Synthesis, anti-amoebic activity and molecular docking simulation of eugenol derivatives against Acanthamoeba sp.

Amoebae of the genus Acanthamoeba can cause diseases such as amoebic keratitis and granulomatous amoebic encephalitis. Until now, treatment options for these diseases have not been fully effective and have several drawbacks. Therefore, research into new drugs is needed for more effective treatment of Acanthamoeba infections. Eugenol, a phenolic aromatic compound mainly derived from cloves, has a variety of pharmaceutical properties. In this study, nine eugenol derivatives (K1-K9), consisting of five new and four known compounds, were synthesized and screened for their antiamoebic properties against Acanthamoeba sp. The structure of these compounds was characterized spectroscopically by Fourier transform infrared (FTIR), Ultraviolet-Visible (UV-Vis), 1H and 13C Nuclear Magnetic Resonance (NMR) and mass spectrometer (MS). The derived molecules were screened for antiamoebic activity by determining IC50 values based on 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and observation of amoeba morphological changes by light and fluorescence microscopy. Most of the tested compounds possessed strong to moderate cytotoxic effects against trophozoite cells with IC50 values ranging from 0.61 to 24.83 µg/mL. Observation of amoebae morphology by light microscopy showed that the compounds caused the transformed cells to be roundish and reduced in size. Furthermore, fluorescence microscopy observation using acridine orange (AO) and propidium iodide (PI) (AO/PI) staining showed that the cells have damaged membranes by displaying a green cytoplasm with orange-stained lysosomes. Acidification of the lysosomal structure indicated disruption of the internal structure of Acanthamoeba cells when treated with eugenol derivatives. The observed biological results were also confirmed by interaction simulations based on molecular docking between eugenol derivatives and Acanthamoeba profilin. These interactions could affect the actin-binding ability of the protein, disrupting the shape and mobility of Acanthamoeba. The overall results of this study demonstrate that eugenol derivatives can be considered as potential drugs against infections caused by Acanthamoeba.

Phytochemical Constituents of Aquilaria malaccensis Leaf Extract and Their Anti-Inflammatory Activity against LPS/IFN-γ-Stimulated RAW 264.7 Cell Line.

This study aims to identify the major phytochemical constituents in Aquilaria malaccensis (Thymelaeaceae) ethanolic leaf extract (ALEX-M) and elucidate their ability to suppress nitric oxide (NO) production from a murine macrophage-like cell line (RAW 264.7) stimulated by lipopolysaccharide (LPS) and interferon-γ (IFN-γ). Dichloromethane (DCM) and ethyl acetate (EtOAc) fractions of ALEX-M were subjected to column chromatography. Eight known compounds were isolated for the first time from this species. Compounds were identified using spectroscopic techniques (IR, UV, HRESIMS, and 1D and 2D NMR). Anti-inflammatory activity of both extract and isolated compounds were investigated in vitro. The fractions offered the isolation of epifriedelanol (1), 5-hydroxy-7,4'-dimethoxyflavone (2), luteolin-7,3',4'-trimethyl ether (3), luteolin-7,4'-dimethyl ether (4), acacetin (5), aquilarinenside E (6), iriflophenone-2-O-α-l-rhamnopyranoside (7), and iriflophenone-3-C-ß-glucoside (8). The findings suggest the pharmacological potential of the crude extract (ALEX-M) and its isolates as natural anti-inflammatory agents, capable of suppressing NO production in RAW 264.7 cells stimulated by LPS/IFN-γ.

The functioning of different beetle (Coleoptera) sampling methods across altitudinal gradients in Peninsular Malaysia.

Biodiversity research relies largely on knowledge about species responses to environmental gradients, assessed using some commonly applied sampling method. However, the consistency of detected responses using different sampling methods, and thus the generality of findings, has seldom been assessed in tropical ecosystems. Hence, we studied the response consistency and indicator functioning of beetle assemblages in altitudinal gradients from two mountains in Malaysia, using Malaise, light, and pitfall traps. The data were analyzed using generalized linear mixed-effects models (GLMM), non-metric multidimensional scaling (NMDS), multivariate regression trees (MRT), and indicator species analysis (IndVal). We collected 198 morpho-species of beetles representing 32 families, with a total number of 3,052 individual beetles. The richness measures generally declined with increasing altitude. The mountains differed little in terms of light and Malaise trap data but differed remarkably in pitfall-trap data. Only light traps (but not the other trap types) distinguished high from middle or low altitudes in terms of beetle richness and assemblage composition. The lower altitudes hosted about twice as many indicators as middle or high altitudes, and many species were trap-type specific in our data. These results suggest that the three sampling methods reflected the altitudinal gradient in different ways and the detection of community variation in the environment thus depends on the chosen sampling method. However, also the analytical approach appeared important, further underlining the need to use multiple methods in environmental assessments.

Incidence and predictors of postpartum depression among postpartum mothers in Kuala Lumpur, Malaysia: A cross-sectional study.

Postpartum depression (PPD) is one of the mental health complications that may arise following childbirth. This cross-sectional study explores the association between socioeconomic factors and PPD literacy with PPD incidence in 350 participants (mean age: 30.58±4.72 years) at one to six months postpartum, who attended the Kuala Lumpur Health Clinic from May to October 2020. PPD incidence and literacy were assessed using the validated Malay versions of the Edinburgh Postpartum Depression Scale (EPDS) and the Postpartum Depression Literacy Scale (PoDLiS), respectively. The participants' socioeconomic characteristics were collected using a self-administered questionnaire. Chi-square tests were performed to determine the association between these factors and PPD incidence. Binary logistic regression models were used to determine the odds ratios (OR). The incidence of postpartum depressive symptoms was 14.29%. Those with low household income were twice likely to have PPD symptoms (OR:2.58, 95% CI:1.23-5.19; p = 0.01) than those with higher incomes. Unemployment (i.e., participants who were housewives/homemakers) was associated with higher PPD incidence (Χ2(2, 350) = 6.97, p = 0.03), but it was not a significant PPD predictor. In conclusion, PPD incidence in the sample of Kuala Lumpur postpartum mothers is significantly associated with low household income. Other socioeconomic characteristics, including PPD literacy, were not significant predictors of PPD incidence.

How mountains and elevations shape the spatial distribution of beetles in Peninsular Malaysia.

This study was conducted to assess the spatial distribution of beetles in mountain ecosystems and their elevational diversity. Malaise, pitfall and light traps were used to collect beetles from nine different mountains in Malaysia from September 2014 to September 2016, where from Gunung Angsi, Gunung Belumut, Gunung Basor and Gunung Tebu samples were collected at 500 m and 1000 m (above sea level) elevations, while beetles were sampled at 500 m, 1000 m and 1500 masl from Gunung Benom, Gunung Inas, Cameron Highland, Gunung Besar Hantu and Gunung Basor. In this study, 9628 beetles belonging to 879 different species were collected with highest representation from family Staphylinidae and Carabidae. Chamah Highland had the highest beetle diversity followed by Gunung Benom, Gunung Inas, Cameron Highland, Gunung Belumut, and Gunung Basor. Chamah Highland was different to all mountains on abundance and species richness. The highest species richness was observed at 1000 m, followed by 500 m and 1500 m. We identified characteristic species associated with habitat conditions at Gunung Benoum and Gunung Inas mountains, according to INDVAL values. The beetle diversity of the sampled mountains showed multiple alpha and beta patterns according to type of mountain ecosystem and elevation, providing guidelines for the scientific community to underpin conservation efforts in Malaysia.

Interactions of Flavone and Steroid from A. subintegra as Potential Inhibitors for Porcine Pancreatic Lipase.

BACKGROUND: Obesity is one serious health condition that contributes to various chronic diseases. The inhibition of pancreatic lipase is a promising treatment for obesity. OBJECTIVE: The present study was designed to investigate anti-porcine pancreatic lipase effect of isolated compounds from Aquilaria subintegra and its mechanism. METHODS: Compounds were isolated with serial column chromatography and their structure were identified using spectroscopic methods. Isolated compounds were tested for anti-lipase potential activity using colorimetric assay. The prediction of energy binding between isolated compounds and enzyme was described using YASARA software. RESULTS: Four compounds were successfully isolated from the bark of A. subintegra, namely, 5- hydroxy-7,4'-dimethoxyflavone, luteolin-7,3',4'-trimethyl ether, 5,3'-dihydroxy-7,4'-dimethoxyflavone and ß-sitosterol. The results indicated that all compounds displayed promising pancreatic lipase inhibitory activity ranging between of 6% to 53% inhibition. Compound 5-hydroxy-7,4'- dimethoxyflavone was a competitive inhibitor and decreases the enzyme catalysis. Meanwhile, ß- sitosterol was a non- competitive inhibitor since the latter was bind allosterically toward enzyme. CONCLUSION: This finding is significant for further investigation of bioactive compounds from A. subintegra on animal study.

Chemical composition, antifeedant, repellent, and toxicity activities of the rhizomes of galangal, Alpinia galanga against Asian subterranean termites, Coptotermes gestroi and Coptotermes curvignathus (Isoptera: Rhinotermitidae).

Dual choice bioassays were used to evaluate the antifeedant property of essential oil and methanolic extract of Alpinia galanga (L.) (locally known as lengkuas) against two species of termites, Coptotermes gestroi (Wasmann) and Coptotermes curvignathus (Holmgren) (Isoptera: Rhinotermitidae). A 4-cm-diameter paper disc treated with A. galanga essential oil and another treated with either methanol or hexane as control were placed in a petri dish with 10 termites. Mean consumption of paper discs (miligram) treated with 2,000 ppm of essential oil by C. gestroi was 3.30 ± 0.24 mg and by C. curvignathus was 3.32 ± 0.24 mg. A. galanga essential oil showed significant difference in antifeedant effect, 2,000 ppm of A. galanga essential oil was considered to be the optimum concentration that gave maximum antifeedant effect. The essential oil composition was determined using gas chromatography-mass spectrometry. The major component of the essential oil was 1,8-cineol (61.9%). Antifeedant bioassay using 500 ppm of 1,8-cineol showed significant reduction in paper consumption by both termite species. Thus, the bioactive agent in A. galangal essential oil causing antifeeding activity was identified as 1,8-cineol. Repellent activity shows that 250 ppm of 1,8-cineol caused 50.00 ± 4.47% repellency for C. gestroi, whereas for C. curvignathus 750 ppm of 1,8-cineol was needed to cause similar repellent activity (56.67 ± 3.33%). C. curvignathus is more susceptible compare to C. gestroi in Contact Toxicity study, the lethal dose (LD50) of C. curvignathus was 945 mg/kg, whereas LD50 value for C. gestroi was 1,102 mg/kg. Hence 1,8-cineol may be developed as an alternative control against termite in sustainable agriculture practices.

Evaluation of a worksite cervical screening initiative to increase Pap smear uptake in Malaysia: a cluster randomized controlled trial.

BACKGROUND: Despite the significant burden of cervical cancer, Malaysia like many middle-income countries relies on opportunistic cervical screening as opposed to a more organized population-based program. The aim of this study was to ascertain the effectiveness of a worksite screening initiative upon Papanicolaou smear test (Pap test) uptake among educated working women in Malaysia. METHODS: 403 female teachers who never or infrequently attended for a Pap test from 40 public secondary schools in Kuala Lumpur were recruited into a cluster randomized trial conducted between January and November 2010. The intervention group participated in a worksite cervical screening initiative whilst the control group received usual care from the existing cervical screening program. Multivariate logistic regression was performed to determine the impact of the intervention program on Pap smear uptake after 24 weeks of followup. RESULTS: The proportion of women attending for a Pap test was significantly higher in the intervention than in the control group (18.1% versus 10.1%, P value < 0.05) with the worksite screening initiative doubling the Pap smear uptake, adjusted odds ratio 2.44 (95% CI: 1.29-4.62). CONCLUSION: Worksite health promotion interventions can effectively increase cervical smear uptake rates among eligible workers in middle-income countries. Policy makers and health care providers in these countries should include such interventions in strategies for reducing cervical cancer burden. This trial is registered with IRCT201103186088N1.

Applying the Transtheoretical Model to evaluate the effect of a call-recall program in enhancing Pap smear practice: a cluster randomized trial.

OBJECTIVE: The objective of this study was to evaluate the effect of a call-recall approach in enhancing Pap smear practice by changes of motivation stage among non-compliant women. METHODS: A cluster randomized controlled trial with parallel and un-blinded design was conducted between January and November 2010 in 40 public secondary schools in Malaysia among 403 female teachers who never or infrequently attended for a Pap test. A cluster randomization was applied in assigning schools to both groups. An intervention group received an invitation and reminder (call-recall program) for a Pap test (20 schools with 201 participants), while the control group received usual care from the existing cervical screening program (20 schools with 202 participants). Multivariate logistic regression was performed to determine the effect of the intervention program on the action stage (Pap smear uptake) at 24 weeks. RESULTS: In both groups, pre-contemplation stage was found as the highest proportion of changes in stages. At 24 weeks, an intervention group showed two times more in the action stage than control group (adjusted odds ratio 2.44, 95% CI 1.29-4.62). CONCLUSION: The positive effect of a call-recall approach in motivating women to change the behavior of screening practice should be appreciated by policy makers and health care providers in developing countries as an intervention to enhance Pap smear uptake.

Factors related to poor practice of Pap smear screening among secondary school teachers in Malaysia.

INTRODUCTION: The Pap smear test has been regarded as a promising cervical screening tool since 1940s. Yet its importance has been overlooked by beneficiaries in Malaysia. This underlines the need to identify the prevalence of Pap smear practice and influencing factors towards the practice among educated working women. METHODS: A survey was conducted with 403 female teachers from 40 public secondary schools in Malaysia selected by cluster random sampling. Data were collected from January to March 2010 using a self-administered questionnaire. Multivariate logistic regression was performed to identify the factors related to the Pap smear practice. RESULTS: The rate for participants who ever had Pap test was only 38% and poor practice of was significantly higher among: those with aged less than 35 years; those practicing hormonal contraceptive method; and individuals perceiving barriers to the Pap smear screening test. In contrast, the findings were significantly lower in women with longer duration of teaching service; higher income groups; ever pregnant; having chronic diseases; health insurance coverage; and who had perceived benefit of Pap smear screening. CONCLUSION: Barriers towards practicing Pap smear exist even among educated career women. Tailor-made health promotion and education on cervical cancer and the benefit of Pap smear screening are essential to change the behavior of the study population.

Enhancement of the cervical cancer screening program in Malaysia: a qualitative study.

INTRODUCTION: Cervical cancer has long been known as a preventable disease. Yet it still is a prime women's health issue globally. In Malaysia, the current cervical cancer screening program, introduced in the 1960s, has been found to be unsuccessful in terms of Pap smear coverage. The aim of this study is to determine providers perceptives on the program and the feasibility of practicing an organized cervical screening program in Malaysia. METHODS: 11 key informant interviews were conducted with policy makers and health care providers from the Ministry of Health in Malaysia from October 2009 to May 2010. Interviewees' perceptions were explored on current and organized cervical screening program based on their expertise and experience. RESULTS: The results highlighted that the existing cervical screening program in Malaysia faced flaws at all levels that failed to reduce cervical cancer morbidity and mortality. The identified weaknesses were poor acceptance by women, lack of commitment by health care providers, nature of the program, an improper follow-up system, limited resources and other competing needs. Complementarily, all interviewees perceived an organized cervical screening program as an alternative approach both feasible and acceptable by women and government to practice in Malaysia. CONCLUSION: Better screening coverage depends on an effective screening program that incorporates a behaviour-based strategy. A new program should be focused in the policy-making context to improve screening coverage and to effectively combat cervical cancer.

The ground beetle fauna (Coleoptera: Carabidae) of Kenyir water catchment, Terengganu, Peninsular Malaysia.

An assemblage of beetle specimens from family Carabidae (ground beetles) was carried out at Kenyir water catchment as an indicator to measure disturbance. The samplings were conducted from 30th July to 1st August 2007 at limestone forest of Teluk Bewah and the dipterocarp forest of Sungai Cicir. 28 individuals from 13 species were collected from Teluk Bewah whereas 54 individuals from ten species was sampled from Sungai Cicir. The carabids were more specious (Simpson Diversity index: 0.97) and more abundant (Margalef index: 5.35) at Teluk Bewah compared to Sungai Cicir (Simpson Diversity index, 0.72: Margalefindex, 2.22). Light trapping was most efficient assembling 97.56% of ground beetles compared to Malaise trap, pitfall and net sweeping. This is the first record of beetle assemblage at Kenyir water catchment, Malaysia. New records for Kenyir, Terengganu, Malaysia are Abacetus sp. 1, Abacetus sp. 2, Acupalpus rectifrotis, Aephnidius adelioides, Dischissus notulatus, Dolichoctis sp., Dolichoctis sp. 2, Dolichoctis straitus, Ophinoea bimaculata, Perigona sp., Pheropsophus piciccollis, Pheropsophus occipitalis, Stenolophus quinquepustulatus, Stenolophus smaragdulus, Stenolophus sp., Tachys coracinus, Casnoidea sp., Orthogonius sp. Seven species coded as Cara C, Cara J, Cara M, Cara N, Cara O, Cara R and Cara S were unidentified and are probably new species to be described in another report. There is moderately high diversity (Simpson Diversity index: 0.846) of Carabidae indicating that ecotourism does not affect diversity of ground beetle at Kenyir Lake.