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Applications of lupeol to manage fungal infections: a promising multi-target molecule.

Lupeol, a pentacyclic triterpene found in various plant species, has gained prominence due to its antioxidant, anticancer, anti-inflammatory, antifungal properties, along with its low toxicity. In view of the increasing resistance to antifungal agents and the limited therapeutic arsenal available, research on natural bioactive compounds with antimicrobial potential, such as lupeol, has intensified. This review compiles and critically discusses evidence identified through a literature search performed in SciELO, PubMed, Scopus, Web of Science, ScienceDirect, and additional relevant sources for

Engineering Bacopa monnieri for improved bacoside content and its neurological evaluation.

Bacosides are triterpenoidal saponins with numerous pharmacological benefits. One of the significant drawbacks is the low availability of these bacosides. The bacoside pathway is not well elucidated, and there is no prior report of a metabolic engineering approach in this plant. In this study, we have over-expressed the active isoform of Bacopa monnieri squalene synthase (BmSQS1-OE) and silenced the B. monnieri G10H (BmG10H-1-KD), the competitive metabolic pathway, to divert the flux towards triterpene biosynthesis. Absolute quantification of bacosides in these BmSQS1(OE)-BmG10H1(KD) lines has

The journey of boswellic acids from synthesis to pharmacological activities.

There has been a lot of interest in using naturally occurring substances to treat a wide variety of chronic disorders in recent years. From the gum resin of Boswellia serrata and Boswellia carteri, the pentacyclic triterpene molecules known as boswellic acid (BA) are extracted. We aimed to provide a detailed overview of the origins, chemistry, synthetic derivatives, pharmacokinetic, and biological activity of numerous Boswellia species and their derivatives. The literature searched for reports of B. serrata and isolated BAs having anti-cancer, anti-microbial, anti-inflammatory, anti-arthritic,

Совпадение в полном тексте источника
… The chief constituents of resin are monoterpenes, diterpenes, tetracyclic triterpenes, and pentacyclic triterpenes. … BAs are pentacyclic triterpenes that majorly contribute to the Boswellia resin composition. …

Nephrotoxicity assessment of Esculentoside A using human-induced pluripotent stem cell-derived organoids.

Drug-induced nephrotoxicity is a leading cause of acute kidney injury (AKI). A major obstacle in predicting AKI is the lack of a comprehensive experimental model that mimics stable and physiologically relevant kidney functions and accurately reflects the changes a drug induces. Organoids derived from human-induced pluripotent stem cells (iPSCs) are promising models because of their reproducibility and similarity to the in vivo conditions. In this study, Esculentoside A, the triterpene saponin with the highest concentration isolated from the root of Phytolacca acinose Roxb., was used to induce

First Evidence of Gastroprotection by Schinus molle: Roles of Nitric Oxide, Prostaglandins, and Sulfhydryls Groups in Its Mechanism of Action.

Schinus molle is a plant traditionally used in Mexico to treat gastric disorders. However, no scientific evidence has been reported on its gastroprotective effect. The aim of the current contribution was to conduct a bioassay-guided study on S. molle to evaluate its gastroprotective activity in a model of Wistar rats given ethanol orally to induce gastric lesions. The hexane and dichloromethane extracts from the tested plant showed over 99% gastroprotection at a dose of 100 mg/kg. From the hexane extract, two of the three fractions (F1 and F2) afforded over 99% gastroprotection. The F1 fractio

Ex-vivo intestinal absorption study of boswellic acid, cyclodextrin complexes and poloxamer solid dispersions using everted gut sac technique.

Acetyl- Keto-β-boswellic acid (AKBA) is a pentacyclic triterpenic acid found in gum resin of Boswellia serrata. Even though it is shown to have anti-inflammatory activity, its bioavailability gets limited due to its poor aqueous solubility and permeability. The present study, hence, deals in enhancement of the intestinal absorption of AKBA from total boswellic acid fraction (TA fraction) using cyclodextrin (CD) and poloxamer solid dispersion (PXM SDs) formulations. Absorption studies were performed using the everted gut sac model prepared from rat jejunum. The glucose uptake assay was performe

Molecular evidence for better efficacy of hypocrellin A and oleanolic acid combination in suppression of HCC growth.

Hepatocellular carcinoma (HCC) is one of the most frequently occurring cancer worldwide and the fifth most common malignancy. The Hippo pathway has been found to play a critical role in cancer development. YAP, a transcriptional coactivator, is the major downstream effector of the Hippo signaling pathway. Hypocrellin A (HA), a natural perylenequinone light-sensitive compound, is usually used for the therapy of eukoplakia of the vulva and keloids in China. Oleanolic acid (OA), a pentacyclic triterpene compound, is prevalent in the treatment of human liver diseases such as viral hepatitis. In th

Synthesis and Biological Evaluations of Cytotoxic and Antiangiogenic Triterpenoids-Jacaranone Conjugates.

BACKGROUND: The development of antiangiogenic agents arises as a more effective and selective therapeutic approach for the treatment of cancer. In addition to reduced acute toxicity, the efficacy of chemotherapy could be improved when administered in combination specific antiangiogenic with cytotoxic agents. The conjugation or hybridization of bifunctional molecules is one of the alternative rational design strategies for co-administration of anticancer drugs. OBJECTIVE AND METHODS: The goal of this work is to prepare the conjugates of an antiangiogenic triterpene, 3-oxo oleanolic acid, and s

Pachymic acid inhibits growth and induces apoptosis of pancreatic cancer in vitro and in vivo by targeting ER stress.

Pachymic acid (PA) is a purified triterpene extracted from medicinal fungus Poria cocos. In this paper, we investigated the anticancer effect of PA on human chemotherapy resistant pancreatic cancer. PA triggered apoptosis in gemcitabine-resistant pancreatic cancer cells PANC-1 and MIA PaCa-2. Comparative gene expression array analysis demonstrated that endoplasmic reticulum (ER) stress was induced by PA through activation of heat shock response and unfolded protein response related genes. Induced ER stress was confirmed by increasing expression of XBP-1s, ATF4, Hsp70, CHOP and phospho-eIF2α. M

Protective effects of esculentic acid against endotoxic shock in Kunming mice.

Esculentic acid (EA), a triterpene compound extracted from the root of Phytolacca esculenta (the Chinese name Shang Lu), has been widely used to therapy a variety of inflammatory diseases such as rheumatoid arthritis, edema, hepatitis and bronchitis. The present study was designed to investigate the protective effects of EA against LPS-induced endotoxic shock by the intraperitoneal injection of EA (1, 5 and 10 mg/kg) prior to LPS stimulation (1 mg/kg, i.p.). We examined the effects of EA on the survival rate of mice, inflammatory cytokine and pro-inflammatory mediator production, histopatholog

Analysis of the mechanism of antinociceptive action of niga-ichigoside F1 obtained from Rubus imperialis (Rosaceae).

We have previously verified that niga-ichigoside F(1) (NI), a triterpene isolated from Rubus imperialis, exhibits significant and potent antinociceptive action when evaluated in some pharmacological models of pain in mice. This effect was confirmed in other experimental models and also the mechanism of action has been evaluated. The antinociception caused by NI (60 mg kg(-1)) in both phases of the formalin test was significantly attenuated by intraperitoneal injection of mice with haloperidol (a dopaminergic antagonist, 0.20 mg kg(-1)) and L-arginine (precursor of nitric oxide, 600 mg kg(-1)).

Design and Synthesis of Betulinic Acid Derivatives as Antifibrotic Agents for Liver Fibrosis.

Hepatic fibrosis is a major contributor to liver-related mortality and overall mortality. Currently, there is no established treatment for hepatic fibrosis. Research indicates that the transforming growth factor (TGF-β) signaling pathway is one of the key pathways involved in hepatic stellate cell (HSC) activation and fibrosis progression. Consequently, inhibiting the TGF-β signaling pathway represents a potential therapeutic strategy to combat hepatic fibrosis progression. Betulinic acid (BA) was widely extractable from natural plants, exhibits significant antifibrotic therapeutic effects. Th

Ameliorating immune-dependent inflammation and apoptosis by targeting TLR4/MYD88/NF-κB pathway by celastrol mitigates the diabetic reproductive dysfunction.

This study aimed to examine the protective effect of celastrol on testicular dysfunction in diabetic rats and the potential underlying mechanisms. All rats included in the study were divided into four groups: a control group treated with sodium citrate buffer and vehicle), a celastrol-treated control group, a streptozotocin (STZ)-induced diabetic group following insulin resistance, and a celastrol-treated diabetic group. Serum glucose, triglyceride, total cholesterol, high-density lipoprotein cholesterol, interleukin (IL)-1β, tumor necrosis factor-α, and testosterone levels were measured. In a

Natural pentacyclic triterpenoid as allosteric modulators of human 5-lipoxygenase with potential anti-inflammatory activity.

This study explored new methods to inhibit human 5-lipoxygenase (5-hLOX) by analyzing natural terpenes that share structural similarities with acetoxyboswellic acid (AKBA). Enzymatic assays were used to evaluate the terpene's ability to inhibit the enzyme, potentially providing anti-inflammatory benefits. Our research focused on how certain types of triterpenes can inhibit 5-hLOX allosterically via a newly discovered allosteric site identified by enzyme crystallization. To determine whether natural boswellic acid analogs mimicked the allosteric known inhibitor AKBA, we combined 5-hLOX inhibiti…

Influence of verapamil on pharmacokinetics of pristimerin in rats.

The aim of this study was to investigate the effects of verapamil on the pharmacokinetics of pristimerin in rats. A sensitive and reliable LC-MS/MS method was developed and applied for the determination of pristimerin in rat plasma. The pharmacokinetics of orally administered pristimerin with and without verapamil pretreatment was investigated. The results indicated that, when the rats were pretreated with verapamil, the peak concentration of pristimerin increased from 189.13 to 277.53 ng/mL (46.7%), and the AUC0-t increased by approximately 82.0%. Additionally, the effects of verapamil on the

Liposomal-lupane system as alternative chemotherapy against cutaneous leishmaniasis: macrophage as target cell.

Leishmania amazonensis causes human diseases that range from self-healing to diffusion cutaneous lesions. The chemotherapy of leishmaniasis requires long-term treatment and has been based on the use of pentavalent antimonials. Liposomes have been used as antileishmanial drug carries and have adjuvant activity in vaccines against several microorganisms, representing an important option to the development of new therapeutics for the disease. In this study, we developed a liposomal formulation containing lupane [3β,6β,16β-trihydroxylup-20(29)-ene], isolated from fruits of Combretum leprosum with

Intelligence metabolic analysis combined with bioinformatics for investigating effect substance of Naoxintong capsule in treating carotid artery thrombosis.

Naoxintong capsule (NXT) is a typical Chinese patent medicine clinically employed to treat the cardiovascular and cerebrovascular disease. H … cially including phthalides, monoterpene glycosides, diterpene ketones, phenolic acids, flavonoids, triterpenes) were screened out based on the key targets (including PTGS1 and PTGS2). The comprehensive strategy has been established to clarify the main active components and action mechanism for Chinese patent medicine treating related disease, which provide a …

Discovery, Biomanufacture, and Derivatization of Licorice Triterpenoids.

Triterpenoids are the major active constituents of licorice, a well-known traditional medicinal herb. Licorice triterpenoids, represented by … view provides new insights into the discovery and synthesis of pharmaceuticals derived from natural triterpenes.

Antimicrobial, Cytotoxic, and Anti-Inflammatory Activities of Tigridia vanhouttei Extracts.

In this work, bulb extracts of Tigridia vanhouttei were obtained by maceration with solvents of increasing polarity. The extracts were evalu … groups, or esters. The GC-MS profile of extracts revealed the presence of phytosterols, tetracyclic triterpenes, multiple fatty acids, and sugars. This report confirms the antimicrobial, cytotoxic, and anti-inflammatory activities of T. vanhouttei.

Bioassay-Guided Isolation of Antiplasmodial Compounds from Hypericum lanceolatum Lam. (Hypericaceae) and Their Cytotoxicity and Molecular Docking.

In Cameroon, malaria is still the cause of several deaths yearly and leading to the continued search for new potent leads to fight against P … by their spectrometric data as two xanthones 1,6-dihydroxyxanthone (1) and norathyriol (2) and two triterpenes betulinic acid (3) and ursolic acid (4). In the antiplasmodial assay against P. falciparum 3D7, the triterpenoids 3 and 4 displayed the most significant potencies with IC50 values of 2.8 ± 0.8 μg/mL and 11.8 ± 3.2 μg/mL, respectively. Furthermore, b …