Carnivorous plants have fascinated researchers and hobbyists for centuries because of their mode of nutrition which is unlike that of other plants. They are able to produce bioactive compounds used to attract, capture and digest prey but also as a defense mechanism against microorganisms and free radicals. The main purpose of this review is to provide an overview of the secondary metabolites with significant biological activity found in the Sarraceniaceae family. The review also underlines the necessity of future studies for the biochemical characterization of the less investigated species. Darlingtonia, Heliamphora and Sarracenia plants are rich in compounds with potential pharmaceutical and medical uses. These belong to several classes such as flavonoids, with flavonol glycosides being the most abundant, monoterpenes, triterpenes, sesquiterpenes, fatty acids, alkaloids and others. Some of them are well characterized in terms of chemical properties and biological activity and have widespread commercial applications. The review also discusses biological activity of whole extracts and commercially available products derived from Sarraceniaceae plants. In conclusion, this review underscores that Sarraceniaceae species contain numerous substances with the potential to advance health. Future perspectives should focus on the discovery of new molecules and increasing the production of known compounds using biotechnological methods.

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Secondary Metabolites with Biomedical Applications from Plants of the Sarraceniaceae Family

BACKGROUND: Natural products and their derivatives, particularly secondary metabolites, have been recognized for many years as an important source of therapeutic agents. In this context, pentacyclic triterpene acids including betulinic acid (BA), oleanolic acid (OA), and ursolic acid (UA) are highly valuable triterpenic acids because of their wide range of biological activities.


AIM: Therefore, the aim of our study was to investigate any potential effect of BA, UA, and OA on human melanoma WM-266-4 cells’ proliferation activity.


METHODS: BA, UA, and OA have been prepared in dimethyl sulfoxide in concentration range from 0.002 to 200 μM separately or in selected combination (UA+OA ratio 1:1 or 3.5:1), while cells in cell culture medium served as controls. The rapid colorimetric MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay was used to measure proliferation activity of the metastatic melanoma cell line WM-266-4 after being exposed to selected concentrations of BA, UA, OA, or UA+OA and during different time periods. Student’s t-test was used for single statistical comparisons. Data were analyzed using IBM SPSS 25.0 (IBM Corp., Armonk, NY). To account for multiple comparisons bias, p < 0.001 was considered statistically significant.


RESULTS: Our results showed decreased cell proliferation activity after 4 h of incubation of WM-266-4 cells with BA, UA, OA, and UA+OA. The highest inhibitory effect was noted when cells were incubated with selected triterpenic acids and both combinations of UA+OA during the incubation period of 48 h. When compared to control cells, concentration of 2 μM was the lowest concentration of BA that showed a significant decrease of the cells’ proliferation activity regardless the incubation period (4 h, 24 h, and 48 h) (p < 0.001).

CONCLUSION: Our encouraging results could be a good starting point for further studies on possible use of BA, UA, and OA in prevention and treatment of metastatic melanoma.

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Antiproliferative Activity of Selected Triterpene Acids from Rosemary on Metastatic Melanoma Cell Line WM-266-4

Ipomoea pes-caprae (Linn.) R. Br. (Convolvulaceae) is a halophytic plant that favorably grows in tropical and subtropical countries in Asia, America, Africa, and Australia. Even though this plant is considered a pan-tropical plant, I. pes-caprae has been found to occur in inland habitats and coasts of wider areas, such as Spain, Anguilla, South Africa, and Marshall Island, either through a purposeful introduction, accidentally by dispersal, or by spreading due to climate change. The plant parts are used in traditional medicine for treating a wide range of diseases, such as inflammation, gastrointestinal disorders, pain, and hypertension. Previous phytochemical analyses of the plant have revealed pharmacologically active components, such as alkaloids, glycosides, steroids, terpenoids, and flavonoids. These phytoconstituents are responsible for the wide range of biological activities possessed by I. pes-caprae plant parts and extracts. This review arranges the previous reports on the botany, distribution, traditional uses, chemical constituents, and biological activities of I. pes-caprae to facilitate further studies that would lead to the discovery of novel bioactive natural products from this halophyte.

https://www.mdpi.com/1660-3397/20/5/329/pdf?version=1652793353

A Medicinal Halophyte Ipomoea pes-caprae (Linn.) R. Br.: A Review of Its Botany, Traditional Uses, Phytochemistry, and Bioactivity

In the last few decades, studies on autophagy regulation and its potential role in cancer therapeutics have expanded to include detailed mechanisms. Since apoptosis exhibits drug resistance in some cancers, efforts have focused on searching for compounds with autophagy modulating properties. Numerous natural compounds have been used in cancer treatment and are considered a significant research area due to their remarkable anti-cancer properties. Celastrol, a quinone methide triterpene, derived from Tripterygium wilfordii, has recently drawn much attention because of its anticancer potential. It enhances tumor suppression and induces autophagy in cancer cells by regulating signaling pathways such as Beclin-1, Akt/mTOR, ROS, NF-κB, MAPK, HSP90, and the proteasome. In the current study, we address the anticancer potential of celastrol, its effect on various cellular pathways, and describe how it functions as an autophagy modulator in cancer therapeutics and helps diminish multidrug resistance in cancer cells.

/pdf/celastrol-mediated-autophagy-regulation-in-cancer-3tewjzlac8.pdf

Celastrol-mediated autophagy regulation in cancer

Unusually cyclized triterpenoids: occurrence, biosynthesis and chemical synthesis.

Myrrh, a resin derived from the damaged bark of Commiphora genus, has traditionally been used for treatment of various human diseases, such as amenorrhea, ache, tumors, fever, and stomach pains. In spite of this widespread use of the myrrh in Ethiopia, the pharmacological activity and chemical composition have not been studied in detail. A new tricyclic triterpene acid (3S,4S,14S,7E,17E,21Z)-3,30-dihydroxypodioda-7,17,21-trien-4-carboxylic acid (commafric A) has been isolated from a crude methanolic extract of Commiphora africana (A. Rich.) Engl. resin along with the known pentacyclic triterpene α-amyrin. The structure of commafric A was characterized using different spectroscopic techniques such as 1D and 2D NMR, IR, and VCD combined with computations. The anti-proliferative activity of both isolated compounds was evaluated using SRB based colorimetric cellular assay against four human cancer cell lines. Etoposide was used as a positive control. Commafric A showed significant anti-proliferative effects against non-small cell lung cancer (A549) with IC50 values of 4.52 μg/ml. The pentacyclic triterpene α-amyrin showed a weak anti-proliferative activity against A2780 (ovarian cancer), MIA-PaCa-2 (pancreatic cancer), and SNU638 (stomach cancer) cell lines tested with IC50 values ranging 9.28 to 28.22 μg/ml. Commafric A possessed anti-proliferative activity against non-small cell lung cancer (A549), which suggests that commafric A has potential to be further optimized being a lead compound in the search for new drugs against cancer diseases.

/pdf/anti-proliferative-activity-of-a-novel-tricyclic-1vsnl0jhxc.pdf

Anti‑proliferative activity of a novel tricyclic triterpenoid acid from Commiphora africana resin against four human cancer cell lines

The present invention relates to a novel benzothiophene derivative, a pharmaceutically acceptable salt thereof or an optical isomer thereof, a method for preparing same, and a pharmaceutical composition, containing same as an active ingredient, for preventing or treating a viral disease.

Novel benzothiophene derivative, pharmaceutically acceptable salt thereof or optical isomer thereof, method for preparing same, and pharmaceutical composition, containing same as active ingredient, for preventing or treating viral disease

A number of strategies through structural modification of pyridinium oximes have been developed to circumvent the Blood-Brain Barrier (BBB). Some of the attempted examples are (1) enhancement of lipophilicity by introduction of a fluorine atom into pyridinium ring, (2) facilitation of glucose transporters introduction of glucose moiety on the pyridinium nitrogen, (3) use of a prodrug by uncharged dihydropyridyl moiety, etc One of the strategies that our group tried was the introduction of fluorine atoms into the heterocyclic ring of pyridinium oximes to increase their lipophilicity.1 In our continuing effort towards the development of new oxime reactivators, we were interested in monoquaternary pyridinium oximes with N-alkyl side chains, because oximes with hydrophobic side chains may penetrate the BBB more easily than 2-PAM with an N-methyl side chain. We also investigated bis-pyridinium oximes with diethyl ether linker between two pyridine rings. The synthesized pyridinium oximes were evaluated their inhibitory activities on AChE, as well as their potency to reactivate AChE inhibited by paraoxon organophosphorus agent. The plasma and brain disposition of oximes were evaluated in male ICR mice, and the oximes concentrations in the plasma and brain were measured by LC-MSMS analysis. Therefore, KR-26256 which is a bis-pyridinium oxime showed higher brain concentration as well as better brain/plasma ratio compared with HI-6.

Sang Ho Lee

Papers

Anti‑proliferative activity of a novel tricyclic triterpenoid acid from Commiphora africana resin against four human cancer cell lines

Novel benzothiophene derivative, pharmaceutically acceptable salt thereof or optical isomer thereof, method for preparing same, and pharmaceutical composition, containing same as active ingredient, for preventing or treating viral disease

Brain exposure of bis-pyridinium oxime kr-26256