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Synthesis and Cytotoxicity Evaluation of Novel C-3 Aminocarbamate Pregnenolone Derivatives
(2025-03-06)
Charoenying, Patchanee
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Chotsaeng, Nawasit
Cancer is one of the leading causes of death worldwide. There are many ongoing studies in the search for new treatments or drugs to combat cancer. Similarly, in this research, twelve 3-aminocarbamate pregnenolones (2a–2l) were designed, synthesized, and evaluated for their cytotoxicity against five cancer cell lines: Human hepatocellular carcinoma (HepG2), Human colon adenocarcinoma (HT-29), Human oral cavity carcinoma (KB), Human breast adenocarcinoma (MCF-7), Murine leukemia (P388), and one normal cell line, African green monkey kidney fibroblast (Vero), using the MTT assay. Notably, 3-aminobenzylcarbamate pregnenolone (2b), 3-diaminoheptylcarbamate pregnenolone (2f), and 3-diaminopropanolcarbamate derivative (2i) were the most potent against these cancer cell lines. Specifically, for P388 cell lines, these compounds were more potent than the positive control drug, vinblastine sulfate salt. Results from the SAR study demonstrated that the length of the alkyl chain of diaminocarbamate derivatives was crucial for their anticancer properties. These findings will be useful in the future research and development of anticancer drugs.
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Utilizing liposomal encapsulation approach to address nephrotoxic challenges of colistimethate sodium through a preclinical study
(2023-01-01)
Mektrirat, Raktham
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Paengjun, Noppanut
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Chongrattanameteekul, Peerawit
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Umsumarng, Sonthaya
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Cheunsri, Suppara
The use of Colistin, a last-resort antimicrobial drug, carries the risk of acute kidney injury. The objective of the study was to assess the effectiveness of colistin-encapsulated liposomes (CL) in reducing nephrotoxicity. Additionally, a liposomal preparation of colistimethate sodium was formulated using the reverse phase evaporation method with a 3:1 ratio of phospholipids to cholesterol. The liposomal properties were evaluated using scanning electron microscopy, photon correlation spectroscopy, and release kinetic assay. The killing kinetics of the formulations on embryonic kidney cells were assessed using in vitro MTT reduction assay. The nephrotoxicity of CL and colistimethate sodium solution (CS) was evaluated in vivo by administering a dose of 20 mg/kg to rats every 12 h for 3 days, with a negative control group receiving a 0.9% saline solution (NSS). The study results revealed that monodisperses of CL showed a smooth surface and distinct boundaries, with an average size of 151.50 ± 0.46 nm and a narrow size distribution of 0.25 ± 0.01. The liposomal particles showed high entrapment efficiency of 96.45% ± 0.41%, with a ζ-potential of −60.80 ± 1.01 mV and a release rate of 50% of colistimethate sodium within the first 480 min. The CL induced nephrocytotoxicity in a concentration- and time-dependent manner. However, CS had notably lower IC<inf>50</inf> values compared to its liposome preparations at 48 and 72 h (p < 0.05). In vivo study results show that serum levels of symmetric dimethylarginine (SDMA) and total white blood cell count (WBC) were significantly lower in the CL group (SDMA = 8.33 ± 1.70 μg/dL; WBC = 7.29 ± 0.99 log<inf>10</inf> cells/mL) compared to the CS group (SDMA = 15.00 ± 1.63 μg/dL; WBC = 9.73 ± 0.51 log<inf>10</inf> cells/mL). Our study findings enhance the understanding of the safety profile of CL and its potential to improve patient outcomes through the use of liposomal colistin medication. Additional clinical studies are necessary to establish the optimal safety regiment in humans.
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Cytotoxic and antibacterial depsidones from the endophytic fungus Chaetomium brasiliense isolated from Thai rice
(2022-01-01)
Promgool, Trinop
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Kanokmedhakul, Kwanjai
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Leewijit, Thianrat
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Song, Jiaojiao
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Soytong, Kasem
Four new depsidones, mollicellins V-Y (1-4), together with eight known depsidones (5-12) were isolated from the endophytic fungus, Chaetomium brasiliense, detached from stems of Thai rice. Their structures were determined by extensive spectroscopic methods. Mollicellins X, H, and F (3, 8 and 10) showed potent cytotoxicity against the human oral epidermoid carcinoma (KB) cell line, and mollicellin F (10) also showed a potent cytotoxicity against the human hepatocellular carcinoma (HepG2) cell line. Besides, mollicellin B (11) exhibited cytotoxicity against the colorectal adenocarcinoma (HT-29) cell line. Moreover, most of the isolated depsidones displayed potent antibacterial activity against Gram-positive bacteria, Bacillus cereus and Bacillus subtilis, and several of them showed moderate activity against Methicillin-resistant Staphylococcus aureus (MRSA) and clinical isolates of S. aureus. In addition, a few of them also showed moderate activity against a Gram-negative bacteria Pseudomonas aeruginosa.
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New Pyrrolobenzoxazine Sesquiterpenoid Derivatives from the Fungus Talaromyces trachyspermus
(2021-07-13)
Chaiyosang, Boonyanoot
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Kanokmedhakul, Kwanjai
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Soytong, Kasem
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Poeaim, Supattra
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Soytong, Mayamor
Three new pyrrolobenzoxazine sesquiterpenoids, talatrachyoxazines A-C (1-3), together with fourteen known compounds (4-17), were isolated from the fungus Talaromyces trachyspermus EU23. Their structures were identified by spectroscopic evidence and mass spectrometry. The absolute configurations of 1-3 were determined by NOESY data and comparison of their calculated and experimental electronic circular dichroism (ECD) spectra. Compound 1 showed cytotoxic activity against HelaS3, KB, HT-29, MCF-7, and HepG2 cell lines with IC50 values of 7, 11, 10, 12, and 10 μM, respectively. Compounds 1 and 14 showed weak antibacterial activity against the gram-positive bacteria Bacillus cereus and Bacillus subtilis, while 1-3 and 14 showed weak antibacterial activity against the gram-negative bacterium Pseudomonas aeruginosa. In addition, compound 1 showed weak antibacterial activity against Escherichia coli.
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Neuroprotective potential of new chromones isolated from the soil actinomycete Microbispora sp. TBRC6027
(2021-01-01)
Kittisrisopit, Suchada
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Bunbamrung, Nantiya
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Thawai, Chitti
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Tadtong, Sarin
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Niemhom, Nantawan
Nine new chromone analogs (1–9) were isolated from the soil actinomycete Microbispora sp. TBRC6027. The chemical structures were determined based upon NMR spectroscopic methods. These compounds were evaluated in vitro by using P19-derived neurons for neuroprotective activity against oxidative stress induced by serum deprivation and showed % viability of neurons at the concentration of 1 ng/mL varied from 43.51% to 52.99% without significant neurotoxicity for P19-derived neurons at the same concentration. Moreover, all tested compounds were inactive for antibacterial activity against both Gram-positive and Gram-negative bacteria and for cytotoxicity against MCF-7 (human breast cancer) and Vero cells at maximum tested concentration 50 μg/mL. However, compounds 4, 6, and 7 displayed weak cytotoxicity against NCI-H187 (human small-cell lung cancer) cells with IC<inf>50</inf> in a range of 87.99–91.57 μM.
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Multilayer nanocoating of Foley urinary catheter by chlorhexidine-loaded nanoparticles for prolonged release and anti-infection of urinary tract
(2020-11-21)
Srisang, Siriwan
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Wongsuwan, Nattarat
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Boongird, Atthaporn
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Ungsurungsie, Malyn
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Wanasawas, Pimphaka
Two types of chlorhexidine-loaded nanoparticles (CHX-loaded nanoparticles) were prepared: poly(ethylene glycol)-block-poly(ε-caprolactone) micelles and poly(ε-caprolactone) nanospheres. They were prepared by the solvent evaporation method and were used to coat the Foley urinary catheters. The 90 bilayers of dip coating with chlorhexidine-micelles and the 40 cycles of spray coating with chlorhexidine-nanospheres were investigated. The coating provided the CHX content as high as 93.59 ± 9.14 μg/cm<sup>2</sup> and the thickness of coating was 9.17 ± 0.08 μm. Coated catheters were also investigated in the in vitro chlorhexidine-release, antibacterial activity, and cytotoxicity. CHX release from the coated catheters was controlled. The bacteria proliferation was inhibited up to 28 days and showed the reduction of bacteria on the coated catheter surface. Coated catheters showed no biofilm on the surface. In addition, the cytotoxicity showed no cytotoxic effect from the coating. These nanocoating systems promoted potential uses for indwelling catheter and urinary tract infection.
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Bioactive xanthoquinodins and epipolythiodioxopiperazines from Chaetomium globosum 7s-1, an endophytic fungus isolated from Rhapis cochinchinensis (Lour.) Mart
(2020-02-16)
Tantapakul, Cholpisut
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Promgool, Trinop
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Kanokmedhakul, Kwanjai
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Soytong, Kasem
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Song, Jiaojiao
A new xanthoquinodin B9 (1), together with two known xanthoquinodins, xanthoquinodin A1 (2) and xanthoquinodin A3 (3), three epipolythiodioxopiperazines, chetomin (4), chaetocochin C (5) and dethio-tetra(methylthio)chetomin (6), and four other compounds, chrysophanol (7), emodin (8), alatinone (9), and ergosterol (10) were isolated from the endophytic fungus Chaetomium globosum 7s-1, isolated from Rhapis cochinchinensis (Lour.) Mart. All isolated structures were established based on their spectroscopic data analyses. Compounds 1–6 showed antibacterial activity against Gram positive bacteria with MICs ranging from 0.02 pM to 10.81 µM. Compounds 1–6 also exhibited cytotoxicity against KB, MCF-7 and NCI-H187 cancer cell lines (IC<inf>50</inf> 0.04–18.40 µM). However, they were cytotoxic towards a normal cell line (Vero cell) with IC<inf>50</inf> values ranging from 0.04 to 3.86 µM.
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Types A and D Trichothecene Mycotoxins from the Fungus Myrothecium roridum
(2019-07-01)
Lakornwong, Waranya
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Kanokmedhakul, Kwanjai
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Soytong, Kasem
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Unartngam, Arm
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Tontapha, Sarawut
Chromatographic separation of extracts from the fungal biomass of a plant pathogenic fungus, Myrothecium roridum, yielded 8 trichothecene toxins including 6 type D trichothecenes (1 - 6) and 2 type A trichothecenes (7 - 8). 6′,12′-Epoxymyrotoxin A (1) and 7′-hydroxymytoxin B (2) were new macrocyclic trichothecenes, while the other trichothecenes were identified as myrotoxin B (3), myrotoxin D hydrate (4), 2′,3′-epoxymyrothecine A (5), miotoxin A (6), and 2 trichothecenes lacking the macrocyclic lactone system, roridin L-2 (7) and trichoverritone (8). The structures of these mycotoxins were characterized using spectroscopic methods. The absolute configurations of 1 and 2 were determined by NOESY and a comparison of their experimental and calculated ECD spectra. Most of these mycotoxins (1 - 4 and 6) exhibited highly potent antimalarial activity against Plasmodium falciparum. They also showed strong cytotoxicity towards KB and NCI-H187 cell lines (IC <inf>50</inf> 0.60-112.28 nM), as well as the Vero cell line (IC <inf>50</inf> 1.50-46.51 nM).
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Design, synthesis, and evaluation of the anticancer activity of 2-amino-aryl-7-aryl-benzoxazole compounds
(2017-11-01)
Khajondetchairit, Patcharaporn
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Phuangsawai, Oraphan
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Suphakun, Praphasri
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Rattanabunyong, Siriruk
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Choowongkomon, Kiattawee
A series of 2-amino-aryl-7-aryl-benzoxazole derivatives have been designed, synthesized, and evaluated as anticancer agents. Fourteen of the compounds exhibited cytotoxic effects toward human A549 lung cancer cells. We found 12l was the most potent with an EC<inf>50</inf> of 0.4 μm, equivalent to the anticancer drug doxorubicin, but had low selectivity following cross screening in monkey kidney Vero cells. Eight of the most potent or most selective compounds were further profiled in additional cell lines (MCF7, NCI-H187, and KB) to better understand their cytotoxic activity. Only compound 12l had a measurable EC<inf>50</inf> in a single cell line (3.3 μm in the KB cell line). Taken together, this data suggest the series as a whole display specific cytotoxicity toward A549 cells. Cheminformatics searches pointed to JAK2 as a possible target. A subset of compounds assayed at this target showed IC<inf>50</inf>s ranging from 10 to 0.08 μm; however, no clear correlation between JAK2 potency and A549 cytotoxicity was observed.
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Mycotoxins from the Fungus Botryotrichum piluliferum
(2017-02-22)
Rajachan, Oue Artorn
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Kanokmedhakul, Kwanjai
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Soytong, Kasem
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Kanokmedhakul, Somdej
Two new sterigmatocystin derivatives, oxisterigmatocystins E and F (1 and 2, respectively), along with nine known compounds, oxisterigmatocystins G and H (3 and 4, respectively), sterigmatocystin (5), N-0532B (6), O-methylsterigmatocystin (7), N-0532A (8), 6-O-methylversicolorin A (9), 6,8-O-dimethylversicolorin A (10), and 8-O-methylaverufin (11), were isolated from the fungus Botryotrichum piluliferum. The structures of these mycotoxins were elucidated by spectroscopic evidence. Among these, compounds 3, 4, and 9 were discovered as natural products for the first time. Compounds 1, 3, and 4 displayed antimalarial activity toward Plasmodium falciparum (IC<inf>50</inf> = 7.9-23.9 μM). In addition, compounds 1-6 and 8-11 exhibited cytotoxicity against KB, MCF-7, and NCI-H187 cell lines (IC<inf>50</inf> = 0.38-78.6 μM). However, compounds 1-9 showed cytotoxic effects against the Vero cell line (IC<inf>50</inf> = 0.65-12.3 μM). This finding should promote awareness of the contamination of B. piluliferum in the food chain and agricultural soil.

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