Antioxidant, Diabetic and Inflammatory Activities of Alpinia calcarata Roscoe Extract.

BACKGROUND: Alpinia calcarata (AC) Roscoe of Zingiberaceae popularly known as lesser galangal has a widespread occurrence in China, India, Sri-Lanka, Bangladesh, Malaysia, Indonesia and Thailand. Essential oil (Eoil) was obtained from leaves/rhizomes of AC via hydro-distillation process. METHODS: To identify chemical ingredients in oil from leaves/rhizomes of AC through GC/MS technique for volatile components and their anti-oxidant, inflammatory/diabetic activities. RESULTS: The 38 and 65 components were found to make up 99.9 and 99.6 %, respectively in total of Eoil composition of AC leaves/rhizomes. Key chemical constituents were eucalyptol (28.7 % in leaves; 25.4 % in rhizomes), camphor (12.8 % in leaves; 4.2 % in rhizomes), and carotol (9.8 % in leaves; 5.6 % in rhizomes) found in oil of AC leaves/rhizomes. Colorimetric assay showed anti-oxidant activities in leaves and rhizomes are IC50 =71.01±0.71 µg/mL and IC50 =73.83±0.49 µg/mL, respectively in the Eoils. Eoils had high anti-oxidant capabilities in IC50 -values of AC-L-Eoil=43.09±0.82&AC-Rh-Eoil=68.11±0.87 in reducing power in µg/mL was found. Albumin test of rhizome oil had IC50 -values of 15.19±0.25 µg/mL. Concentrations range of 7.81 µg/mL and 250 µg/mL in the Eoils of AC leaves and rhizome, respectively by α-glucosidase inhibition assay. CONCLUSION: Our findings demonstrated that leaf oil was slightly more promising results than rhizome oil of AC extract, which was ultimately showed medicinal potential of secondary metabolites with anti-oxidant, diabetic/inflammatory activities. Further, Eoils of AC have a wide range of pharmacological potential and promising anti-diabetic effects.

Glomerella fusarioides-catalyzed structural transformation of steroidal drugs mesterolone and methasterone, and anti-inflammatory activity of resulting derivatives.

Transformation of steroidal drug mesterolone (1) with Glomerella fusarioides yielded two new (17α-hydroxy-1α-methyl-5α-androstan-3-one-11α-yl acetate (2) and 15α-hydroxy-1-methyl-5α-androstan-1-en-3,17-dione (3)), and four known derivatives (15α,17ß-dihydroxy-1α-methyl-5α-androstan-3-one (4), 15α-hydroxy-1α-methyl-5α-androstan-3,17-dione (5), 1α-methyl-androsta-4-en-3,17-dione (6) and 15α,17ß-dihydroxy-1-methyl-5α-androstan-1-en-3-one (7). Similarly, G. fusarioides-catalyzed transformation of steroidal drug methasterone (8) afforded four new metabolites, 11α,17ß-dihydroxy-2,17α-dimethylandrosta-1,4-diene-3-one (9), 3a,11α,17ß-trihydroxy-2α,17α-dimethyl-5α-androstane (10), 1ß,3ß,17ß-trihydroxy-2α,17α-dimethyl-5α-androstane (11), and 11α,17ß-dihydroxy-2,17α-dimethylandrosta-1,4-diene-3-one (12). Structures of new derivatives were determined by using 1D-, and 2D-NMR, HREI-MS, and IR spectroscopic data. New derivative 3 was identified as a potent inhibitor of NÈ® production with the IC50 value of 29.9 ± 1.8 µM, in comparison to the standard l-NMMA (IC50 = 128.2 ± 0.8 µM) in vitro. In addition, methasterone (8) (IC50 = 83.6 ± 0.22 µM) also showed a significant activity comparable to new derivative 12 (IC50 = 89.8 ± 1.2 µM). New derivatives 2 (IC50 = 102.7 ± 0.5 µM), 9 (IC50 = 99.6 ± 5.7 µM), 10 (IC50 = 123.5 ± 5.7 µM), and 11 (IC50 = 170.5 ± 5.0 µM) showed a moderate activity. NG-MonomethylL-arginine acetate (IC50 = 128.2 ± 0.8 µM) was used as standared NO⋅- free radicals have an important role in the regulation of immune responses and cellular events. Their overproduction is associated with the pathogenesis of numerous ailments, such as Alzheimer's cardiac disorders, cancer, diabetes, and degenerative diseases. Therefore, inhibition of NÈ® production can help in the treatment of chronic inflammation and associated disorders. All derivatives were found to be non-cytotoxic to human fibroblast (BJ) cell line. The results presented here form the basis of further research for the development of new anti-inflammatory agents with improved efficacy through biotransformation approaches.

Biotransformation of contraceptive drug desogestrel with Cunninghamella elegans, and anti-inflammatory activity of its metabolites.

Biotransformation of an orally active contraceptive drug, desogestrel (1), with Cunninghamella elegans yielded a new metabolite, 13ß-ethyl-11-methylene-18,19-dinor-17α-pregn-4-en-20-yn-17ß-ol-3,6-dione (2), along with five known metabolites, i.e., 13ß-ethyl-11-methylene-18,19-dinor-17α-pregn-4-en-20-yn-3ß,6ß,17ß-triol (3), 13ß-ethyl-11-methylene-18,19-dinor-17α-pregn-4-en-20-yn-6ß,17ß-diol-3-one (4), 13ß-ethyl-11-methylene-18,19-dinor-17α-pregn-4-en-20-yn-17ß-ol-3-one (5), 13ß-ethyl-11-epoxy-18,19-dinor-17α-pregn-4-en-20-yn-17ß-ol-3-one (6), and 13ß-ethyl-11-methylene-18,19-dinor-17α-pregn-4-en-20-yn-10ß,17ß-diol-3-one (7). The structure of new metabolite 2 was elucidated by using 1H-, 13C-, and 2D-NMR, EI-, and HREI-MS, IR, and UV spectroscopic data. Compounds 1-7 were evaluated for anti-inflammatory activities, i.e., inhibition of T-cell proliferation, and pro-inflammatory cytokine (TNF-α). Compounds 1 (IC50 = 1.12 ± 0.03 µg/mL), 2 (IC50 = 1.15 ± 0.05 µg/mL), 3 (IC50 = 1.15 ± 0.05 µg/mL), 4 (IC50 = 1.40 ± 0.03 µg/mL), 5 (IC50 = 1.78 ± 0.08 µg/mL), and 6 (IC50 = 1.36 ± 0.07 µg/mL) were identified as potent inhibitors of T-cells proliferation, in comparison to the standard drug, prednisolone (IC50 = 3.51 ± 0.03 µg/mL). Compound 7 (IC50 = 6.18 ± 0.04 µg/mL) showed a good activity. In addition, substrate 1 (IC50 ≤ 1 µg/mL), and its metabolites 2 (IC50 = 4.1 ± 0.60 µg/mL), and 6 (IC50 = 6.8 ± 0.8 µg/mL) also showed a potent inhibition of pro-inflammatory cytokine (TNF-α) production, as compared to the standards drug, pentoxifilline (IC50 = 94.8 ± 2.1 µg/mL). Whereas compounds 3 (IC50 = 57.9 ± 7.6 µg/mL), and 5 (IC50 = 27.2 ± 6.8 µg/mL) showed a moderate inhibition of TNF-α production, while compounds 4 and 7 showed no inhibition. Compounds 1-7 were found to be non-cytotoxic to 3T3 normal cell line (mouse fibroblast).

Evidence for a curriculum review for secondary schools in Fiji.

This pilot study aimed to gather information about knowledge of and attitudes towards a range of health and dietary issues, with a focus on obesity and NCDs. It involved 967 children equally distributed between Form 3 (age range 13-14) and form 5 (age range 16-17) from three schools, one from each of the health divisions in Fiji. It was found that almost half of the sample group were of "normal" weight, whilst 18% were classified as "overweight" and 16% as "obese". Half the children took an inactive mode of transport (bus/car) to school and a higher percentage of those who went by bus/car were overweight. The average daily consumption of fruit and vegetables was very low and the consumption of fried foods was high, particularly in urban-based schools. The majority of students did not know the full and correct definition of "balanced meals". Despite the majority of children (83.7%) recognizing the importance of PA and 75% of children reporting that they exercised "for health", only 14% of boys and 10% of girls said they looked forward to PE classes as it was good for their health. Ninety percent of children indicated that being overweight is not healthy and that 75% of children think that being underweight is not healthy. Overall, the children recognized the importance of good diet and exercise for health. However, gaps existed in the curriculum--particularly regarding the importance of engaging in PE for health, the role of obesity in increasing the risks of NCDs and the specific meanings of terms such as "health" and "balanced meals". Modification of the curriculum to enforce knowledge of the importance of PE/PA and the way they impact upon health, may improve the dietary and PA trends seen in schools in Fiji.