In vitro antiplasmodial, cytotoxic and antioxidant effects, and phytochemical constituents of eleven plants used in the traditional treatment of malaria in Akwa Ibom State, Nigeria

Purpose: To evaluate the antiplasmodial effects of eleven plants (Bombax buonopozense, Carica papaya, Anthocleista djalonensis, Milicia excelsa, Heterotis rotundifolia, Homalim letestui, Starchystarpheta cayennnensis, Ocimum gratissimum, Cleistopholis patens, Chromolaena odorata and Hippocratea africana) reportedly used in the treatment of malaria in Akwa Ibom State of Nigeria. Methods: Phytochemical analysis was done by standard methods, while in vitro antiplasmodial evaluation was carried out using Plasmodium falciparum chloroquine-sensitive and chloroquineresistant strains using lactate dehydrogenase (pLDH) assay.  Cytotoxicity test was undertaken by MTT assay on LLC-MK2 cells and the concentration killing 50 % of the cells (CC50) was calculated.Antioxidant activity of the ethanol extract was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. Results: Milicia excelsa, Heterotis rotundifolia and Chromolaena odorata had moderate antiplasmodial activity. Ocimum gratissimum and Hippocratea africana were weakly active. Milicia excelsa showed a considerable level of cytotoxicity, while Bombax buonopozense exhibited moderate cytotoxicity. Bombax buonopozense (95.3 %) and Ocimum gratissimum (92.0 %) exhibited high DPPH scavengingeffect comparable to Vitamin C (98.7 %). There was a significant correlation (p < 0.05) between DPPH inhibition and the total phenolic contents of the eleven plants studied (r2 = 0.6616), between DPPH inhibition and flavonoids (r2 = 0.3553), between antiplasmodial activity and saponin content (r2= 0.3992), and between the two antiplasmodial evaluation assay methods (r2 = 0.614).Conclusion: The results of this work provide some justification for the use of Milicia excelsa, Heterotis rotundifolia, Chromolaena odorata, Ocimum gratissimum and Hippocratea africana in the treatment of malaria. Keywords: Antiplasmodial, Antioxidant, Cytotoxicity, Phytochemicals, Antimalari

Establishment of criminal/profile DNA database and use of forensic intelligence to combat nationwide insecurity issues in Nigeria

Criminal activity is on the rise in Nigeria. The nefarious activity of bandits is on the increase with kidnapping of students and attack on farmers. This creates fear in the terrorized communities. Armed robbery as well as rape of citizens going about their normal duties is also on the increase. The road is becoming increasingly unsafe for the citizenry as well as government officials. The government has mandated individuals to register in the National Identification Number NIN which is linked to the Bank Verification Number (BVN) (a database established to curb crime in the banking sector) and the Subscriber Identity module (SIM). The Establishment of such databases is pertinent however the NIN, BVN, SIM-NIN linkage and fingerprints may not be sufficient in solving criminal cases without DNA profiling of convicted individuals, establishment of forensic laboratories and the creation of criminal DNA profile database CRODER – a Criminal offender DNA Exert Repertoire. The role of DNA profiling as an additional measure is to keep a record of all convicted individuals and the CRODER will be an additional useful measure in profiling criminals and individuals can be adopted as a forensic tool in addition to the captured databases of NIN, BVN and NIN-SIM and will be on the watch list of security operatives. The CRODER forensic tool can be done stepwise by availability of an emergency number to dial for emergency, a dispatch personnel to respond to the call, and vigilante groups or other adhoc security officer in the vicinity of the emergency call to get to the vicinity and preserve the crime scene environment for investigators and detectives to work on. CRODER Forensic tool can then be adopted to solve the crime. Offenders trying to escape enroute the airport, can be checked via CRODER and fingerprint compared and matched with the collection in the database. The CRODER may be a necessary stride to bring kidnappers, bandits, and armed robbers to book in record time and curb the rise in criminal activity, insurgency, banditry, and insecurity in general. If properly done, Nigeria will be a haven for citizens and would-be investors

Synthesis of some esters of cinnamic acid and evaluation of their in vitro antidiabetic and antioxidant properties

Purpose: To synthesize various ester derivatives of cinnamic acid and to evaluate their in vitro antidiabetic and antioxidant properties. Methods: Esters of cinnamic acid were synthesized by refluxing the parent compound (cinnamic acid) with different alcohols using concentrated sulphuric acid as a catalyst. Physicochemical analyses (solubility, boiling point, refractive index) and spectrophotometric analyses (ultraviolet-visible spectroscopy (UV-VIS), Fourier-transform infrared spectroscopy (FT-IR) and gas chromatography-mass spectroscopy (GC-MS)) were carried out on the synthesized products. The antioxidant inhibitory property, uptake of glucose by yeast, and haemoglobin glycosylation of the synthesized products were also evaluated using standard methods. Results: The identities of methylcinnamate, ethylcinnamate, propylcinnamate, 2-propylcinnamate, butylcinnamate and 2-butylcinnamate were confirmed, at m/z ratios of (131,103,77 and M+ of162), (131,103,77 and M+ of 176), (147,103,77and M+ of 190), (147,103,77 and M+ of 204), (143, 103, 77 and M+ of 190), and finally (147,103,77 and M+ of 204) respectively. FT-IR results revealed the following important bonds for the synthesized compounds: C=O, C-C, C-O, C=H, C-H and adjacent H. The results for glucose uptake by yeast and of haemoglobin glycosylation test indicate that all the products facilitated the transport and detachment of glucose at varying concentrations, respectively. The DPPH scavenging activity of propylcinnamate, 2-butylcinnamate and methylcinnamate with the absorbance of 63.06, 56.85 and 53.06 at 50 μg/mL - 250 μg/mL, respectively, recorded the highest values when compared with the control (ascorbic acid). Conclusion: The results reveal that the six ester derivatives of cinnamic acid exhibit a certain degree of antidiabetic activity by facilitating the uptake of glucose by yeast and reducing glycation of haemoglobin; thus, showing a reasonable level of inhibition against free radicals

Betulinic and ursolic acids from Nauclea latifolia roots mediate their antimalarial activities through docking with PfEMP-1 and PfPKG proteins

Abstract Background Chemotherapies target the PfEMP-1 and PfPKG proteins in Plasmodium falciparum, the parasite that causes malaria, in an effort to prevent the disease’s high fatality rate. This work identified the phytochemical components of Nauclea latifolia roots and docked the chemical compounds against target proteins, and examined the in vivo antiplasmodial effect of the roots on Plasmodium berghei-infected mice. Methods Standard protocols were followed for the collection of the plant’s roots, cleaning, and drying of the roots, extraction and fraction preparation, assessment of the in vivo antiplasmodial activity, retrieval of the PfEMP-1 and PfPKG proteins, GCMS, ADME, and docking studies, chromatographic techniques were employed to separate the residual fraction’s components, and the Swis-ADME program made it possible to estimate the drug’s likeness and pharmacokinetic properties. The Auto Dock Vina 4.2 tool was utilized for molecular docking analysis. Results The residual fraction showed the best therapeutic response when compared favorably to amodiaquine (80.5%) and artesunate (85.1%). It also considerably reduced the number of parasites, with the % growth inhibition of the parasite at 42.8% (D2) and 83.4% (D5). Following purification, 25 compounds were isolated and characterized with GCMS. Based on their low molecular weights, non-permeation of the blood–brain barrier, non-inhibition of metabolizing enzymes, and non-violation of Lipinski’s criteria, betulinic and ursolic acids were superior to chloroquine as the best phytochemicals. Hence, they are lead compounds. Conclusion In addition to identifying the bioactive compounds, ADME, and docking data of the lead compounds as candidates for rational drug design processes as observed against Plasmodium falciparum target proteins (PfEMP-1 and PfPKG), which are implicated in the pathogenesis of malaria, the study has validated that the residual fraction of N. latifolia roots has the best antiplasmodial therapeutic index