Chemistry, Biological Activities, and Pharmacological Properties of Gastrodin: Mechanism Insights.

Gastrodin, a bioactive compound derived from the rhizome of the orchid Gastrodia elata, exhibits a diverse range of biological activities. With documented neuroprotective, anti-inflammatory, antioxidant, anti-apoptotic, and anti-tumor effects, gastrodin stands out as a multifaceted therapeutic agent. Notably, it has demonstrated efficacy in protecting against neuronal damage and enhancing cognitive function in animal models of Alzheimer's disease, Parkinson's disease, and cerebral ischemia. Additionally, gastrodin showcases immunomodulatory effects by mitigating inflammation and suppressing the expression of inflammatory cytokines. Its cytotoxic activity involves the inhibition of angiogenesis, suppression of tumor growth, and induction of apoptosis. This comprehensive review seeks to elucidate the myriad potential effects of Gastrodin, delving into the intricate molecular mechanisms underpinning its pharmacological properties. The findings underscore the therapeutic potential of gastrodin in addressing various conditions linked to neuroinflammation and cancer.

Bioactive substances of cyanobacteria and microalgae: Sources, metabolism, and anticancer mechanism insights.

Cyanobacteria and microalgae contain various phytochemicals, including bioactive components in the form of secondary metabolites, namely flavonoids, phenolic acids, terpenoids, and tannins, with remarkable anticancer effects. This review highlights the recent advances in bioactive compounds, with potential anticancer activity, produced by cyanobacteria and microalgae. Previous in vitro investigations showed that many of these bioactive compounds exhibit potent effects against different human cancer types, such as leukemia and breast cancers. Multiple mechanisms implicated in the antitumor effect of these compounds were elucidated, including their ability to target cellular, subcellular, and molecular checkpoints linked to cancer development and promotion. Recent findings have highlighted various mechanisms of action of bioactive compounds produced by cyanobacteria and microalgae, including induction of autophagy and apoptosis, inhibition of telomerase and protein kinases, as well as modulation of epigenetic modifications. In vivo investigations have demonstrated a potent anti-angiogenesis effect on solid tumors, as well as a reduction in tumor volume. Some of these compounds were examined in clinical investigations for certain types of cancers, making them potent candidates/scaffolds for antitumor drug development.

Anticancer properties and mechanism insights of α-hederin.

α-Hederin is a natural bioactive molecule very abundant in aromatic and medicinal plants (AMP). It was identified, characterized, and isolated using different extraction and characterization technologies, such as HPLC, LC-MS and NMR. Biological tests have revealed that this natural molecule possesses different biological properties, particularly anticancer activity. Indeed, this activity has been investigated against several cancers (e.g., esophageal, hepatic, breast, colon, colorectal, lung, ovarian, and gastric). The underlying mechanisms are varied and include induction of apoptosis and cell cycle arrest, reduction of ATP generation, as well as inhibition of autophagy, cell proliferation, invasion, and metastasis. In fact, these anticancer mechanisms are considered the most targeted for new chemotherapeutic agents' development. In the light of all these data, α-hederin could be a very interesting candidate as an anticancer drug for chemotherapy, as well as it could be used in combination with other molecules already validated or possibly investigated as an agent sensitizing tumor cells to chemotherapeutic treatments.

Phenolic Profile, Antioxidant, Antidiabetic, and Antigout Potential of Stem Extracts of Four Sweet Cherry Cultivars.

In order to highlight the activities of bioactive compounds present in the stem of sweet cherries, four different cultivars (Van, Burlat, Napoleon, and Cœur pigeon) were collected in Sefrou city in Morocco and were studied. Several assays were performed for this purpose, such as the quantification of phenolic compounds (TPC, TFC, and CTC) and the evaluation of the antioxidant activity using DPPH, ABTS, and FRAP assays. The phenolic profile of each extract was characterized by UHPLC-DAD/MS analysis. The antidiabetic (α-amylase inhibition) and antigout (xanthine oxidase inhibition) activities were also investigated. The results showed high levels of phenolic compounds, with the values of 340 ± 12.06, 244 ± 10.20, 232 ± 5.07, and 19 ± 3.10 mg gallic acid equivalent/g extract for the cultivars Napoleon, Coeur de pigeon, Van, and Burlat, respectively. According to the same order, the flavonoids showed amounts of 34.31 ± 2.08, 23.75 ± 1.02, 24.37 ± 1.20, and 23.31 ± 0.90 mg (rutin equivalent) RE/g extract. These values were correlated with the results of the antioxidant assays, where the Napoleon cultivar proved to be the most potent using the DPPH (IC50 = 2.51 µg/mL) and ABTS (IC50 = 55.38 µg/mL) assays. The phenolic profile of each extract resulted in the identification of twenty-two compounds belonging to five distinct groups. The major phenolic compounds identified were sakuranetin and dihydrowgonin with their glucosides. Antidiabetic activity assays showed that only stem extracts from Burlat and Napoleon cultivars were able to inhibit the α-amylase enzyme with values of 85.57 ± 1.09% and 68.01 ± 3.52%, respectively. All stem extracts proved their ability to inhibit the xanthine oxidase enzyme which is directly linked to the gout disease, with a high value for Van cultivar (40.63 ± 2.37%). These new findings could provide new opportunities for the valorization of cherry stems for the pharmaceutical application of their active phytochemicals.

Natural sources, biological effects, and pharmacological properties of cynaroside.

Cynaroside is a flavonoid, isolated from several species belonging to the Apiaceae, Poaceae, Lamiaceae, Solanaceae, Zingiberaceae, Compositae and other families and it can be extracted from seeds, roots, stems, leaves, barks, flowers, fruits, aerial parts, and the whole plant of these species. This paper discloses the current state of knowledge on the biological/pharmacological effects and mode of action to better understand the numerous health benefits of cynaroside. Several research works revealed that cynaroside could have beneficial effects on various human pathologies. Indeed, this flavonoid exerts antibacterial, antifungal, antileishmanial, antioxidant, hepatoprotective, antidiabetic, anti-inflammatory, and anticancer effects. Additionally, cynaroside exhibits its anticancer effects by blocking MET/AKT/mTOR axis by decreasing the phosphorylation level of AKT, mTOR, and P70S6K. For antibacterial activity, cynaroside reduces biofilm development of Pseudomonas aeruginosa and Staphylococcus aureus. Moreover, the incidence of mutations leading to ciprofloxacin resistance in Salmonella typhimurium was reduced after the treatment with cynaroside. In addition, cynaroside inhibited the production of reactive oxygen species (ROS), which reduced the damage to mitochondrial membrane potential caused by hydrogen peroxide (H2O2). It also enhanced the expression of the anti-apoptotic protein Bcl-2 and lowered that of the pro-apoptotic protein Bax. Cynaroside abrogated the up-regulation of c-Jun N-terminal kinase (JNK) and p53 protein expression triggered by H2O2. All these findings suggest that cynaroside could be used to prevent certain human diseases.

Comparative Investigation of Chemical Constituents of Kernels, Leaves, Husk, and Bark of Juglans regia L., Using HPLC-DAD-ESI-MS/MS Analysis and Evaluation of Their Antioxidant, Antidiabetic, and Anti-Inflammatory Activities.

Leaves, husk, kernels, and bark methanolic extracts of Juglans regia L. were tested for their in vitro antidiabetic, anti-inflammatory, and antioxidant activities. For these purposes, α-amylase and α-glucosidase were used as the main enzymes to evaluate antidiabetic activities. Moreover, lipoxidase and tyrosinase activities were tested to estimate anti-inflammatory properties. Antioxidant properties of Juglans regia L., extracts were determined using three different assays. Leaves extract has an important radical scavenging activity and a-amylase inhibition. Similarly, husk extracts showed high total phenolic content (306.36 ± 4.74 mg gallic acid equivalent/g dry extract) with an important α-amylase inhibition (IC50 = 75.42 ± 0.99 µg/mL). Kernels exhibit significant tyrosinase (IC50 = 51.38 ± 0.81 µg/mL) correlated with antioxidant activities (p < 0.05). Husk and bark extracts also showed strong anti-lipoxidase activities with IC50 equal to 29.48 ± 0.28 and 28.58 ± 0.35 µg/mL, respectively. HPLC-DAD-ESI-MS/MS analysis highlights the phenolic profile of methanolic extracts of Juglans regia L. plant parts. The identified polyphenols were known for their antioxidant, antidiabetic (dicaffeoyl-quinic acid glycoside in kernels), and anti-inflammatory (3,4-dihydroxybenzoic acid in leaves) activities. Further investigations are needed to determine molecular mechanisms involved in these effects as well as to study the properties of the main identified compounds.

Traditional Knowledge, Phytochemistry, and Biological Properties of Vachellia tortilis.

Vachellia tortilis is a medicinal plant of the Fabaceae family, widely distributed in arid and semi-arid regions of North, East and Southern Africa, the Middle East and the Arabian Peninsula. In traditional medicine. It's commonly used to treat certain ailments, including diabetes, asthma, hepatitis and burns. Different scientific search databases were used to obtain data on V. tortilis, notably Google Scholar, Scopus, Wiley Online, Scifinder, Web of Science, ScienceDirect, SpringerLink, and PubMed. The knowledge of V. tortilis was organized based on ethnomedicinal use, phytochemistry, and pharmacological investigations. Phytochemical studies revealed the presence of a variety of phytocompounds, including fatty acids, monosaccharides, flavonoids, chalcones, and alcohols. Essential oils and organic extracts prepared from V. tortilis showed several biological properties, specifically antibacterial, antifungal, antiparasitic, antioxidant, antiproliferative, anti-diabetic, and anti-inflammatory effects. Antimicrobial and antiparasitic activities are due to the disturbance of cellular membranes and ultra-structural changes triggered by V. tortilis phytochemicals. While physiological and molecular processes such as apoptosis induction, preventing cell proliferation, and inflammatory mediators are responsible for the anti-diabetic, anti-cancer, and anti-inflammatory activities. However, further investigations concerning pharmacodynamics and pharmacokinetics should be carried out to validate their clinical applications.

Pharmacological Effects of Grifolin: Focusing on Anticancer Mechanisms.

Grifolin is a volatile compound contained in essential oils of several medicinal plants. Several studies show that this substance has been the subject of numerous pharmacological investigations, which have yielded interesting results. Grifolin demonstrated beneficial effects for health via its multiple pharmacological activities. It has anti-microbial properties against bacteria, fungi, and parasites. In addition, grifolin exhibited remarkable anti-cancer effects on different human cancer cells. The anticancer action of this molecule is related to its ability to act at cellular and molecular levels on different checkpoints controlling the signaling pathways of human cancer cell lines. Grifolin can induce apoptosis, cell cycle arrest, autophagy, and senescence in these cells. Despite its major pharmacological properties, grifolin has only been investigated in vitro and in vivo. Therefore, further investigations concerning pharmacodynamic and pharmacokinetic tests are required for any possible pharmaceutical application of this substance. Moreover, toxicological tests and other investigations involving humans as a study model are required to validate the safety and clinical applications of grifolin.

Phytochemical properties, biological activities and medicinal use of Centaurium erythraea Rafn.

ETHNOPHARMACOLOGICAL RELEVANCE: Centaurium erythraea is an important medicinal plant in many countries, e.g. Morocco, Algeria, Italy, Spain, Portugal, and countries of Balkan Peninsula. It is used in folk medicine to treat various illnesses. It is also used as an antiapoplectic, anticoagulant, anticholagogue, antipneumonic, hematocathartic, and as a hypotensive agent. AIM OF THE REVIEW: In this review, previous reports on the taxonomy, botanical description, geographic distribution, ethnomedicinal applications, phytochemistry, pharmacological properties, and toxicity of Centaurium erythraea were critically summarized. MATERIALS AND METHODS: Scientific search engines including PubMed, ScienceDirect, SpringerLink, Web of Science, Scopus, Wiley Online, SciFinder, and Google Scholar were consulted to collect data on C. erythraea. The data presented in this work summarized the main reports on C. erythraea phytochemical compounds, ethnomedicinal uses, and pharmacological activities. RESULTS: C. erythraea is used in traditional medicine to treat various diseases such as diabetes, fever, rhinitis, stomach ailments, urinary tract infections, dyspeptic complaints, loss of appetite, and hemorrhoids, and as diuretic. The essential oils and extracts of C. erythraea exhibited numerous biological properties such as antibacterial, antioxidant, antifungal, antileishmanial, anticancer, antidiabetic, anti-inflammatory, insecticidal, diuretic, gastroprotective, hepatoprotective, dermatoprotective, neuroprotective, and inhibitory agent for larval development. Phytochemical characterization of C. erythraea revealed the presence of several classes of secondary metabolites such as xanthonoids, terpenoids, flavonoids, phenolic acids, and fatty acids. CONCLUSIONS: Ethnomedicinal studies demonstrated the use of C. erythraea for the treatment of various disorders. Pharmacological reports showed that C. erythraea especially its aerial parts and roots exhibited potent, and beneficial activities. These findings confirmed the link between the traditional medicinal use and the results of the scientific biological experiments. Considering these results, further investigation using diverse in vivo pharmacological assays are strongly recommended to validate the results of its traditional use. Toxicological tests and pharmacokinetic studies are also required to validate the safety and efficacy of C. erythraea and its bioactive contents.

Ethnomedicinal use, phytochemistry, pharmacology, and toxicology of Daphne gnidium: A review.

ETHNOPHARMACOLOGICAL RELEVANCE: Daphne gnidium L., (Lazaz or Metnan) is a perennial plant that grows around the Mediterranean basin, in Southern Europe, North Africa and the Middle East. It is used in different countries for hair care and to treat several diseases including skin cancer, diabetes, nervous breakdowns, sinusitis, poisoning, rheumatic disorders, odontalgia, muscular pain, and gastrointestinal infections. It is also used as anti-inflammatory, insecticide, and anti-parasitic remedy. AIM OF THE REVIEW: In this review, previous studies on D. gnidium including its botanical description, taxonomy, geographical distribution, medicinal use, phytochemistry, and pharmacological properties were critically highlighted and discussed for suggesting the exploration of this specie and its bioactive compounds in medical applications. MATERIALS AND METHODS: Data on D. gnidium were gathered from Scientific search engines including PubMed, ScienceDirect, SpringerLink, Web of Science, Scopus, Wiley Online, SciFinder, and Google Scholar. Reports on D. gnidium written in English published before September 2020 were summarized. RESULTS: In traditional medicine, D. gnidium is used to treat diabetes, gastrointestinal infections, skin cancer, nervous breakdowns, and sinusitis. The extracts and essential oil of D. gnidium exhibited several biological properties such as antibacterial, antifungal, antiviral, antigenotoxic, hemolytic, anti-inflammatory, immunomodulatory, neuroprotective, allelopathic, and insecticidal effects. Phytochemical investigations identified several chemical classes of secondary metabolites in D. gnidium essential oil and extracts including terpenoids, coumarins, flavonoids, fatty acids, and alkanes. CONCLUSIONS: The findings presented in this study showed a link between the traditional medicinal use and scientific biological results about D. gnidium. However, further investigations should be carried out to support medical and cosmetic applications of this species. Indeed, D. gnidium and its main compounds should be confirmed concerning their safety and their bioavailability. Moreover, pharmacodynamic studies should be conducted to support their efficacy in medical applications.

Traditional use, phytochemistry, toxicology, and pharmacology of Origanum majorana L.

ETHNOPHARMACOLOGICAL RELEVANCE: Origanum majorana L., is an aromatic and medicinal plant distributed in different parts of Mediterranean countries. This species is widely used in traditional medicine for the treatment of many diseases such as allergies, hypertension, respiratory infections, diabetes, stomach pain, and intestinal antispasmodic. AIM OF THE REVIEW: This work reports previous studies on O. majorana concerning its taxonomy, botanical description, geographical distribution, traditional use, bioactive compounds, toxicology, and biological effects. MATERIALS AND METHODS: Different scientific data bases such as Web of Science, Scopus, Wiley Online, SciFinder, Google Scholar, PubMed, ScienceDirect, and SpringerLink were consulted to collect data about O. majorana. The presented data emphasis bioactive compounds, traditional uses, toxicological investigations, and biological activities of O. majorana. RESULTS: The findings of this work marked an important correlation between the traditional use of O. majorana as an anti-allergic, antihypertensive, anti-diabetic agent, and its biological effects. Indeed, pharmacological investigations showed that essential oils and extracts from O. majorana exhibit different biological properties, particularly; antibacterial, antifungal, antioxidant, antiparasitic, antidiabetic, anticancer, nephrotoxicity protective, anti-inflammatory, analgesic and anti-pyretic, hepatoprotective, and antimutagenic effects. Toxicological evaluation confirmed the safety and innocuity of this species and supported its medicinal uses. Several bioactive compounds belonging to different chemical family such as terpenoids, flavonoids, and phenolic acids were also identified in O. majorana. CONCLUSIONS: The results suggest that the pharmacological properties of O. majorana confirm its traditional uses. Indeed, O. majorana essential oils showed remarkable antimicrobial, antioxidant, anticancer, anti-inflammatory, antimutagenic, nephroprotective, and hepatoprotective activities. However, further investigations regarding the evaluation of molecular mechanisms of identified compounds against human cancer cell lines, inflammatory process, and microbial infections are needed to validate pharmacodynamic targets. The toxicological investigation of O. Majorana confirmed its safety and therefore encouraged pharmacokinetic evaluation tests to validate its bioavailability.

Phytochemical and biological activities of Pinus halepensis mill., and their ethnomedicinal use.

ETHNOPHARMACOLOGICAL RELEVANCE: Pinus halepensis Mill., is a Mediterranean medicinal plant with numerous traditional applications such as anti-scarring, antiseptic, astringent, antifungal, and anti-tuberculosis. It is used against diarrhea, wounds, rheumatism, cough, gastrointestinal illnesses, hypertension, and hemorrhoids. AIM OF THE REVIEW: We critically summarized previous reports on the botanical, taxonomical, ecological, geographical distribution, phytochemical, and pharmacological results of P. halepensis Mill. MATERIALS AND METHODS: To gather data on P. halepensis Mill., different scientific search engines were consulted such as Google Scholar, Scopus, Wiley Online, Scifinder, Web of Science, ScienceDirect, SpringerLink, PubMed. The collected data on P. halepensis Mill., were organised according to ethnomedicinal use, phytochemistry, and pharmacology. RESULTS: Ethnomedicinal studies indicated that P. halepensis Mill., is used as a protective remedy against respiratory and digestive disorders, arterial hypertension, microbial infections. These medicinal uses vary based on the part used and regions. The extracts and essential oils of P. halepensis Mill., demonstrated several biological effects including antimicrobial, antidiabetic anti-inflammatory, cytotoxic, antiparasitic, and hepatoprotective. Traditional uses and biological effects of P. halepensis Mill., were attributed to the numerous molecules that belong to different chemical classes such as terpenoids, phenolic acids, flavonoids, fatty acids and steroids, aldehydes and ketones. CONCLUSIONS: In vitro and in vivo investigations of P. halepensis Mill., extracts and essential oils showed interesting pharmacological activities supporting the traditional use of this species. Previous reports indicated that P. halepensis Mill., extracts and their constituents exhibited potent antibacterial, antifungal, antioxidant, protective, anticoagulant, anti-hemolytic, and anti-inflammatory effects. Further investigation is needed to reveal the full biological spectra of P. halepensis Mill., extracts and essential oils (using in vivo models) and to validate their industrial applications as a food additive. However, in-depth studies are required to investigate the biological properties and molecular mechanisms of P. halepensis Mill., secondary metabolites in the management of diabetes mellitus and the prevention of the neurodegenerative disorders development such as Alzheimer's and Parkinson's disease. Studies exploring pharmacological effects of P. halepensis Mill., bioactive components such as the antimicrobial, anti-inflammatory, and antiparasitic drugs are required to validate the clinical use of these molecules. The safety of P. halepensis Mill., and its bioactive compounds should be also investigated by carrying out further pharmacokinetic and toxicological experiments.

Origanum compactum Benth., from traditional use to biotechnological applications.

Origanum compactum Benth., is a Moroccan medicinal plant known by its local name as Zaatar. In Morocco, it has various traditional applications such as the use to treat diabetes, metabolic disorders, digestive, and respiratory problems. In this review, we critically highlighted current investigations on the ethnopharmacological studies, the phytochemistry, pharmacological investigations, biotechnological applications, and future perspective of O. compactum. A bibliometric electronic search in worldwide accepted scientific databases such as ScienceDirect, PubMed, SpringerLink, Web of Science, Scopus, Wiley Online, and Google Scholar was carried out to gather on O. compactum. Chemical analysis using GC-MS and/or HPLC allowed the identification of several bioactive compounds such as terpenoids and phenolic acids. Furthermore, O. compactum extracts and essential oils have been tested for various biological activities such as antibacterial, antioxidant, antiparasitic, antifungal, and anticancer effects. Moreover, an alignment between traditional use and biological effects was demonstrated, in particular for the antimicrobial activity. These properties are related to O. compactum bioactive components, especially the volatile compounds such as thymol and carvacrol. The pharmacological mechanisms involve several cellular and molecular targeted actions. Moreover, the biological potential of this species had led some laboratories to apply the biotechnological tools for its regeneration. PRACTICAL APPLICATIONS: Origanum compactum is applied as traditional drug against different illnesses and for food preservation. Scientific investigations proved the application of O. compactum essential oils in food industries as antioxidants and antimicrobials. These volatile compounds could be applied also in pharmaceutical industries, in particular as antibacterial, antifungal, and antileishmanial drugs. Moreover, further investigations concerning toxicological evidences and pharmacokinetic as well as pharmacodynamic mechanistic targets and clinical trials could develop anticancer, antimalaria and anti-inflammatory, and antidiabetic drugs. Finally, the results of the findings of these purposes encourage other research groups to carry out further investigations on the pharmacological properties of O. compactum.

Ethnomedicinal use, phytochemistry, pharmacology, and food benefits of Thymus capitatus.

ETHNOPHARMACOLOGICAL RELEVANCE: Thymus capitatusHoffm. et Link. is an endemic medicinal plant to the Mediterranean region. It is used in folk medicine to treat various diseases including diabetes, flu, cough, flatulence, dermatitis, indigestion, respiratory disorders, asthma, rheumatic, diarrhea, and influenza. It is also used as antiseptic, analgesic, stimulant, and sedative. AIM OF THE REVIEW: In this review, previous reports on T. capitatusconcerningits taxonomy, botanical description, geographical distribution, ethnomedicinal use, phytochemistry, pharmacological properties, and food benefits were critically summarized. MATERIALS AND METHODS: Scientificsearch engines including PubMed, ScienceDirect, SpringerLink, Web of Science, Scopus, Wiley Online, Scifnder, and Google Scholar were consulted to gather data on T. capitatus. The data presented in this work summarize T. capitatus phytochemical compounds, ethnomedicinaluses, pharmacological properties, and food value. RESULTS: In traditional medicine, T. capitatusis used to treat various illnesses including diabetes, dermatitis, and diarrhea. The essential oils and extracts of T. capitatus exhibited several biological properties such as antibacterial, antioxidant, antifungal, antiparasitic, hypoglycemic, anticancer, antiviral, and hepatoprotective effects. T. capitatus possesses high nutritional value and its essential oil showed promising activity in food preservation. Phytochemical characterization of T. capitatus revealed the presence of several classes of secondary metabolites such as terpenoids, flavonoids, and phenolic acids. CONCLUSIONS: Ethnomedicinal surveys indicated the use of T. capitatus for the treatment of various disorders. Pharmacological reports showed that T. capitatus especially its essential oils, exhibited potent antimicrobial, antioxidant, antidiabetic and hepatoprotective effects. These findings confirmed the link between traditional medicinal use and scientific biological results. Moreover, T. capitatus exhibited a potent food preservative effect which justifies its use in traditional medicine as a food additive. In light of these findings, further studies to validate the industrial applications of T. capitatus essential oils as a food additive are required. Further investigations on the in vivo pharmacological properties of T. capitatus are strongly recommended to validate the results of its clinical uses as an antimicrobial, hepatoprotective, and antiviral agent. Toxicological tests and pharmacokinetic investigations are also needed to validate the safety and efficacy ofT. capitatus and its bioactive compounds.