Materials and Methods: SF1 was produced by optimized methodology for bioassay-guided fractionation. Fourier transform infrared (FTIR) spectroscopy and liquid chromatography-mass spectrometry (LC-MS) were carried out to characterize the SF1. SF1 was screened for cytotoxicity activity toward HeLa, SiHa, and normal cells (NIH) cells by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay. The anticancer mechanism of SF1 was evaluated toward SiHa cells, which showed highest cytotoxicity toward SF1 treatment. The mechanism includes cell cycle progression and protein expression, which was detected using specific antibody-conjugated fluorescent dye, p53-FITC, by flow cytometry.
Results: Major constituents of SF1 were alkaloids with amines as functional group. SF1 showed highest cytotoxic activity against SiHa (half-maximal inhibitory concentration [IC50] < 10 µg/mL) compared to HeLa cells. Cytoselectivity of SF1 was observed with no IC50 detected on normal NIH cells. On flow cytometry analysis, SF1 was able to induce apoptosis on SiHa cells by arresting cell cycle at G1/S and upregulation of p53 protein.
Conclusion: SF1 showed anticancer activity by inducing apoptosis through arrested G1/S cell cycle checkpoint-mediated mitochondrial pathway.
METHODS: Methadone-maintained therapy (MMT) users from three centers in Malaysia had their exhaled carbon monoxide (eCO) levels recorded via the piCO+ and iCOTM Smokerlyzers®, their nicotine dependence assessed with the Malay version of the Fagerström Test for Nicotine Dependence (FTND-M), and daily tobacco intake measured via the Opiate Treatment Index (OTI) Tobacco Q-score. Pearson partial correlations were used to compare the eCO results of both devices, as well as the corresponding FTND-M scores.
RESULTS: Among the 146 participants (mean age 47.9 years, 92.5% male, and 73.3% Malay ethnic group) most (55.5%) were moderate smokers (6-19 cigarettes/day). Mean eCO categories were significantly correlated between both devices (r=0.861, p<0.001), and the first and second readings were significantly correlated for each device (r=0.94 for the piCO+ Smokerlyzer®, p<0.001; r=0.91 for the iCOTM Smokerlyzer®, p<0.001). Exhaled CO correlated positively with FTND-M scores for both devices. The post hoc analysis revealed a significantly lower iCOTM Smokerlyzer® reading of 0.82 (95% CI: 0.69-0.94, p<0.001) compared to that of the piCO+ Smokerlyzer®, and a significant intercept of -0.34 (95% CI: -0.61 - -0.07, p=0.016) on linear regression analysis, suggesting that there may be a calibration error in one or more of the iCOTM Smokerlyzer® devices.
CONCLUSIONS: The iCOTM Smokerlyzer® readings are highly reproducible compared to those of the piCO+ Smokerlyzer®, but calibration guidelines are required for the mobile-phone-based device. Further research is required to assess interchangeability.
AIM OF THE STUDY: To test extracts of P. glaucus in a number of bioassays and determine the legitimacy of its traditional use.
MATERIALS AND METHODS: The stems, leaves, roots and fruits of P. glaucus were collected and extracted sequentially with hexane, chloroform and ethanol, respectively. The anti-inflammatory activity was assessed by testing the ability of the extracts to inhibit heat induced protein denaturation, stabilise human red blood cells under hypotonic stress and by testing the inhibitory activity of the extracts against cyclooxygenases 1 and 2. Cytotoxicity was tested using the human lung epithelial cell line MRC-5 and nasopharangeal carcinoma cell line HK1 in the MTT assay.
RESULTS: Many of the samples showed an ability to prevent heat induced protein denaturation, as well as prevent lysis of red blood cells. Most of the extracts demonstrated inhibitory activity towards both of the COX enzymes. The ethanol extracts tended to demonstrate greater toxicity than other extracts, with some of the other extracts significantly enhancing growth and metabolism of the cells.
CONCLUSION: The benefit of P. glaucus for the treatment of diseases related to inflammation and cancer was supported by the in vitro assays adopted in this study.
OBJECTIVE: The objective of this study was the quantitative analysis of the alkaloid content of areca chewable products from different countries and regions using HPLC-UV, as well as the benefit of their safety evaluation products.
METHOD: An HPLC-UV method was established for qualitative and quantitative analyses of 65 batches of areca chewable products from different countries and regions. Additionally, similarity evaluation of chromatographic fingerprints was applied for data analysis.
RESULTS: These results reveal a significant variation in the levels of areca alkaloids among tested products, specifically guvacoline (0.060-1.216 mg/g), arecoline (0.376-3.592 mg/g), guvacine (0.028-1.184 mg/g), and arecaidine (0.184-1.291 mg/g). There were significant differences in the alkaloid content of areca chewable products from different producing areas.
CONCLUSIONS: The method will be useful in the safety evaluation of different areca chewable products.
HIGHLIGHTS: The established HPLC-UV method can be adopted for safety evaluation of areca chewable products from different countries and regions due to its general applicability.
AIM OF THE STUDY: This present study sought to investigate kratom use motives among regular kratom users in Malaysia.
MATERIALS AND METHODS: A total of 116 regular kratom users were recruited for this cross-sectional survey. The Drinking Motives Questionnaire (DMQ) was administered to measure kratom use motives.
RESULTS: Our results indicate that heavy (>3 glasses daily, each glass contains 48.24-50.4 mg of mitragynine) kratom use was associated with coping (t87.09 =3.544, p 3 glasses daily) kratom consumption (p 3 glasses daily) kratom consumption among regular kratom users in traditional, rural settings.
METHOD: A literature survey of published kratom studies among humans was conducted. Forty published studies relevant to the objective were reviewed.
RESULTS: Apart from the differences in the sources of supply, patterns of use and social acceptability of kratom within these two regions, the most interesting finding is its evolution to a recreational drug in both settings and the severity of the adverse effects of kratom use reported in the West. While several cases of toxicity and death have emerged in the West, such reports have been non-existent in South East Asia where kratom has had a longer history of use. We highlight the possible reasons for this as discussed in the literature. More importantly, it should be borne in mind that the individual clinical case-reports emerging from the West that link kratom use to adverse reactions or fatalities frequently pertained to kratom used together with other substances. Therefore, there is a danger of these reports being used to strengthen the case for legal sanction against kratom. This would be unfortunate since the experiences from South East Asia suggest considerable potential for therapeutic use among people who use drugs.
CONCLUSION: Despite its addictive properties, reported side-effects and its tendency to be used a recreational drug, more scientific clinical human studies are necessary to determine its potential therapeutic value.