Christian Bailly

• Expert at Oncowitan

Medicinal plants from the genus Saururus are commonly used to treat inflammatory pathologies. They contain numerous bioactive compounds, notably the polycyclic lignan sauchinone from the species Saururus chinensis. An in-depth analysis of benzoxanthenone lignans related to sauchinone, and the analogous products carpanone and polemannones, has been...

A variety of sulfur‐containing small molecules can be found in the spears of asparagus ( Asparagus Officinalis L.) including compounds derived from asparagusic acid such as the amino acid derivatives asparaptines A, B, and C. The previous characterization of asparaptine A as an inhibitor of angiotensin‐converting enzyme (ACE) prompted us to compare...

Background/Objectives: Microcolins A–M are cytotoxic marine lipopeptides produced by the cyanobacterium Moorena producens, also known as Lyngbya majuscula. Recent studies have shown that two compounds in the series, microcolins B and H, can form covalent complexes with phosphatidylinositol transfer proteins α and β (PITPα/β) upon the reaction of th...

The genus Ruspolia refers to a small group of plants in the Acanthaceae family, with two dominant species R. decurrens and R. hypocrateriformis essentially distributed in tropical parts of Africa. Decoctions from these plants are used in folk medicine for the treatment of a few human pathologies but the active ingredients at the origin of the bioac...

The histone methyltransferase DOT1L (DOT1 like, disruptor of telomeric silencing) is responsible of methylation of H3K79, leading to oncogene transcription, and its involved in the development of different types of...

Inhibitors of monoamine oxidases (MAOs) are of interest for the treatment of neurodegenerative disorders and other human pathologies. In this frame, the present work describes different synthetic strategies to obtain MAO inhibitors via the coupling of the aminocoumarin core with arylsulfonyl chlorides followed by copper azide-alkyne cycloaddition,...

Aim: New microtubule-targeting agents are needed to improve cancer treatment. The recent characterization of the anticancer alkaloid securinine as a tubulin-binding agent prompted us to explore the interaction of related monomeric and dimeric analogues with tubulin. The interaction between the α/β-tubulin dimer and alkaloids fluevirines A–F and flu...

The medicinal plant Securinega virosa (Roxb ex. Willd) Baill., also known as Flueggea virosa (Roxb. ex Willd.) Royle, is commonly used in traditional medicine in Africa and Asia for the management of diverse pathologies, such as parasite infections, diabetes, and gastrointestinal diseases. Numerous alkaloids have been isolated from the twigs and le...

Different types of limonoids have been isolated from plants of the Chisocheton genus, notably from the species Chisocheton ceramicus Miq. which is largely distributed in the Indonesian archipelago and Malaysia region. A variety of natural products have been found in the bark of the tree and characterized as antimicrobial and/or antiproliferative ag...

Tetraspanin CD81 is a transmembrane protein used as a co-receptor by different viruses and implicated in some cancer and inflammatory diseases. The design of therapeutic small molecules targeting CD81 lags behind monoclonal antibodies and peptides but different synthetic and natural products binding to CD81 have been identified. We have investigate...

Limonoids are extremely diversified in plants, with many categories of products bearing an intact, rearranged or fragmented oxygenated scaffold. A specific subgroup of fragmented or degraded limonoids derives from the tetranortriterpenoid prieurianin, initially isolated from the tree Trichilia prieuriana but also found in other plants of the Meliac...

Ephedra species are among the most popular herbs used in traditional medicine for a long time. The ancient Chinese medical book “Treatise on Febrile Diseases” refers to the classic traditional Chinese medicine prescription Ge Gen decoction, which consists of seven herbs, including an Ephedra species. Ephedra species are utilized all over the world...

The yellow-flowering plant Cladanthus arabicus (L.) Cass., commonly called Arabian Cladanthus or palm springs daisy, is typical of the West Mediterranean region and is particularly abundant in Morocco. The plant is used in traditional Moroccan medicine for the treatment of diabetes and other ailments. Over the past 20 years, this abundant wild plan...

The white berry bush, officially Flueggea virosa (Roxb. ex Willd.) Royle is a medicinal plant distributed throughout tropical areas and traditionally used in Africa, India and China. Root decoctions are used to treat abdominal pain, whereas extracts from the aerial parts serve to treat liver and urinary diseases, inflammatory pathologies and diabet...

Background Telmisartan (TLT) is a prototypic angiotensin receptor blocker largely used to treat hypertension worldwide. In addition to its cardioprotective effects, TLT presents pleiotropic activities and notably displays noticeable anti-inflammatory and antitumor effects. The repression of the programmed cell death-1 (PD-1)/programmed death-ligand...

The species Fissistigma oldhamii (Hemsl.) Merr. (Annonaceae) has long been used as a traditional herbal medicine in China to treat diverse human diseases. Decoctions from the roots of the plant (Guā Fù Mù) are used to treat body pain and inflammatory pathologies, such as rheumatic syndromes, sciatica, and osteoarthritis. The phytochemical content o...

Aim: Harzianoic acids A and B (Hz-A/B) are two rare cyclobutene-containing sesquiterpenes isolated from a marine strain of the sponge-associated fungus Trichoderma harzianum. They display anticancer and antiviral effects, reducing the entry of hepatitis C virus (HCV) into hepatocarcinoma cells. The large extracellular loop (LEL) of the tetraspanin...

Ethnopharmacological relevance: The herbal medicine designated Chai-Ling-Tang in China, Siryung-tang in South Korea, and Sairei-To (or Tsumura Saireito extract granules, TJ-114) in Japan is a complex polyherbal formulations with 12 plant components. It is used historically to treat Shaoyang syndrome, recorded in an ancient Chinese medical text "Tr...

The roots of the plant Euphorbia ebracteolata Hayata (Yue Xian Da Ji) are commonly used in traditional Chinese medicine to treat multiple diseases such as chronic liver diseases, oedema, pulmonary diseases and cancer. It is the main ingredient of the TCM called Langdu which can be prepared also from roots of E. fischeriana Steud. and occasionally f...

For more than 40 years, the epipodophyllotoxin drug etoposide is prescribed to treat cancer. This semi-synthetic compound remains extensively used to treat advanced small-cell lung cancer and in various chemotherapy regimen for autologous stem cell transplantation, and other anticancer protocols. Etoposide is a potent topoisomerase II poison, causi...

Among bryophytes, the Plagiochila genus represents a large group of leafy liverworts with over 500 species. Plagiochilins A to X are sesquiterpenoids isolated from Plagiochila species. The lead compound plagiochilin A (Plg-A), endowed with anticancer and antiparasitic properties, has been characterized as a potent mitosis inhibitor, acting selectiv...

Among bryophytes, the Plagiochila genus represents a large group of leafy liverworts, with over 500 species. Plagiochilins A-to-X are sesquiterpenoids isolated from Plagiochila species. The lead compound plagiochilin A (Plg-A), endowed with anticancer and anti-parasitic properties, has been characterized as a potent mitosis inhibitor, acting select...

Orally-active anticancer small molecules targeting the PD-1/PD-L1 immune checkpoint are actively searched. Phenyl-pyrazolone derivatives with a high affinity for PD-L1 have been designed and characterized. In addition, the phenyl-pyrazolone unit acts as a scavenger of oxygen free radicals, providing antioxidant effects. The mechanism is known for t...

Simple Summary Novel therapeutic targets are needed to improve treatments of aggressive cancers and viral diseases. Tetraspanins represent an emerging class of anticancer targets, notably the transmembrane protein CD81 which has been structurally well characterized. CD81 plays key roles in tumor growth and dissemination, and serves as a co-receptor...

The present analysis retraces the discovery of plagiochilins A-to-W, a series of seco-aromadendrane-type sesquiterpenes isolated from diverse leafy liverworts of the genus Plagiochila. Between 1978, with the first isolation of the leader product plagiochilin A from P. yokogurensis, and 2005, with the characterization of plagiochilin X from P. asple...

N-glycosylation of eukaryotic proteins plays roles in protein folding, trafficking, and signal transduction. The biological influence of the process is well understood, whereas the pharmacological impact of protein N-glycosylation is not well under discerned. The role of N-glycosylation on drug binding to protein has been rarely studied. We have mo...

The antitumor drug topotecan (TPT) is a potent inhibitor of topoisomerase I, triggering DNA breaks lethal for proliferating cancer cells. The mechanism is common to camptothecins SN38 (the active metabolite of irinotecan) and belotecan (BLT). Recently, TPT was shown to bind the ribosomal protein L15, inducing an antitumor immune activation independ...

The genus Ruta in the family Rutaceae includes about 40 species, such as the well-known plants R. graveolens L. (common rue) or R. chalepensis L. (fringed rue), but also much lesser-known species such as R. angustifolia Pers. (narrow-leaved fringed rue). This rue specie, originating from the Mediterranean region, is well-distributed in Southeast As...

Immune checkpoints inhibition is a privileged approach to combat cancers and other human diseases. The TIM-3 (T cell immunoglobulin and mucin-domain containing-3) inhibitory checkpoint expressed on different types of immune cells is actively investigated as an anticancer target, with a dozen of monoclonal antibodies in (pre)clinical development. A...

Introduction: The quest for small molecule inhibitors of the PD-1/PD-L1 checkpoint continues in parallel to the extensive development of monoclonal antibodies directed against this immune checkpoint. Drug screening strategies are being set up to identify novel PD-L1 inhibitors. Methods: A virtual screening based on molecular docking with the PD-...

Cryptoconcatones A-L represent a series of 12 dihydropyrone derivatives isolated from the evergreen tree Cryptocarya concinna Hance, which is well distributed in southeast Asia. The lead compound in the series, cryptoconcatone L, has revealed antiproliferative activity against cultured cancer cells but its mechanism of action remains unknown. Based...

Neglected tropical parasitic diseases (NTD) are prevalent in many countries and cost-effective treatments remain urgently needed. Novel approaches have been proposed to address these diseases through an action on immune co-inhibitory checkpoints which are exploited by parasites to evade the immune system. Among these checkpoints, TIM-3 has been sho...

The medicinal plant Artabotrys hexapetalus (synonyms: A. uncinatus and A. odoratissimus) is known as yingzhao in Chinese. Extracts of the plant have long been used in Asian folk medicine to treat various symptoms and diseases, including fevers, microbial infections, ulcers, hepatic disorders and other health problems. In particular, extracts from t...

The para-terphenyl derivative vialinin A (Vi-A), isolated from Thelephora fungi, has been characterized as a potent inhibitor of the ubiquitin-specific protease 4 (USP4). Blockade of USP4 contributes to the anti-inflammatory and anticancer properties of the natural product. We have investigated the interaction of Vi-A with USP4 by molecular modelin...

Objective Bouchardatine (1) is a β-indoloquinazoline alkaloid isolated from the plant Bouchardatia neurococca, acting as a modulator of adipogenesis and lipogenesis, and as an anticancer agent. The natural product functions as an activator of proteins adenosine 5’-monophosphate (AMP)-activated protein kinase (AMPK) and sirtuin 1 (SIRT1). We used mo...

Panduratin A (Pa-A) is a prenylated cyclohexenyl chalcone isolated from the rhizomes of the medicinal and culinary plant Boesenbergia rotunda (L.) Mansf., commonly called fingerroots. Both an ethanolic plant extract and Pa-A have shown a marked antiviral activity against the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), responsible...

More than 100 protostane triterpenoids have been isolated from the dried rhizomes of Alisma species, designated Alismatis rhizoma (AR), commonly used in Asian traditional medicine to treat inflammatory and vascular diseases. The main products are the alisols, with the lead compounds alisol-A/-B and their acetate derivatives being the most abundant...

Epalrestat (EPA) is a potent inhibitor of aldose reductases AKR1B1 and AKR1B10, used for decades in Japan for the treatment of diabetic peripheral neuropathy. This orally-active, brain-permeable small molecule, with a relatively rare and essential 2-thioxo-4-thiazolidinone motif, functions as a regulator intracellular carbonyl species. The repurpos...

The enzyme cystathionine β-synthase (CBS), implicated in the trans-sulfuration pathway, is a target to combat different pathologies including cancers. Various types of CBS inhibitors have been characterized, such as the C-3/C-3ʺ biflavanone sikokianin-C (Sik-C), isolated from the plant Wikstroemia sikokiana. Sik-C, which displays marked anticancer...

The review highlights how protein–protein interactions (PPIs) have determining roles in most life processes and how interactions between protein partners are involved in various human diseases. The study of PPIs and binding interactions as well as their understanding, quantification and pharmacological regulation are crucial for therapeutic purpose...

Monoclonal antibodies targeting the PD-1/PD-L1 immune checkpoint have considerably improved the treatment of some cancers, but novel drugs, new combinations, and treatment modalities are needed to reinvigorate immunosurveillance in immune-refractory tumors. An option to elicit antitumor immunity against cancer consists of using approved and markete...

Small molecule inhibitors of GTPases are increasingly considered for the treatment of multiple human pathologies. The GTPase Rac1 (Ras-related C3 botulinum toxin substrate 1) plays major roles in vital cellular processes, notably in the control cell motility and dynamic, the regulation of oxidative stress, and in inflammatory and immune surveillanc...

DOI: 10.1002/sscp.202200031 The cover picture shows how the reactivity of the phenyl‐pyrazolone drug edaravone in the presence of vanillin, used here as a model aromatic aldehyde. Edaravone (EDA) is an injectable drug commonly used to treat amyotrophic lateral sclerosis, acting as a free radical scavenger to reduce oxidative damages in cells. In ad...

Fungi from the genus Thelephora have been exploited to identify bioactive compounds. The main natural products characterized are para-terphenyl derivatives, chiefly represented by the lead anti-inflammatory compound vialinin A isolated from species T. vialis and T. terrestris. Different series of p-terphenyls have been identified, including vialini...

Bladder pathologies, very common in the aged population, have a considerable negative impact on quality of life. Novel targets are needed to design drugs and combinations to treat diseases such as overactive bladder and bladder cancers. A promising new target is the ubiquitous Rho GTPase Rac1, frequently dysregulated and overexpressed in bladder pa...

Glycogen synthase kinase‐3β (GSK‐3β) is a target enzyme considered for the treatment of multiple human diseases, from neurodegenerative pathologies to viral infections and cancers. Numerous inhibitors of GSK‐3β have been discovered but thus far only a few have reached clinical trials and only one drug, tideglusib (1), has been registered. Natural p...

We have investigated the interaction of the steroidal alkaloid tomatidine (TD) and its glycosylated derivative α-tomatine (αTM) with the 3C-like protease (3CLpro) of PEDV and with the main protease (Mpro) from the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) responsible for COVID-19, using molecular modeling. αTM can generate more s...

Small molecules targeting the PD-1/PD-L1 checkpoint are actively searched to complement the anticancer arsenal. Different molecular scaffolds have been reported, including phenyl-pyrazolone derivatives which potently inhibit binding of PD-L1 to PD-1. These molecules are structurally close to antioxidant drug edaravone (EDA) used to treat amyotrophi...

Naming a newly discovered natural product (NP) is a pleasant but difficult exercise. In most cases, the NP name will be given with reference to the species of origin, be it a plant, a marine organism, a mammalian or microbial species. For a long time, the use of biologically-based trivial names has been recommended to identify the parental linkage...

Platonia insignis Mart., Clusiaceae, or the bacuri tree is found in the Amazon rainforest and several countries of South America. The tree is known for its solid timber, its edible fruit, and some derived products such as the bacuri seed butter used in phytotherapeutic preparations and cosmetics. Many bioactive natural products have been isolated f...

Immuno-therapy has become a leading strategy to fight cancer. Over the past few years, immuno-therapies using checkpoint inhibitor monoclonal antibodies (mAbs) against programmed death receptor 1 (PD-1) and programmed death ligand 1 (PD-L1) have demonstrated improved survival compared with chemotherapy. We describe the microwave-assisted synthesis...

Despite novel targeted and immunotherapies, the prognosis remains bleak for patients with hepatocellular carcinoma (HCC), especially for advanced and/or metastatic forms. The rapid emergence of drug resistance is a major obstacle in the success of chemo-, targeted-, immuno-therapies of HCC. Novel targets are needed. The prominent roles of the small...

Edaravone (EDA) is an antioxidant drug used for the treatment of amyotrophic lateral sclerosis. Edaravone has been shown to react with aldehydes, such as 6‐formylpterin. We investigated the reaction of edaravone with vanillin (used as a model aromatic aldehyde) to evidence the reaction products formed in an aqueous solution. Mono‐ and bis‐adducts v...

The santol tree (Sandoricum koetjape Merr.) is largely distributed in Southeast Asia. It produces useful timber and edible fruits, consumed fresh, and transformed. It has a wide range of traditional medicinal uses for the treatment of inflammatory disorders and digestive troubles. Numerous bioactive natural products have been isolated from the root...

Objective and design Japonicone A (Jap-A) is a sesquiterpene lactone (SL) dimer isolated from the plant Inula japonica Thunb. and the leading compound in the japonicone series of SL dimers which comprises 25 members (Jap-A to Jap-Y). We have analyzed the anticancer properties of Jap-A and the associated molecular targets. Methods All literature da...

Novel affordable medications are needed to treat chronic periodontitis, which is one of the most common dental pathologies worldwide. Extracts prepared from the rhizome of the medicinal plant Boesenbergia rotunda (L.) Mansf., commonly known as fingerroot, are used to treat a variety of human pathologies. These extracts contain potent anti-inflammat...

Background Names of natural products (NP) are usually given depending on the species of origin, be it a plant, a marine organism or a microbial species. In some cases, names have been given with reference to people, animals, music, foods or places. Many NP refer to countries, cities or specific places such as mountains, deserts, seas and oceans. P...

Objective The mangrove tree Xylocarpus granatum J. Koenig (X. granatum) is a medicinal plant used to treat various diseases in several Asian countries. Many bioactive natural products have been isolated from the plants, particularly several groups of limonoids, including 18 xylogranatins (Xyl-A to R), all of which bear a furyl-δ-lactone core common...

The dried flower buds of the plant Daphne genkwa Sieb. et Zucc. have been largely used in traditional Chinese medicine for the treatment of inflammatory diseases. Numerous diterpenoids have been isolated from the Genkwa Flos (yuanhua in Chinese), including a series of daphnane-type diterpene designated as yuanhuacin (YC, often improperly designated...

The tetracyclic phenolic compound brazilin, derived from the wood of Caesalpinia sappan, has been shown to bind to the chromatin protein BAF1 (barrier‐to‐autointegration factor 1), a protein essential to maintain integrity of the nuclear envelope in cells. BAF1 plays a role in cancer development. Using molecular docking, we have located the binding...

The roots of the plant Cynanchum otophyllum C. K. Schneid ( Apocynaceae ), known as Qingyangshen in Chinese, are used for a long time as a traditional medicine by different ethnic communities in the Yunnan province (China). The multiple properties and applications of this herbal medicine have been analyzed. C. otophyllum is a perennial herbal liana...

The disaccharide lactose is an excipient commonly used in pharmaceutical products. The two anomers, α- and β-lactose (α-L/β-L), differ by the orientation of the C-1 hydroxyl group on the glucose unit. In aqueous solution, a mutarotation process leads to an equilibrium of about 40% α-L and 60% β-L at room temperature. Beyond a pharmaceutical excipie...

The bacterial thiopeptide thiostrepton (TS) is used as a veterinary medicine to treat bacterial infections. TS is a protein translation inhibitor, essentially active against Gram-positive bacteria and some Gram-negative bacteria. In procaryotes, TS abrogates binding of GTPase elongation factors to the 70S ribosome, by altering the structure of rRNA...

Amlexanox (AMX) is an azoxanthone drug used for decades for the treatment of mouth aphthous ulcers and now considered for the treatment of diabetes and obesity. The drug is usually viewed as a dual inhibitor of the non-canonical IκB kinases IKK-ɛ (inhibitor-kappaB kinase epsilon) and TBK1 (TANK-binding kinase 1). But a detailed target profile analy...

The pseudoguaianolide-type sesquiterpene lactone (SL) britannin (BRT), found in different Inula species, has been characterized as a potent anticancer agent acting via modulation of the transcription factor NFkB and the Nrf2-Keap1 signaling pathway. In addition, a BRT-induced down-regulation of the immune checkpoint PD-L1 (programmed cell death lig...

Bailly C. 2021. Review: Natural products isolated from Portulaca oleracea (purslane, Ma-Chi-Xian): Focus on oleraciamides and oleracones. Nusantara Bioscience 13: 202-210. The plant Portulaca oleracea L., known as purslane in English and Ma-Chi-Xian in Chinese, is largely used in traditional medicine to treat a variety of diseases and conditions, i...

Ethnopharmacological relevance Extracts of the plant Selaginella tamariscina (P.Beauv.) Spring (spike moss) are used for a long time in Asia, for the treatment of multiple diseases and conditions. Aqueous and alcoholic leave extracts are used by local communities. In China, the plant (Juan bai) is listed on the Pharmacopoeia. In South Korea, the us...

The steroidal glycoalkaloid α-tomatine (αTM) and its aglycone tomatidine (TD) are abundant in the skin of unripe green tomato and present in tomato leaves and flowers. They mainly serve as defensive agents to protect the plant against infections by insects, bacteria, parasites, viruses, and fungi. In addition, the two products display a range of ph...

The roots of the plant Wikstroemia indica (L.) C.A. Mey., also known as Radix Wikstroemiae or Liaogewanggen in China, are used in traditional medicine as decoctions for the treatment of diverse inflammatory diseases, such as arthritis, bronchitis, and many other conditions. A large diversity of bioactive natural products have been characterized in...

Polyprenylated acylphloroglucinols represent an important class of natural products found in many plants. Among them, the two related products oblongifolin C (Ob-C) and guttiferone K (Gt-K) isolated from Garcinia species (notably from edible fruits), have attracted attention due to their marked anticancer properties. The two compounds only differ b...

Sesquiterpene lactones (SLs) are abundant in plants and display a large spectrum of bioactivities. The compound britannin (BRT), found in different Inula species, is a pseudoguaianolide-type SL equipped with a typical and highly reactive α-methylene-γ-lactone moiety. The bioproperties of BRT and related pseudoguaianolide SLs, including helenalin, g...

The renin protein is an upstream enzymatic regulator of the renin-aldosterone-angiotensin system (RAAS) essential for the maintenance of blood pressure. The angiotensin-converting enzyme-2 (ACE2) is a major component of the RAAS and a cell surface receptor exploited by the SARS-CoV-2 virus to enter host cells. A recent molecular modeling study has...

The barrier-to-autointegration factor 1 (BAF1) protein is a DNA-binding protein implicated in nuclear envelop repair and reformation after mitosis. This nuclear protein is frequently overexpressed in cancer cells and plays a role in the occurrence and development of different tumors. It is a potential therapeutic target for gastric cancer, breast c...

Phytolacca (Shanglu) is a well-known traditional herbal medicine that has been used for thousands of years in China. Phytolacca is also used worldwide in different traditional phyto-medicines and homeopathic preparations. The present work reviewed advances in the traditional uses, plant origin, chemical constituents, pharmacology, and medicinal pro...

Extracts of the plant Glycyrrhiza glabra (licorice) are used in traditional medicine to treat malaria. The main active components are the saponin glycyrrhizin (GLR) and its active metabolite glycyrrhetinic acid (GA) which both display activities against Plasmodium falciparum. We have identified three main mechanisms at the origin of their anti-plas...

Bailly C. 2021. Anticancer mechanism of artonin E and related prenylated flavonoids from the medicinal plant Artocarpus elasticus. Asian J Nat Prod Biochem 19: 44-56. Plants of the Artocarpus genus are largely distributed throughout tropical Asia and Oceania. Species such as A. altilis (Parkinson) Fosberg and A. heterophyllus Lam. are popular trees...

The plant Walsura robusta Roxb. (Meliaceae) is a robust tree largely distributed in south-east Asia, including provinces of southern China. A few traditional usages of the plant have been mentioned, notably for the treatment of microbial infections. But experimental studies using different types of plant extracts only revealed modest antibacterial...

The porcine epidemic diarrhea virus (PEDV) and severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) are two highly pathogenic viruses causing tremendous damages to the swine and human populations, respectively. Vaccines are available to prevent contamination and to limit dissemination of these two coronaviruses, but efficient and widely aff...

The plant Machilus thunbergii Siebold & Zucc., known as Makko tree, is distributed in many countries of south Asia: China, Taiwan, Japan, South Korea, Philippines, Vietnam, Cambodia, Laos. The bark of the tree is used for the preparation of incense powder, and the wood is exploited locally. A few applications of the plant in Chinese and Korean trad...

Amyotrophic lateral sclerosis (ALS) is a rare but severe neuro-degenerative disease. Edaravone, an FDA-approved small molecule drug, can slow functional loss and disease progression in ALS, at least during the early stage. This synthetic phenyl-pyrazolone derivative is a potent scavenger of oxygen free radicals but it is also a reactive molecule wh...

Acankoreagenin (ACK, also known as acankoreanogenin and HLEDA) and impressic acid are two lupane‐type triterpenes that can be isolated from various Acanthopanax and Schefflera species. They efficiently block activation of the NF‐κB signaling pathway and the release of proinflammatory cytokines and/or the action of inflammation mediators (HMGB1, iNO...

Upon T-cell receptor stimulation, the Programmed cell Death-1 receptor (PD-1) expressed on T-cells can interact with its ligand PD-L1 expressed at the surface of cancer cells or antigen-presenting cells. Monoclonal antibodies targeting PD-1 or PD-L1 are routinely used for the treatment of cancers, but their clinical efficacy varies largely across t...

Folates (vitamin B9) are essential components of our diet and our gut microbiota. They are omnipresent in our cells and blood. Folates are necessary for DNA synthesis, methylation, and other vital bioprocesses. Folic acid (FA), as the synthetic form of folates, is largely found in supplements and fortified foods. FA and folate drugs are also extens...

Numerous C-21 steroidal glycosides have been isolated from Cynanchum plants. Many of them derive from the aglycone caudatin (CDT) which includes a tetracyclic deacylmetaplexigenin unit and an ikemaoyl ester side chain. CDT can be found in diverse traditional medicines, such as Baishouwu radix used to treat gastro-intestinal disorders. The compound...

The lysosomal enzyme palmitoyl-protein thioesterase 1 (PPT1) removes thioester-linked fatty acid groups from membrane-bound proteins to facilitate their proteolysis. A lack of PPT1 (due to gene mutations) causes the progressive death of cortical neurons and is responsible for infantile neural ceroid lipofuscinosis (INCL), a severe neurodegenerative...

Acankoreagenin (ACK) is a lupane triterpene found in several Acanthopanax and Schefflera plant species. ACK, also known as acankoreanogenin or HLEDA, bears a major structural analogy with other lupane triterpenoids such as impressic acid (IA) and the largely used phytochemical betulinic acid (BA). These compounds display marked anti-inflammatory, a...

Biflavonoids are divided in two classes: C–C type compounds represented by the dimeric compound amentoflavone and C–O–C-type compounds typified by hinokiflavone (HNK) with an ether linkage between the two connected apigenin units. This later sub-group of bisflavonyl ethers includes HNK, ochnaflavone, delicaflavone and a few other dimeric compounds,...