The anti-tubercular activity of Melia azedarach L. and Lobelia chinensis Lour. and their potential as effective anti-Mycobacterium tuberculosis candidate agents

Objective: To evaluate the anti-mycobacterial activity of Melia azedarach L. (M. azedarach) and Lobelia chinensis Lour. (L. chinensis) extracts against the growth of Mycobacterium tuberculosis (M. tuberculosis). Methods: The anti-M. tuberculosis activity of M. azedarach and L. chinensis extracts were evaluated using different indicator methods such as resazurin microtiter assay (REMA) and mycobacteria growth indicator tube (MGIT) 960 system assay. The M. tuberculosis was incubated with various concentrations (50–800 mg/mL) of the ex-tracts for 5 days in the REMA, and for 4 weeks in MGIT 960 system assay. Results: M. azedarach and L. chinensis extracts showed their anti-M. tuberculosis ac-tivity by strongly inhibiting the growth of M. tuberculosis in a concentration-dependent manner in the REMA and the MGIT 960 system assay. Particularly, the methanol extract of M. azedarach and n-hexane extract of L. chinensis consistently exhibited their effects by effectively inhibiting the growth of M. tuberculosis in MGIT 960 system for 4 weeks with a single-treatment, indicating higher anti-M. tuberculosis activity than other extracts, and their minimum inhibitory concentrations were measured as 400 mg/mL and 800 mg/mL, respectively. Conclusions: These results demonstrate that M. azedarach and L. chinensis extracts not only have unique anti-M. tuberculosis activity, but also induce the selective anti-M. tuberculosis effects by consistently inhibiting or blocking the growth of M. tuberculosis through a new pharmacological action. Therefore, this study suggests the potential of them as effective candidate agents of next-generation for developing a new anti-tuberculosis drug, as well as the advantage for utilizing traditional medicinal plants as one of effective strategies against tuberculosis.

The anti-tubercular activity of Melia azedarach L. and Lobelia chinensis Lour. and their potential as effective anti-Mycobacterium tuberculosis candidate agents

Objective To evaluate the anti-mycobacterial activity of Melia azedarach L. (M. azedarach) and Lobelia chinensis Lour. (L. chinensis) extracts against the growth of Mycobacterium tuberculosis (M. tuberculosis). Methods The anti-M. tuberculosis activity of M. azedarach and L. chinensis extracts were evaluated using different indicator methods such as resazurin microtiter assay (REMA) and mycobacteria growth indicator tube (MGIT) 960 system assay. The M. tuberculosis was incubated with various concentrations (50–800 μg/mL) of the extracts for 5 days in the REMA, and for 4 weeks in MGIT 960 system assay. Results M. azedarach and L. chinensis extracts showed their anti-M. tuberculosis activity by strongly inhibiting the growth of M. tuberculosis in a concentration-dependent manner in the REMA and the MGIT 960 system assay. Particularly, the methanol extract of M. azedarach and n-hexane extract of L. chinensis consistently exhibited their effects by effectively inhibiting the growth of M. tuberculosis in MGIT 960 system for 4 weeks with a single-treatment, indicating higher anti-M. tuberculosis activity than other extracts, and their minimum inhibitory concentrations were measured as 400 μg/mL and 800 μg/mL, respectively. Conclusions These results demonstrate that M. azedarach and L. chinensis extracts not only have unique anti-M. tuberculosis activity, but also induce the selective anti-M. tuberculosis effects by consistently inhibiting or blocking the growth of M. tuberculosis through a new pharmacological action. Therefore, this study suggests the potential of them as effective candidate agents of next-generation for developing a new anti-tuberculosis drug, as well as the advantage for utilizing traditional medicinal plants as one of effective strategies against tuberculosis.

Triterpenoids and sterols from Melia azedarach and their anti-diabetes activities / 中草药

Objective: To investigate the chemical constituents from the barks of Melia azedarach and their antidiabetes activities. Methods: The constituents were isolated and purified by silica gel, reverse phase silica gel, and Sephadex LH-20 column chromatography, and their structures were identified by spectra and physiochemical characteristic analysis. The agonist activities of the isolated triterpenoids against glucokinase (GK) and SIRT1, and the inhibitory activity against dipeptidyl peptidasesIV (DPPIV), and 11β-hydroxysteroid dehydrogenase (11β-HSD) were tested in vitro. Results: Six triterpenoids and three sterols were obtained from MeOH extract in the barks of M. azedarach and were elucidated as meliastatin 3 (1), kulonic acid (2), kulactone (3), sendanolactone (4), dubione B (5), 20, 24-cyclotirucalla-7(8)-en-16β, 21α, 25-trihydroxy-3-one (6), 3β-hydroxy-5, 8-epidioxy-ergosta-6, 22-diene (7), 2β, 3β, 4β-trihydroxy-pregn-16-one (8), and 3β-hydroxy-pregn-5, 17 (20)-dien-16-one (9). Compound 2 showed the inhibitory activity against 11β-HSD1 with the IC50 value of 54.15 nmol/L. Conclusion: Compounds 6-9 are obtained from this species for the first time. The tested compounds 1-4 are inactive against GK, SIRT1, and DPPIV, but compound 2 shows high selectivity against human 11β-HSD.

The Toxicity and Anti-cancer Activity of the Hexane Layer of Melia azedarach L. var. japonica Makino's Bark Extract

In this study, the 4-week oral toxicity and anti-cancer activity of the hexane layer of Melia azedarach L. var. japonica Makino's bark extract were investigated. We carried out a hollow fiber (HF) assay and 28-day repeated toxicity study to confirm the anti-cancer effect and safety of the hexane layer. The HF assay was carried out using an A549 human adenocarcinoma cell via intraperitoneal (IP) site with or without cisplatin. In the result, the 200 mg/kg b.w of hexane layer with 4 mg/kg b.w of cisplatin treated group, showed the highest cytotoxicity aginst A549 carcinoma cells. For the 28-day repeated toxicity study, 6 groups of 10 male and female mice were given by gavage 200, 100, or 50 mg/kg b.w hexane layer with or without 4 mg/kg b.w of cisplatin against body weight, and were then sacrificed for blood and tissue sampling. The subacute oral toxicity study in mice with doses of 200, 100, and 50 mg/kg b.w hexane layer showed no significant changes in body weight gain and general behavior. The cisplatin-treated group significantly decreased in body weight compared to the control group but regained weight with 100 and 200 mg/kg b.w of hexane layer. The biochemical analysis showed significant increase in several parameters (ALT, total billirubin, AST, creatinine, and BUN) in cisplatin-treated groups. However, in the group given a co-treatment of hexane layer (200 mg/kg b.w), levels of these parameters decreased. In hematological analysis, cisplatin induced the reduction of WBCs and neutrophils but co-treatment with hexane layer (100 and 200 mg/kg b.w) improved these toxicities caused by cisplatin. The histological profile of the livers showed eosinophilic cell foci in central vein and portal triad in cisplatin treated mice. These results show that hexane layer might have an anti-cancer activity and could improve the toxicity of cisplatin.

Minor Phenolic Constituents of Chinaberry-tree (Melia azedarach) / 中草药

Five minor ferulic acid esters (Ⅰ～Ⅴ) were identified in a petrol extract of Melia azedarach stem bark, one (Ⅰ) of which was isolated with no impurity for the first time. By chemical and spectral methods, their structures were elucidated as hexacosylferulate (Ⅰ); tetracosylferulate (Ⅱ); pentacosylferulate (Ⅲ); heptacosylferulate (Ⅳ) and octacosylferulate (Ⅴ), respectively.