Antibacterial activity was conducted by disc diffusion and microdilution methods, whereas antioxidant activities were done by ferric thiocyanate method and DPPH radical scavenging. RESULTS The phytochemical study led to the isolation of α,β-mangostin and cycloart-24-en-3β-ol. α-Mangostin exhibited cytotoxic activity against HSC-3 cells with an IC(50) of 0.33 μM. β- and α-mangostin showed activity against K562 cells with IC(50) of 0.40 μM and 0.48 μM, respectively. α-Mangostin was active against Gram-positive bacteria, Staphylococcus aureus (S. aureus) and Bacillus anthracis (B. anthracis) with inhibition zone and MIC value of (19 mm; 0.025 mg/mL) and (20 mm; 0.013 mg/mL), respectively. In antioxidant assay, α-mangostin exhibited activity as an inhibitor of lipid peroxidation. CONCLUSIONS G. malaccensis presence α- and β-mangostin and cycloart-24-en-3β-ol. β-Mangostin was found very active against HSC-3 cells and K562. The results suggest that mangostins derivatives have the potential to inhibit the growth of cancer cells by inducing apoptosis. In addition, α-and β-mangostin was found inhibit the growth of Gram-positive pathogenic bacteria and also showed the activity as an inhibitor of lipid peroxidation.

Isolation of fucoxanthin and fatty acids analysis of Padina australis and cytotoxic effect of fucoxanthin on human lung cancer (H1299) cell lines

Fucoxanthin has been successfully isolated from species of Malaysian brown seaweed, namely Padina australis . The purity of the fucoxanthin is >98% as indicated by high performance liquid chromatography analysis. This seaweed also contains a considerable amount of unsaturated fatty acids. Thirteen fatty acids were detected with gas chromatography. However, fatty acid methyl ester (FAMEs) of eicosapentanoic acid (C20:5n-3), arachidonic acid (C20:4n-6), linoleic acid (C18:2n-6) and alpha-linolenic acid (C18:3n-3) contents of P. australis were found to be 2.06, 9.50, 6.37, and 2.83%, respectively. For saturated fatty acids, palmitic acid (C16:0) was found to be the major fatty acid with about 23.97%. Furthermore, data obtained from the methyl thiazolyl tetrazolium (MTT) assay indicated that fucoxanthin reduced the viability of H1299 cell lines, showing an IC 50 value of 2.45 mM. Key words : Brown seaweed, Padina australis , fucoxanthin, fatty acid methyl ester, H1299 cell lines, human lung cancer, MTT assay.

ANALYSIS OF FUCOXANTHIN CONTENT AND PURIFICATION OF ALL-TRANS-FUCOXANTHIN FROM Turbinaria turbinata AND Sargassum plagyophyllum BY SiO2 OPEN COLUMN CHROMATOGRAPHY AND REVERSED PHASE-HPLC

Reversed phase-high performance liquid chromatography (RP-HPLC) was used to analyze fucoxanthin content of two species of Malaysian brown seaweeds, Turbinaria turbinate, and Sargassum plagyophyllum. The fucoxanthin contents of T. turbinata and S. plagyophyllum were 0.59 ± 0.08 and 0.71 ± 0.01 mg/g dry-weight, respectively. Ultraviolet spectrum of fucoxanthin showed the maximum absorbance at 450 nm. Furthermore, the HPLC chromatograms of purified all-trans-fucoxanthin from showed one major peak with a retention time of 7.8 min.

Apoptotic activities of thymoquinone, an active ingredient of black seed (Nigella sativa), in cervical cancer cell lines.

Thymoquinone (TQ) is the main constituent of black seed (Nigella sativa, spp) essential oil which shows promising in vitro and in vivo anti-neoplastic activities in different tumor cell lines. However, to date there are only a few reports regarding the apoptotic effects of TQ on cervical cancer cells. Here, we report that TQ stimulated distinct apoptotic pathways in two human cervical cell lines, Siha and C33A. TQ markedly induced apoptosis as demonstrated by cell cycle analysis in both cell lines. Moreover, quantitative PCR revealed that TQ induced apoptosis in Siha cells through p53-dependent pathway as shown by elevated level of p53-mediated apoptosis target genes, whereas apoptosis in C33A cells was mainly associated with the activation of caspase-3. These results support previous findings on TQ as a potential therapeutic agent for human cervical cancer.

Microencapsulation of alpha-mangostin into PLGA microspheres and optimization using response surface methodology intended for pulmonary delivery

Abstract Documented to exhibit cytotoxicity and poor oral bioavailability, alpha-mangostin was encapsulated into PLGA microspheres with optimization of formulation using response surface methodology. Mixed levels of four factors Face central composite design was employed to evaluate critical formulation variables. With 30 runs, optimized formula was 1% w/v polyvinyl alcohol, 1:10 ratio of oil to aqueous and sonicated at 2 and 5 min time for primary and secondary emulsion, respectively. Optimized responses for encapsulation efficiency, particle size and polydispersity index were found to be 39.12 ± 0.01%, 2.06 ± 0.017 µm and 0.95 ± 0.009, respectively, which matched values predicted by mathematical models. About 44.4% of the encapsulated alpha-mangostin was released over 4 weeks. Thermal analysis of the microspheres showed physical conversion of alpha-mangostin from crystallinity to amorphous with encapsulated one had lower in vitro cytotoxicity than free alpha-mangostin. Aerodynamic diameter (784.3 ± 7.5 nm) of this alpha-mangostin microsphere suggests suitability for peripheral pulmonary delivery.