Development of AB3-Type Novel Phthalocyanine and Porphyrin Photosensitizers Conjugated with Triphenylphosphonium for Higher Photodynamic Efficacy.

There are a number of lipophilic cations that can be chosen; the triphenylphosphonium (TPP) ion is particularly unique for mitochondrion targeting, mainly due to its simplicity in structure and ease to be linked to the target molecules. In this work, mitochondrion-targeted AB3-type novel phthalocyanine and porphyrin photosensitizers (PSs) were synthesized and their photophysical photochemical properties were defined. Fluorescence quantum yields (ΦF) are 0.009, 0.14, 0.13, and 0.13, and the singlet-oxygen quantum yields (ΦΔ) are 0.27, 0.75, 0.57, and 0.58 for LuPcPox(OAc), AB 3 TPP-Pc, AB 3 TPP-Por-C4, and AB 3 TPP-Por-C6, respectively. To evaluate the photodynamic efficacy of the TPP-conjugated PS cell viabilities of A549 and BEAS-2B lung cells were comparatively measured and IC-50 values were determined. AB 3 TPP-Por-C4, AB 3 TPP-Por-C6, and AB 3 TPP-Pc compounds compared to the reference molecules ZnPc and H 2 TPP were found to be highly cytotoxic (sub-micromolar concentration) under the light. LuPcPox(OAc) is the most effective molecule regarding cell killing (the activity). The cell killing of the TPP-conjugated porphyrin derivatives exhibits a similar response compared to LuPcPox(OAc) when the light absorbing factor of the PS is normalized at 660 nm: TPP-conjugated porphyrins absorb less light (lower extinction coefficient) but produce more radical species (higher singlet-oxygen quantum yield) and therefore effectively kill the cells. The singlet oxygen-producing capacity of AB 3 TPP-Pc is almost 3 times higher compared to LuPcPox(OAc) and 50% more efficient with respect to ZnPc, suggesting that TPP-conjugated phthalocyanine may serve as a good photosensitizer for photodynamic therapy (PDT). The high singlet oxygen generation capacity of these novel TPP-conjugated porphyrin and phthalocyanine PS suggests that they might be useful for PDT requiring lower photosensitizer concentration and reduced energy deposited through less light exposure.

Synthesizing and evaluating the photodynamic efficacy of asymmetric heteroleptic A7B type novel lanthanide bis-phthalocyanine complexes.

In this study heteroleptic A7B type novel Lu(iii) and Eu(iii) lanthanide phthalocyanines (LnPc(Pox)[Pc'(AB3SH)]) with high extinction coefficients have been synthesized as candidate photosensitizers with reaction yields higher than 33%. The singlet oxygen quantum yields of LuPc(Pox)[Pc'(AB3SH)] and EuPc(Pox)[Pc'(AB3SH)], respectively, were measured 17% and 1.4% by the direct method in THF. The singlet oxygen quantum yield of LuPc(Pox)[Pc'(AB3SH)] in THF is the highest among lutetium(iii) bis-phthalocyanine complexes to date. The photodynamic efficacy of the heteroleptic lanthanide phthalocyanines was evaluated by measuring cell viabilities of A549 and BEAS-2B lung cells, selected to representing in vitro models for testing cancer and normal cells against potential drugs. The cell viabilities demonstrated concentration dependent behavior and were varied by the type of phthalocyanines complexes. Irradiation of the cells for 30 minutes with LED array at 660 nm producing flux of 0.036 J cm-2 s-1 increased cell death for LuPcPox-OAc, LuPc(Pox)[Pc'(AB3SH)] and ZnPc. The IC50 concentrations of LuPc(Pox)[Pc'(AB3SH)] and ZnPc were determined to be below 10 nM for both cell lines, agreeing very well with the singlet oxygen quantum yield measurements. These findings suggest that LuPc(Pox)[Pc'(AB3SH)] and particularly LuPcPox-OAc are promising drug candidates enabling lowered dose and shorter irradiation time for photodynamic therapy.

Health benefits of Quran memorization for older men.

OBJECTIVE: To examine the association between Quran memorization and health among older men. METHODS: This cross-sectional study included older Saudi men (age ≥ 55 years) from Buraidah, Al-Qassim. The neighborhoods were selected randomly (20 out of 96); eligible men from the mosques were recruited. Demographics, lifestyle, and depression were assessed with standardized questionnaires; height, weight, blood pressure, and random blood glucose (glucometer) were measured with standard protocol. RESULTS: The mean and standard deviation for age, body mass index, and Quran memorization were 63 years (7.5), 28.9 kg/m2 (4.8), and 4.3 sections (6.9). Prevalence of hypertension, diabetes, and depression were 71%, 29%, and 22%, respectively. Those who memorized at least 10 sections of Quran were 64%, 71%, and 81% less likely to have hypertension, diabetes, and depression compared to those who memorized less than 0.5 sections, after controlling for covariates. CONCLUSION: There was a strong linear association between Quran memorization and hypertension, diabetes, and depression indicating that those who had memorized a larger portion of the Quran were less likely to have one of these chronic diseases. Future studies should explore the potential health benefits of Quran memorization and the underlying mechanisms.

Chronic disease prevalence among elderly Saudi men.

OBJECTIVE: Saudi demographic composition has changed because of increased life expectancy and decreased fertility rates. Little data are available about health conditions among older adults in Saudi Arabia, who are expected to represent 20% of the population by 2050. The study aim was to assess the prevalence and risk factors for chronic conditions among older Saudi men. METHODS: The sample pertained to 400 men (age ≥55 years) from Buraidah, Al-Qassim. Research assistants recruited participants in all the mosques from the randomly selected neighborhoods (16 of 95). They administered a structured questionnaire that assessed self-reported disease history (heart disease, hypertension, diabetes, asthma, gastric/peptic ulcer, and cancer), and medication use; participants' height, weight, blood pressure, and random blood glucose (glucometer) were measured. Multinomial logistic regressions were employed to assess correlates of number of chronic diseases. RESULTS: The mean and standard deviation for age and body mass index (BMI) were 63.0 ± 7.5 years and 28.9 ± 4.8 (kg/m2), respectively. 78% (77.8%) were overweight or obese, 35.0% were employed, 54.5% walked daily, 9.3% were current smokers, and 85.0% belonged to the middle class. The prevalence of hypertension, diabetes, heart disease, asthma, ulcer, and cancer were: 71.3% 27.3%, 16.4%, 9.7%, 8.9%, and 2.0%, respectively. Of the participants, 31.0% had one, 34.5% had two or more, and 34.5% did not have any chronic diseases. The likelihood of chronic diseases increased with increased age, higher BMI, and current smoking. CONCLUSION: The chronic disease prevalence among the Saudi elderly men is substantial.