A series of lupeol derivatives 2, 2a-2f, 2a-2h, 3a-3e, and 4a-4b were designed, synthesized and evaluated for their α-glucosidase inhibitory and cytotoxic activities. Among synthetic derivatives, lupeol analogues 2b and 2e containing a benzylidene chain exhibited the best activity against α-glucosidase and superior to the positive agent with the IC 50 values of 29.4 ± 1.33 and 20.1 ± 0.91 μM, respectively. Lupeol analogues 2d and 3a showed weak cytotoxicity against K562 cell line with the IC 50 values of 76.6 ± 2.40 and 94.4 ± 1.51 μM, respectively.
Trichostemonoate (1), a new tirucallane, together with four known compounds, 11α,20-dihydroxydammar-24-ene-3-one (2), sapelin E acetate (3), grandifolinolenenone (4) and α-mangostin (5), were isolated from the stem bark of Walsura trichostemon. The structural assignment of the new compound was based on spectroscopic methods. All isolated compounds were evaluated for their cytotoxicity against five cancer cell lines.
The genus Clerodendrum belongs to the family Verbenaceae and consists of about 30 species. It is mainly distributed in Thailand, India, and China. From the plants of this genus were isolated abietane diterpenoids, iridoids, phenylethanoid glycosides, triterpenes, and saponins. Some of them have been reported to possess many biological activities, including antimalarial, antitumor, anti-HIV [1], and antiasthmatic activities [2].Clerodendrum paniculatum L. is commonly known as glorybower, bagflower, and bleeding-heart. It is a shrub, liana, or small tree. There are no reports on phytochemical investigations of this plant. In continuation of our search for anticancer compounds of Thai medicinal plants, we have examined the CH 2 Cl 2 extract of this plant for cytotoxic constituents [3]. The roots of this plant were collected from Khon Kaen Province in September 2011 and identified by Dr. Suttira Khumkratok, a botanist at the Walairukhavej Botanical Research Institute, Mahasarakham University, and a specimen was retained as a reference .The dried roots of C. paniculatum (5.13 kg) were extracted with CH 2 Cl 2 at room temperature. The solvent was evaporated in vacuo to give the CH 2 Cl 2 extract (23.37g). This extract was chromatographed on a silica gel column eluted with gradient systems of hexane, CH 2 Cl 2 , EtOAc, and MeOH. Then the compounds were separated and purified using various chromatrographic methods such as open-column chromatography, preparative thin-layer chromatography, chromatotron, and Sephadex LH-20 chromatography to afforded compounds 1-6. The six compounds were found to be identical with E-sitosterol (1) [4], lupeol (2) [5], oleanolic aldehyde acetate (3) [6], stigmasta-4,25-dien-3-one (4) [7], (22E)-stigmasta-4,22,25-trien-3-one (5) [7], and (3E-stigmasta-4,22,25-trien-3-ol (6) [7]. The isolated compounds were identified by a combination of spectroscopic methods ( 1 H NMR, 13 C NMR, and MS) as well as by comparison with the literature and authentic samples. Compounds 1-6 were isolated from this plant for the first time.All isolated compounds were tested for their cytotoxicity against KB and HeLa cell lines. Oleanolic aldehyde acetate (3) showed significant cytotoxic activity against the KB cell line with an IC 50 value of 9.58 Pg/mL. On the other hand, (3E)-stigmasta-4,22,25-trien-3-ol (6) also exhibited moderate cytotoxic activity against the KB cell line with an IC 50 value of 13.14 Pg/mL. The standard agent (adriamycin) showed an IC 50 value of 0.018 Pg/mL against both cell lines. E-Sitosterol (1), colorless needles. ESI-MS m/z 415 [M + H] + . This compound is identical to an authentic sample. Lupeol (2), colorless needles, mp 215qC [5]. Oleanolic aldehyde acetate (3), white crystals. 1 H NMR (400 MHz, CDCl 3 , G, ppm, J/Hz): 0.74 (3H, s, H-26), 0.87 (3H, s, H-24), 0.90 (3H, s, H-23), 0.93 (3H, s, H-30), 0.94 (3H, s, H-25), 0.94 (3H, s, H-29), 1.16 (3H, s, H-27), 1.46 (1H, dd, J = 16.0, 8.0, H-9), 1.89 (1H, d, J = 8.0, H-2), 1.89 (1H, d, J = 8.0, H-22), 1.98 (1H, dt, J = 16.0, 4.0, H-11), 2.07 ...
Plant oils derived from medicinal herbs have furnished bioactive synergistics, as well as antibacterial and antifungal properties. The study was to evaluate the antibacterial activity of essential oils (EOs) against Cutibacterium acnes and to analyze the chemical compositions of the effective oils. The experiment was conducted using a completely randomized design with duplications. Three EOs obtained from Allium sativum (garlic), Gardenia jasminoides (gardenia), and Hedychium coronarium (hydechium) cultivated in Thailand were tested for antibacterial activity using an agar well diffusion assay and the macro-dilution method. The chemical compositions of the selected oil were determined by gas chromatography and mass spectrometry (GC-MS). To compare the data, Duncan’s multiple range test (DMRT) was performed, and significance was determined at the p < 0.05 level. The results showed that garlic oil had the highest potent inhibitory zone on C. acnes, according to the findings. As a bactericidal, garlic oil had MIC and MBC values of 0.39 and 0.78 mg/mL, and even a MIC index (MBC/MIC) of 4. Diallyl thiosulfinate (allicin) (20.53%), 1,3-dithiane (12.53%), cyclic octaatomic sulfur (5.02%), 1,4-dihydro-2,3-benzoxathiin-3-oxide (4.73%), and carvone (3.40%) were the major components of garlic oil. The results suggest that garlic oil might be used to develop topical anti-acne treatments.
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