In vitro antimalarial activity of Syzygium cumini fruit fraction.

Background: Malaria is still one of the most severe public health problems worldwide. The development of treatment, prevention, and control of malaria is one of the substantial problems in the world. Aims: To investigate the in vitro antimalarial activity of Syzygium cumini methanol fruit fraction. Methods: Syzygium cumini L fruit powder was macerated with methanol (PA) and the extract obtained was fractionated using the liquid-liquid partition method with n-hexane, ethyl acetate, butanol, chloroform, methanol, and water solvents. In vitro antimalarial assay was conducted using the culture of Plasmodium falciparum 3D7 strain culture that had reached >5% growth and was examined for IC50 values using a 24-well microplate in duplicate. Each treatment and control well contained 1,080 µl of complete media. Well, number 1 was added with 120 µl fraction, and then the solution was diluted until it reached 0.01, 0.1, 1, 10, and 100 µg/ml the final concentration in the microtiter well. The control only contained complete media and infected erythrocytes without the addition of anti-malarial drugs. The microplate was incubated for 48 hours. After 48 hours, a thin blood smear was made fixed with methanol and stained with 20% Giemsa for 20 minutes to determine the IC50 value by plotting sample concentrations and percentage of parasitemia in Excel. Results: The IC50 values of ethyl acetate fraction, n.hexane fraction, butanol fraction, and water fraction were 1.189, 76.996, 1,769, and 15.058 µg/ml, respectively. Whereases the IC50 values of C1 fraction (mix fraction from chloroform: methanol 100:0 and 90:10) and C4 fraction (mix fraction from chloroform: methanol 20:80, 10:90, and 0:100) were 100.126 and 1.015 µg/ml, respectively. The results showed that the IC50 value of ethyl acetate, butanol, and C4 fraction were lower than 10µg/ml and were considered as good activity (strong antimalarial activity). Conclusion: The ethyl acetate, butanol and C4 subfraction from S. cumini fruit have the potential to be developed as an antimalarial agent.

Challenges in the provision of natural medicines by community pharmacists in East Java Province, Indonesia.

OBJECTIVES: Community pharmacist has been widely known as a health professional who can be easily accessed to provide medicines and reliable medicine information. However, this was not always in the case of dispensing natural medicines. Several international studies revealed that community pharmacists were less likely to deliver natural medicines accompanied with detailed information. Therefore, this study aimed to investigate factors influencing Indonesian community pharmacists in the supply of, delivery of, and provision of information about natural medicines. METHODS: A qualitative study with purposively selected community pharmacists in four areas (district or municipality) in East Java Province was designed. In-depth, semi-structured interviewed were conducted using a Capability-Opportunity-Motivation-Behaviour approach. All interviews were audio-recorded, transcribed ad verbatim, and thematically analysed. RESULTS: Data saturation was reached after interviewing 14 community pharmacists. All informants reported dispensing non-prescribed natural medicines. Nine had experienced dispensing prescribed natural medicines, mainly fulfilling paediatricians' requests. The most common information given was about product usage, while information about safety (i.e. side effects, interaction) was rarely provided. Although numerous registered natural medicines have been available, informants had low motivation to supply a variety of types, primarily because little opportunity to receive requests from doctors and the community. Limited capability due to a lack reliable source of information about natural medicines was another reason. CONCLUSIONS: Poor motivation to supply natural medicines was because community pharmacists had little opportunity for such requests and limited capability due to scarcity of information. This indicated support from natural medicine manufacturers, researchers, and the government is highly required.

Exploration of several plants from Baung Forest on bone formation cell models.

OBJECTIVES: Osteoporosis is an ailment described by a skeletal degradation of bone skeletal dominating to increases the chance of fracture. In order to find out the bone formation agents from Baung Forest plants, this research analyzed the effects of 96% ethanol extract of several plants from Baung Forest on antioxidant activity and the effect of osteoblast differentiation-related to the bone formation on the most potent extract. METHODS: The antioxidant effect and osteoblast differentiation of 96% ethanol extracts were evaluated by measuring DPPH scavenging and alkaline phosphatase in p-nitrophenyl phosphate effects by the enzyme-linked immunosorbent assay (ELISA) reader method, respectively. RESULTS: The 96% ethanol extract of Elaeocarpus serratus L. from Baung Forest had the strongest DPPH radical scavenging as anti oxidant (82.17%) and stimulated osteoblast differentiation (116%). Then, this extract had been fractionated based on polarity to become hexane, ethyl acetate, butanol, and aqueous fractions. All the fractions stimulated their alkaline phosphatase (ALP) activity to 138.11 ± 9.72%, 108 ± 5.05%, 148.56 ± 8.47, and 144.58 ± 1.04, respectively. CONCLUSIONS: The extract and fractions of E. serratus L. can successfully inhibit DPPH radical scavenging value and increase ALP activities as markers of osteoblast functions.

Structural revision of sesbagrandiflorains A and B, and synthesis and biological evaluation of 6-methoxy-2-arylbenzofuran derivatives.

Sesbagrandiflorains A (1) and B (2), isolated from the stem bark of the Indonesian fabaceous plant Sesbania grandiflora, were reported to be 6-methoxy-2-(2´,3´-dihydroxy-5´-methoxyphenyl)-1-benzofuran-3-carbaldehyde and 6-hydroxy-2-(2´,3´-dihydroxy-5´-methoxyphenyl)-1-benzofuran-3-carbaldehyde, respectively. However, based on reevaluation of their 1D and 2D NMR data, the chemical structures of 1 and 2 have been revised to 4-hydroxy-2-(4´-hydroxy-2´-methoxyphenyl)-6-methoxybenzofuran-3-carbaldehyde and 4-hydroxy-2-(4´-hydroxy-2´-hydroxyphenyl)-6-methoxybenzofuran-3-carbaldehyde, respectively. In addition, seven new derivatives of 1 have been synthesized from the natural product in good yields (65 - 93%). The chemical structures of the synthetic compounds-one diester (6), four ethers (7-10), one secondary amine (11), and one oxime (12)-were confirmed by MS and NMR analysis. Compound 6 exhibited moderate antibacterial activity against the plant pathogen Rhodococcus fascians with a MIC of 0.1 mg/mL. Compounds 8 and 12 demonstrated respectable cytotoxicity against A375 melanoma cancer cells line with the relative IC50 values of 22.8 and 32.7 µM, respectively.

Structure Characterization and Biological Activity of 2-Arylbenzofurans from an Indonesian Plant, Sesbania grandiflora (L.) Pers.

A new 2-arylbenzofuran, sesbagrandiflorain C (1), together with four known compounds, 2-(3,4-dihydroxy-2-methoxyphenyl)-4-hydroxy-6-methoxybenzofuran-3-carbaldehyde (2), 2-(4-hydroxy-2-methoxyphenyl)-5,6-dimethoxybenzofuran-3-carboxaldehyde (3), sesbagrandiflorain A (4) and sesbagrandiflorain B (5), have been isolated from the stem bark of an Indonesian plant, Sesbania grandiflora (L.) Pers. The chemical structure of compound 1 was elucidated by UV, IR, MS, and NMR spectroscopic techniques. The proton and carbon NMR resonances of 1 were also compared with the predicted chemical shifts obtained from DFT quantum mechanical calculations with Gaussian. None of the compounds showed antibacterial activity against Bacillus subtilis, Escherichia coli, Mycobacterium smegmatis, Pseudomonas aeruginosa, and Staphylococcus aureus in an agar diffusion assay. However, sesbagrandiflorains A (4) and B (5) exhibited moderate activity against Mycobacterium tuberculosis H37Rv. In addition, compounds 1 - 5 have moderate cytotoxicity against HeLa, HepG2, and MCF-7 cancer cell lines.

Sesbagrandiflorain A and B: isolation of two new 2-arylbenzofurans from the stem bark of Sesbania grandiflora.

Native to tropical Asia, Sesbania grandiflora (L.), Pers is a member of the Fabaceae family of flowering plants. All parts of S. grandiflora are used in traditional medicine and phytochemical investigations have been conducted on extracts of the leaves, seeds and roots of S. grandiflora to provide scientific validation of its properties. However, to date, no study has determined the phytochemical constituents of S. grandiflora stem bark. The stem bark powdered of S. grandiflora was extracted exhaustively with n-hexane, EtOAc and 90% aqueous MeOH sequentially. In this study, we successfully isolated two new 2-arylbenzofurans, sesbagrandiflorain A and B, from the EtOAc stem bark of S. grandiflora. The structure elucidation of these compounds was determined by using one- and two-dimensional nuclear magnetic resonance, ultraviolet and infrared spectroscopy and electrospray ionisation time-of-flight mass spectrometry. The finding expands the understanding of the natural constituents of the Fabaceae and, in particular, the Papilionoideae genera.

A virtual screening approach for identifying plants with anti H5N1 neuraminidase activity.

Recent outbreaks of highly pathogenic and occasional drug-resistant influenza strains have highlighted the need to develop novel anti-influenza therapeutics. Here, we report computational and experimental efforts to identify influenza neuraminidase inhibitors from among the 3000 natural compounds in the Malaysian-Plants Natural-Product (NADI) database. These 3000 compounds were first docked into the neuraminidase active site. The five plants with the largest number of top predicted ligands were selected for experimental evaluation. Twelve specific compounds isolated from these five plants were shown to inhibit neuraminidase, including two compounds with IC50 values less than 92 µM. Furthermore, four of the 12 isolated compounds had also been identified in the top 100 compounds from the virtual screen. Together, these results suggest an effective new approach for identifying bioactive plant species that will further the identification of new pharmacologically active compounds from diverse natural-product resources.