Bicarbonate In-Vitro Effect on Beta-Hematin Inhibition by Artemisia sieberi Aqueous Infusion

Malaria is still considered the most threatening disease in Africa. Plasmodium; the malaria parasite, forms during its intra-erythrocytic stage a pigment called hemozoin, which acts as a protection shield against oxygen radical-mediated stress that leads to parasite’s death. Many drugs targeting hemozoin formation such as chloroquine and amodiaquine, but recently strains of Plasmodium have gained resistance to such drugs. Artemisia sieberi stem and leaf water infusion extract compared with A. sieberi bicarbonate aqueous infusion were tested using a semi-quantitative in-vitro method based on the inhibition of ferriprotoporphyrin IX (FP) bio- mineralization developed by Deharo et al. to reveal the differences in antimalarial activity. Reversed phase preparative liquid chromatography coupled to Photo Diode Array (HPLC-PDA) detector was also used to explain this dissimilarity in antimalarial activity. We found that A. sieberi bicarbonate aqueous infusion inhibits the formation of β-hematin better than standard water infusion. The bicarbonate addition increases the extraction of more compounds as the chromatographic HPLC results revealed. Other Artemisia plants (A. vulgaris and A. herba alba) were also tested to explore any inhibition effects

Cinnamon bark water-infusion as an in-vitro inhibitor of β-hematin formation

Malaria remains one of the prominent public health problems that lead to severe morbidity and mortality in many developing countries around the globe. New antimalarial drugs are urgently needed due to the emergence of antimalarial-resistant strains of Plasmodium falciparum. In previous studies, we tested several plants extracts that are capable of inhibiting β-hematin formation, with efficiency similar to chloroquine. In the current study, the effect of cinnamon ethanol and water extracts on inhibiting β- hematin formation was studied. Powdered cinnamon extracts and bark in a stick form were investigated using various extraction methods. A semi-quantitative in vitro method, based on the inhibition of ferriprotoporphyrin IX (FP) bio-crystallization developed by Deharo et al. (2002) was utilized. Water extracts of cinnamon revealed potential activity even at low concentration of infusions, which was manifested by a high capability to inhibit β-hematin formation in vitro

Pure Isolates and Preparative HPLC Fractions or Crude Extract of Inula viscosa: Effect on β-hematin Inhibition in vitro

The antimalarial activity of wild Inula viscosa (I. viscosa) plant leaves was investigated. The efficacy of the whole crude extract versus preparative HPLC fractions versus pure isolates were compared by measuring their effect on β-hematin inhibition in-vitro. The preparative HPLC experiments consisted of reversed phase preparative column (22.2mm x 250mm, 10μm) and linear gradient of water, acetonitrile as the mobile phase. Injection volume was 1000μl and the wavelengths range were from 200-450 nm using photodiode array detector (PDA). While fractions (IV, V and VI) showed antimalarial potential in comparison to chloroquine positive control, the rest of the fractions did not show any significant inhibition to the β-hematin formation. The antimalarial results showed that whole crude exact of the plant works better than the preparative fractions or the pure isolates presumably due to synergistic effect. The chemical identity of some of the pure isolates was explored using UHPLC-ESi-MS. Moreover, I. viscosa extract powder stayed stable over several years, while many other products such as Artemisia annua extract or Artemisin Combined Therapy (ACT) drugs rapidly lost their efficiency under tropical storage conditions.None

Fasting of Ramadan in peoples with diabetes in Benghazi, Libya: an exploratory study

Background: The epidemiology of diabetes and Ramadan fasting was reported from many Muslim countries, but not from Libya. Methodology: We interviewed 493 consecutive diabetic patients at Benghazi Diabetes and Endocrine Center for the potential complications of fasting during Ramadan. Results: We found 70% of diabetic patients completed the 30 days of Ramadan fasting. Hypo- and hyperglycemia was the most commonly reported complications especially during the first two weeks of Ramadan month. Conclusion: It seems majority of diabetic patients in Libya manage to fast during Ramadan month. Patient education and early planned adjustment of diabetic medication is needed to decrease the frequency of diabetic complication during Ramadan month

Clinical experience with biphasic insulin aspart in people with type 2 diabetes: Results from the Libya cohort of the A 1 chieve study

Background: The A 1 chieve, a multicentric (28 countries), 24-week, non-interventional study evaluated the safety and effectiveness of insulin detemir, biphasic insulin aspart and insulin aspart in people with T2DM (n = 66,726) in routine clinical care across four continents. Materials and Methods: Data was collected at baseline, at 12 weeks and at 24 weeks. This short communication presents the results for patients enrolled in biphasic insulin aspart sub group from Libya. Results: A total of 179 patients were enrolled in the biphasic insulin aspart subgroup. All the patients were prior insulin users. At baseline glycaemic control was poor (mean HbA 1 c: 9.3%). After 24 weeks of treatment there was an improvement in HbA 1 c (−0.9%). Hypoglycaemic events reduced from 7.2 events/patient-year to 3.7 events/patient-year in 24 weeks. SADRs did not occur in any of the study patients. Conclusion: Starting or switching to biphasic insulin aspart was associated with improvement in glycaemic control with a low rate of hypoglycaemia

Dichloro-<i>bis</i>-(pyridine-2-yl-undecyl-amine)zinc(II), [ZnCl₂(C₁₆N₂H₂₆)₂]: Synthesis, characterization and antimalarial activity

<p>A nitrogen-based ligand (pyridine-2-yl-undecyl-amine) (<b>1</b>) was synthesized and used for the synthesis of a Zn(II) compound (dichloro-bis(pyridine-2-yl-undecyl-amine)zinc(II)) (<b>2</b>). Compound <b>2</b> was synthesized and characterized using IR, ¹H NMR, and ¹³C{¹H} NMR spectroscopy. The crystal structure of <b>2</b> was determined using single-crystal X-ray crystallography. The compound was tested for its anti-malarial activity using two methods, a semi-quantitative micro-assay and a previously self-developed quantitative <i>in vitro</i> method. Both methods were used to study the efficiency of <b>2</b> to inhibit the formation of the malaria pigment considered an important target of many anti-malarial drugs such as chloroquine and amodaquine. The efficiency of <b>2</b> to prevent the formation of β-hematin was 71.4%. The efficiency of amodiaquine as a standard drug was reported at 93.8%.</p

Uncovering the Chemical Composition and Biological Potentials of <i>Bupleurum lancifolium</i> Hornem. from Jordan

The current study was designed to uncover the chemistry and bioactivity potentials of Bupleurum lancifolium growing wild in Jordan. In this context, the fresh aerial parts obtained from the plant material were subjected to hydrodistillation followed by GC/MS analysis. The main components of the HDEO were γ-patchoulene (23.79%), β-dihydro agarofuran (23.50%), α-guaiene (14.11%), and valencene (13.28%). Moreover, the crude thanolic extract was partitioned to afford two main major fractions, the aqueous methanol (BLM) and butanol (BLB). Phytochemical investigation of both fractions, using conventional chromatographic techniques followed by careful inspection of the spectral data for the isolated compounds (NMR, IR, and UV-Vis), resulted in the characterization of five known compounds, including α-spinasteryl (M1), ethyl arachidate (M2), ethyl myristate (M3), quercetin-3-O-β-d-glucopyranosyl-(1-4”)-α-L-rhamnopyranosyl (B1), and isorhamnetin-3-O-β-d-glucopyranosyl-(1-4”)-α-L-rhamnopyranosyl (B2). The TPC, TFC, and antioxidant activity testing of both fractions and HDEO revealed an interesting ABTS scavenging potential of the BLB fraction compared to the employed positive controls, which is in total agreement with its high TP and TF contents. Cytotoxic evaluation tests revealed that BLM had interesting cytotoxic effects on the normal breast cell line MDA-MB-231 (ATCC–HTB-26) and the normal dermal fibroblast (ATCC® PCS-201-012) and normal African green monkey kidney Vero (ATCC-CCL-81) cell lines. Despite both the BLB and BLM fractions showing interesting AChE inhibition activities (IC50 = 217.9 ± 5.3 µg/mL and 139.1 ± 5.6 µg/mL, respectively), the HDEO revealed an interestingly high AChE inhibition power (43.8 ± 2.7 µg/mL) that far exceeds the one observed for galanthamine (91.4 ± 5.2 µg/mL). The HDEO, BLM, and BLB exhbitied no interesting antimicrobial activity against Bacillus cereus, Bacillus subtilis, Staphylococcus aureus, Escherichia coli, or Pseudomonas aeruginosa