Healthy Change Intervention: A Cluster RCT in Preschooler Mothers in Mexico and the United States.

OBJECTIVE: To assess effects of Healthy Change intervention on maternal perception of her child's body weight (MPCW), maternal feeding style, and obesogenic home environment. METHODS: A randomized control trial was conducted, consisting of two arms: the intervention group received the Healthy Change program, and the control group received the Hygiene and Accident Prevention program. A total of 356 mother-preschool child dyads participated, 182 in the intervention group and 174 in the control group, residing in Mexico and the United States. Data were collected at baseline and after the program through self-administered questionnaires completed by mothers and child anthropometric measurements. RESULTS: Although no significant between-group difference in pre- and post-intervention change of MPCW was found, sub-analyses revealed that a higher proportion of mothers in the intervention group accurately perceived their child's body weight at the study endpoint using categorical (67% vs. 57.1%, p < 0.005) and visual scales (48.9% vs. 41.8%, p < 0.015). Additionally, more mothers of overweight children in the intervention group accurately perceived their children's overweight and obese status compared to those in the control group (29.8% vs. 10.3%, X2 = 4.26, df = 1, p < 0.039). The intervention group also displayed a higher proportion of mothers with authoritative feeding style (26.4% vs. 16.5%, p < 0.036) and significantly higher family nutrition and physical activity scores (29.1 vs. 28.0, p < 0.000) at the study endpoint. CONCLUSIONS FOR PRACTICE: Healthy Change Intervention led to improved accuracy of MPCW, a shift toward maternal authoritative feeding styles, and positive changes in obesogenic home environments.

Latino church-going parents' insights on childhood obesity prevention.

Childhood obesity continues to be a priority health concern in the United States. Faith communities present a viable venue for health promotion programming. The majority of obesity prevention programming focuses on African American populations. Subsequently, insights for obesity prevention programming in Latino faith communities are lacking. This qualitative study aimed to gain insight into Latino church-going parents' perspectives on childhood obesity and faith-based obesity prevention strategies. Participants were Latino church-going parents with children ages 10-18, recruited from predominantly Latino churches in south Texas, United States. Focus groups were conducted with a total of 56 Latino participants from nine churches. Discussions were audio-taped and transcribed verbatim. Inductive content analysis was performed and assisted by NVivo. Participants were aware of the obesity facing their congregations. Parents' affirmation of the physical body being God's Temple supported the development of obesity prevention programs in faith community settings. Participants suggested integration of spiritual and physical health promotion through health sermons, Bible study, Sunday school, nutrition classes and physical activities for both children and adults. In brief, Latino church-going parents were concerned about childhood obesity and perceived the need for developing obesity prevention programs integrating both faith and health promotion.

Study protocol for a cluster randomized controlled trial to test "¡Míranos! Look at Us, We Are Healthy!" - an early childhood obesity prevention program.

BACKGROUND: One in three Head Start children is either overweight or obese. We will test the efficacy of an early childhood obesity prevention program, "¡Míranos! Look at Us, We Are Healthy!" (¡Míranos!), which promotes healthy growth and targets multiple energy balance-related behaviors in predominantly Latino children in Head Start. The ¡Míranos! intervention includes center-based (policy changes, staff development, gross motor program, and nutrition education) and home-based (parent engagement/education and home visits) interventions to address key enablers and barriers in obesity prevention in childcare. In partnership with Head Start, we have demonstrated the feasibility and acceptability of the proposed interventions to influence energy balance-related behaviors favorably in Head Start children. METHODS: Using a three-arm cluster randomized controlled design, 12 Head Start centers will be randomly assigned in equal number to one of three conditions: 1) a combined center- and home-based intervention, 2) center-based intervention only, or 3) comparison. The interventions will be delivered by trained Head Start staff during the academic year. A total of 444 3-year-old children (52% females; n = 37 per center at baseline) in two cohorts will be enrolled in the study and followed prospectively 1 year post-intervention. Data collection will be conducted at baseline, immediately post-intervention, and at the one-year follow-up and will include height, weight, physical activity (PA) and sedentary behaviors, sleep duration and screen time, gross motor development, dietary intake and food and activity preferences. Information on family background, parental weight, PA- and nutrition-related practices and behaviors, PA and nutrition policy and environment at center and home, intervention program costs, and treatment fidelity will also be collected. DISCUSSION: With endorsement and collaboration of two local Head Start administrators, ¡Míranos!, as a culturally tailored obesity prevention program, is poised to provide evidence of efficacy and cost-effectiveness of a policy and environmental approach to prevent early onset of obesity in low-income Latino preschool children. ¡Míranos! can be disseminated to various organized childcare settings, as it is built on the Head Start program and its infrastructure, which set a gold standard for early childhood education, as well as current PA and nutrition recommendations for preschool children. TRIAL REGISTRATION: ClinicalTrials.Gov ( NCT03590834 ) July 18, 2018.

Process evaluation of a community-based diabetes prevention program in China: the Pathway to Health (PATH).

High prevalence of diabetes and prediabetes has emerged as a concern in China. The Pathway to Health Program was designed to prevent type 2 diabetes onset in prediabetic women in a north China urban community. This process evaluation of a randomized controlled trial analysed participant surveys at the 6- and 12-month assessment times, participant weekly logs, class attendance records and post-study participant focus group results. The reported levels of participant engagement in physical activity (PA)-related behaviors were higher than diet-related behaviors at the 6-month assessment. The engagement in both PA- and diet-related behaviors declined during the 6-month follow-up period. Step counts from the participants' pedometers indicated an increase in PA in the first 6 months of the intervention. Study participants expressed high levels of satisfaction with the intervention and increased their scores on diabetes-related knowledge. Conflicts with work and family responsibilities were the main barriers for missing health lessons, likely contributing to minimal weight loss. There was good fidelity in program implementation. Intensive lifestyle modification programs are difficult to sustain once the program is complete. A more structured 6-month follow-up phase may have provided needed support to enable participants to maintain their lifestyle changes.

Study protocol: intervention in maternal perception of preschoolers' weight among Mexican and Mexican-American mothers.

BACKGROUND: Childhood obesity is a public health issue negatively affecting children's physical and psychosocial health. Mothers are children's primary caregivers, thus key players in childhood obesity prevention. Studies have indicated that mothers underestimate their children's weight. If mothers are unaware of their children's weight problem, they are less likely to participate in activities preventing and treating excess weight. The "Healthy Change" intervention is designed to change maternal perception of child's weight (MPCW) through peer-led group health education in childcare settings. METHODS/DESIGN: The "Healthy Change" is a multicenter two-arm randomized trial in four centers. Three centers are in Mexican States (Nuevo Leon, Tamaulipas, and Zacatecas). The fourth center is in San Antonio, Texas, USA. A total of 360 mother-child pairs (90 pairs per center) are to be randomly and evenly allocated to either the intervention or the control group. Intervention group will receive four-session group obesity prevention education. Control group will receive a four-session personal and food hygiene education. The education is delivered by trained peer-mother promotoras. Data will be collected using questionnaires and focus groups. The primary outcome is a change in proportion of mothers with accurate MPCW. Secondary outcomes include change in maternal feeding styles and practices, maternal self-efficacy and actions for managing child excessive weight gain. McNemar's Test will be used to test the primary outcome. The GLM Univariate procedure will be used to determine intervention effects on secondary outcomes. The models will include the secondary outcome measures as the dependent variables, treatment condition (intervention/control) as the fixed factor, and confounding factors (e.g., mother's education, children's gender and age) as covariates. Sub-analyses will be performed to compare intervention effects on primary and secondary outcomes between the samples from Mexico and Texas, USA. Qualitative data will be analyzed through analysis of inductive content. A combined coding model will be developed and used to code transcripts using the NVivo software. DISCUSSION: Healthy Change intervention could help change MPCW, an initial step for obesity prevention among preschoolers. This study presents a first of its kind intervention available in Spanish and English targeting Mexican and Mexican-American mothers in Mexico and USA. TRIAL REGISTRATION: ISRCTN12281648.

¡Miranos! (Look at Us! We Are Healthy!): Home-Based and Parent Peer-Led Childhood Obesity Prevention.

Parent interventions for childhood obesity prevention have traditionally experienced low participation rates or used passive methods such as newsletters. In contrast, the ¡Miranos! intervention home-based activities included parent-led face-to-face meetings delivered after school, take-home bags with educational materials, and scavenger hunt games to deliver health information to Head Start families regarding nutrition, physical activity, and healthy growth promotion for their preschooler. This study employed a quasi-experimental design with three intervention centers (two that received only center-based activities and one that received center- and home-based activities) and one comparison center. Data were collected on participating Head Start children and their parents/guardians and included parent attendance, parent health message recall through intercept interviews, parent knowledge through pre- and posttests, and family supportive behaviors and child health behaviors through a parent questionnaire. Parents/guardians that received both center- and home-based activities significantly increased knowledge scores (t = 2.50, degrees of freedom = 123, p < .05) and family supportive behaviors from baseline to follow-up (t = 2.12, degrees of freedom = 122, p < .05). This study demonstrates the effects home-based interventions can have when coupled with center-based activities and implemented in the center at the end of the school day.

Participants' Perspectives on Diabetes Self-Management Programming at Church: Faith-Placed Versus Faith-Based Approach.

PURPOSE: The purpose of the study was to explore Hispanic adults' experiences participating in the Building a Healthy Temple diabetes self-management education and support (DSMES) cluster randomized trial and collect their insights on intervention approach, delivery, content, impact, and suggested improvements for future DSMES programs delivered at church. METHODS: Focus groups were conducted with participants from both intervention arms, that is, faith-based (FB) group and faith-placed group. Participating churches were predominantly Hispanic and located in San Antonio, Texas. Focus groups were audiotaped and transcribed verbatim. Inductive content analysis was performed with the assistance of NVivo software to code and categorize emerging themes. RESULTS: A total of 138 adult participants took part in the current study. Participants in both groups highly valued the church setting for its convenient location and support system and reported positive changes in diabetes-related beliefs, knowledge, skills, behaviors, and health outcomes. FB participants appreciated the incorporation of spiritual teachings and facilitation by lay leaders, which created a sense of empowerment and improved outlook on living with diabetes. CONCLUSIONS: Church holds promise as a setting for DSMES program delivery in Hispanic communities. Church-based DSMES programs using a FB approach may further facilitate program adoption and sustainability.

Association between environmental tobacco smoke exposure and dementia syndromes.

OBJECTIVES: Environmental tobacco smoke (ETS) has a range of adverse health effects, but its association with dementia remains unclear and with dementia syndromes unknown. We examined the dose-response relationship between ETS exposure and dementia syndromes. METHODS: Using a standard method of GMS, we interviewed 5921 people aged ≥60 years in five provinces in China in 2007-2009 and characterised their ETS exposure. Five levels of dementia syndrome were diagnosed using the Automated Geriatric Examination for Computer Assisted Taxonomy instrument. The relative risk (RR) of moderate (levels 1-2) and severe (levels 3-5) dementia syndromes among participants exposed to ETS was calculated in multivariate adjusted regression models. RESULTS: 626 participants (10.6%) had severe dementia syndromes and 869 (14.7%) moderate syndromes. Participants exposed to ETS had a significantly increased risk of severe syndromes (adjusted RR 1.29, 95% CI 1.05 to 1.59). This was dose-dependently related to exposure level and duration. The cumulative exposure dose data showed an adjusted RR of 0.99 (95% CI 0.76 to 1.28) for >0-24 level years of exposure, 1.15 (95% CI 0.93 to 1.42) for 25-49 level years, 1.18 (95% CI 0.87 to 1.59) for 59-74 level years, 1.39 (95% CI 1.03 to 1.84) for 75-99 level years and 1.95 (95% CI 1.34 to 2.83) for ≥100 level years. Significant associations with severe syndromes were found in never smokers and in former/current smokers. There were no positive associations between ETS and moderate dementia syndromes. CONCLUSIONS: ETS should be considered an important risk factor for severe dementia syndromes. Avoidance of ETS may reduce the rates of severe dementia syndromes worldwide.

Obesogenic neighbourhoods: the impact of neighbourhood restaurants and convenience stores on adolescents' food consumption behaviours.

OBJECTIVE: To examine the relationship between the neighbourhood food environment and dietary intake among adolescents. DESIGN: Cross-sectional design using: (i) a geographic information system to assess characteristics of the neighbourhood food environment and neighbourhood socio-economic status; (ii) the modified Healthy Eating Index (HEI) to assess participants' overall diet quality; and (iii) generalized linear models to examine associations between HEI and home and school food environmental correlates. SETTING: Mid-sized Canadian city in Ontario, Canada. Participants Grade 7 and 8 students (n 810) at twenty-one elementary schools. RESULTS: Students living in neighbourhoods with a lower diversity of land-use types, compared with their higher diversity counterparts, had higher HEI scores (P < 0.05). Students with more than 1 km between their home and the nearest convenience store had higher HEI scores than those living within 1 km (P < 0.01). Students attending schools with a distance further than 1 km from the nearest convenience store (P < 0.01) and fast-food outlet (P < 0.05) had higher HEI scores than those within 1 km. Those attending schools with three or more fast-food outlets within 1 km had lower HEI scores than those attending schools with no fast-food outlet in the school surroundings (P < 0.05). CONCLUSIONS: Close proximity to convenience stores in adolescents' home environments is associated with low HEI scores. Within adolescents' school environments, close proximity to convenience and fast-food outlets and a high density of fast-food outlets are associated with low HEI scores.

Room Temperature Engineering Crystal Facet of Cu2O for Photocatalytic Degradation of Methyl Orange.

Cuprous oxide (Cu2O) has received enormous interest for photocatalysis owing to its narrow band gap of 2.17 eV, which is beneficial for visible-light absorption. In this work, we succeeded in synthesizing Cu2O nanocrystals with two morphologies, cube and sphere, at room temperature via a simple wet-chemistry strategy. The morphologies of Cu2O change from cube to sphere when adding PVP from 0 g to 4 g and the mainly exposed crystal faces of cubic and spherical Cu2O are (100) and (111), respectively. The photocatalytic properties of the as-prepared Cu2O were evaluated by the photocatalytic degradation of methyl orange (MO). Cubic Cu2O(100) showed excellent photocatalytic activity. After the optical and photoelectric properties were investigated, we found that cubic Cu2O(100) has better photoelectric separation efficiency than spherical Cu2O(111). Finally, the possible mechanism was proposed for cubic Cu2O(100) degrading MO under visible light.

Northern Fruit and Vegetable Pilot Program: a process evaluation.

PURPOSE: A process evaluation was conducted of the Northern Fruit and Vegetable Pilot Program (NFVPP), a government-funded health promotion initiative. The objectives were to determine how the program was implemented and to identify program facilitators and challenges. METHODS: Facilitators and challenges in the implementation of the free fruit and vegetable snack program were assessed through qualitative interviews with school-level stakeholders (i.e., food preparers, teachers, and principals) and tracking wasted produce. The implementation of an enhanced nutrition education (ENE) component was assessed through a teacher survey. RESULTS: School-level stakeholders saw the NFVPP as a valuable program. Key facilitators included teacher role-modelling and sufficient funding for supplies and personnel. Key challenges included produce delivery, quality, wastage, and variety. The ENE component was minimally implemented. CONCLUSIONS: The study identified program strengths and areas that could be improved. As a result, changes were made to how the NFVPP was implemented in schools the following year. The use of qualitative methods enabled program planners to understand the program implementation process.

Screen-related sedentary behaviours of school-aged children: Principals' and teachers' perspectives.

OBJECTIVE: To solicit school principals' and teachers' perspectives on children's screen-related sedentary behaviour and to identify possible solutions to reduce sedentary behaviours among school-aged children. METHOD: In-person interviews using a semi-structured interview guide were conducted with school principals and grades five and six classroom teachers in 14 randomly selected elementary schools in London and Middlesex County, Ontario. Fourteen principals and 39 classroom teachers participated in the study. Inductive content analysis was performed independently by two researchers. RESULTS: Both principals and teachers were very concerned about children's excessive screen activities, but they did not perceive that they could play a key role in reducing these behaviours. Key barriers were identified to reducing screen-related sedentary behaviour and to children's active living both at and away from school. They included competing demands from other subjects, limited gym resources/space within the school, a lack of control over the home environment, and a perception that parents were poor role models. Notwithstanding the above barriers, principals and teachers still recommended increasing children's daily physical activity both within and outside of school hours. Furthermore, they stressed the need for parents to play a key role in reducing their children's screen-related sedentary behaviours and increasing their level of physical activity. CONCLUSION: School principals and teachers were very concerned about excessive screen-behaviour among school-aged children when away from school and suggested that interventions should emphasize increasing daily physical education, promoting recreational sports at or away from school, and engaging parents in regulating screen time at home.

SAR and molecular mechanism study of novel acylhydrazone compounds targeting HIV-1 CA.

We synthesized a series of acylhydrazone compounds bearing naturally occurring amino acids' side chains as HIV assembly inhibitors. Biological evaluation indicated that the compounds had anti-SIV and capsid assembly inhibitory activities. The structure-activity relationship (SAR) study showed that compounds bearing proper aromatic side chains had potential antiviral activities. The molecular modeling experiments revealed the molecular mechanism that they could bind to CA in the same manner as CAP-1 and occupy two more grooves.

Canadian global village reality: anthropometric surrogate cutoffs and metabolic abnormalities among Canadians of East Asian, South Asian, and European descent.

OBJECTIVE: To test the appropriateness of body mass index (BMI) and waist circumference (WC) cutoff points derived in largely white populations (ie, those of European descent) for detecting obesity-related metabolic abnormalities among East Asian and South Asian Canadians. DESIGN: Cross-sectional survey. SETTING: Primary care and community settings in Ontario. PARTICIPANTS: Canadians of East Asian (n = 130), South Asian (n = 113), and European (n = 111) descent. MAIN OUTCOME MEASURES: Variables for metabolic syndromes, including BMI, WC, body fat percentage, blood pressure, lipid profile, and fasting blood glucose and insulin levels, were measured. Receiver operating characteristics curve analysis was used to generate BMI and WC cutoff points based on various criteria for metabolic syndromes. RESULTS: Adjusting for sex and age, East Asian Canadians had a significantly lower mean BMI (23.2 kg/m(2)) and mean WC (79.6 cm) than did those of South Asian (26.1 kg/m(2) and 90.3 cm) and European (26.5 kg/m(2) and 89.3 cm) descent (P < .05). The BMI cutoffs for an increased risk of metabolic abnormalities ranged from 23.1 to 24.4 kg/m(2) in East Asian Canadians; 26.6 to 26.8 kg/m(2) in South Asian Canadians; and 26.3 to 28.2 kg/m(2) in European Canadians. Waist circumference cutoffs for increased risk of metabolic abnormalities were relatively low in East Asian men (83.3 to 85.2 cm) and women (74.1 to 76.7 cm), compared with South Asian men (98.8 cm) and women (90.1 to 93.5 cm), as well as European men (91.6 to 95.2 cm) and women (82.8 to 88.3 cm). CONCLUSION: The BMI and WC cutoffs used for defining risk of metabolic abnormalities should be lowered for East Asian Canadians but not for South Asian Canadians. The World Health Organization ethnic-specific BMI and WC cutoffs should be used with caution, particularly with Asian migrants who have resided in Canada for a long period of time.

Healthier snacks in school vending machines: a pilot project in four Ontario high schools.

PURPOSE: The Healthy Vending Machine Pilot Project (HVMPP) was a public health initiative intended to create a healthier school nutrition environment by making healthier snacks available in vending machines, while maintaining a profit margin. The HVMPP was evaluated using quantitative and qualitative measures. METHODS: Vending machines were stocked with healthier choices and conventional vending products at a 50:50 ratio. The HVMPP was implemented from February to May 2007 in four Ontario secondary schools in Middlesex-London, Elgin, and Oxford counties. Product sales were tracked, and focus groups were conducted to obtain students' opinions about healthy eating and vending choices. RESULTS: "Healthier choice" sales ranged from 14% to 17%. In all schools, vending revenues declined from 0.7% to 66%. A majority of participants had substantial knowledge of healthy eating and were in favour of healthier choices in vending machines; however, price, value, and taste were barriers that led them to purchase these products rarely. Students preferred to have "real" healthy snacks, such as yogurt, fruit, and vegetables, available in schools. CONCLUSIONS: Replacing 50% of vending stock with healthier snacks resulted in a decline in vending revenues. Future health programs in schools need to provide "real" healthy snacks, such as low-fat dairy products, fruits, and vegetables.

Building a Healthy Temple diabetes self-management education support program in Hispanic faith community settings: A cluster randomized controlled trial.

Diabetes self-management is key to preventing diabetes complications disproportionately affecting Hispanics. Church appears a promising setting for delivering a diabetes self-management education support (DSMES) program. "Faith-placed" (FP) programing refers to health interventions implemented in the church setting; while "faith-based" (FB) signifies integrating spirituality with health interventions. The Building a Health Temple (BHT) DSMES program integrates spirituality with DSMES to improve diabetic outcomes. This cluster-randomized trial tests the effectiveness of BHT DSMES by adapting an existing DSMES program into faith-based context. A total of 360 participants will be recruited from 18 churches (~20 participants/church). Churches will be randomly assigned to either the FB or FP intervention arm. Intervention activities will be implemented over 14 consecutive weeks. Participants in the FB arm will participate in BHT DSMES including a Health Sermon, the Self-Management Resource Center (SMRC) Diabetes Self-Management Program (DSMP), and a 7-session Healthy Bible Study, delivered by two trained church lay health leaders. Participants in the FP arm will attend the same SMRC DSMP facilitated by outside health professional, followed by a 7-session community health and safety curriculum as a partial attention control intervention. The primary outcome will be a change in Hemoglobin A1c (HbA1c) level. Secondary outcomes include: changes in body mass index, waist circumference, diabetes distress score, diabetes self-care behaviors, eating behavior, and physical activity level. Data will be collected at baseline, 6, 9, and 12 months during the study period. The proposed study will lead to innovative DSMES program delivery through faith settings for Hispanic persons with diabetes.

The influence of the physical environment and sociodemographic characteristics on children's mode of travel to and from school.

OBJECTIVES: We examined whether certain characteristics of the social and physical environment influence a child's mode of travel between home and school. METHODS: Students aged 11 to 13 years from 21 schools throughout London, Ontario, answered questions from a travel behavior survey. A geographic information system linked survey responses for 614 students who lived within 1 mile of school to data on social and physical characteristics of environments around the home and school. Logistic regression analysis was used to test the influence of environmental factors on mode of travel (motorized vs "active") to and from school. RESULTS: Over 62% of students walked or biked to school, and 72% from school to home. The likelihood of walking or biking to school was positively associated with shorter trips, male gender, higher land use mix, and presence of street trees. Active travel from school to home was also associated with lower residential densities and lower neighborhood incomes. CONCLUSIONS: Our findings demonstrate that active travel is associated with environmental characteristics and suggest that school planners should consider these factors when siting schools in order to promote increased physical activity among students.

Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein.

HIV-1 capsid protein (CA) plays important roles in the viral replication cycle. A number of acylhydrazone derivatives that act as inhibitors of HIV-1 CA assembly, were designed and synthesized. The synthesized compounds were tested for their antiviral activities and cytotoxicities using CEM cells. Some derivatives also were assayed for their ability to inhibit HIV-1 CA assembly in vitro. Among them, compounds 14f and 14i display the most promising potency with EC(50) values of 0.21 and 0.17 microM respectively.

Design, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors.

Thirty-two quinoline derivatives were designed and synthesized as HIV-1 Tat-TAR interaction inhibitors. All the compounds showed high antiviral activities in inhibiting the formation of SIV-induced syncytium in CEM174 cells. Nine of them with low cytotoxicities were evaluated by Tat dependent HIV-1 LTR-driven CAT gene expression colorimetric enzyme assay in human 293T cells, indicating effective inhibitory activities of blocking the Tat-TAR interaction. Molecular modeling experiments indicated that these compounds may inhibit Tat-TAR interaction by binding to Tat protein instead of TAR RNA.

Discovery of dual inhibitors targeting both HIV-1 capsid and human cyclophilin A to inhibit the assembly and uncoating of the viral capsid.

HIV-1 assembly and disassembly (uncoating) processes are critical for the HIV-1 replication. HIV-1 capsid (CA) and human cyclophilin A (CypA) play essential roles in these processes. We designed and synthesized a series of thiourea compounds as HIV-1 assembly and disassembly dual inhibitors targeting both HIV-1 CA protein and human CypA. The SIV-induced syncytium antiviral evaluation indicated that all of the inhibitors displayed antiviral activities in SIV-infected CEM cells at the concentration of 0.6-15.8 microM for 50% of maximum effective rate. Their abilities to bind CA and CypA were determined by ultraviolet spectroscopic analysis, fluorescence binding affinity and PPIase inhibition assay. Assembly studies in vitro demonstrated that the compounds could potently disrupt CA assembly with a dose-dependent manner. All of these molecules could bind CypA with binding affinities (Kd values) of 51.0-512.8 microM. Fifteen of the CypA binding compounds showed potent PPIase inhibitory activities (IC(50) values<1 microM) while they could not bind either to HIV-1 Protease or to HIV-1 Integrase in the enzyme assays. These results suggested that 15 compounds could block HIV-1 replication by inhibiting the PPIase activity of CypA to interfere with capsid disassembly and disrupting CA assembly.