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Man has probably used since his existence plants and plant-derived compounds for his health care and well-being. This has led to the development of life-saving drugs for treating a multitude of conditions including infectious, cardiovascular, malignant, and diabetic disease. More recently, the amazing biodiversity represented by the world's oceans...
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... pseudopterosins are tricyclic diterpenepentose glycosides isolated from the sea whip Pseudopterogorgia elisabethae Bayer 1961 (Gorgoniidae), a Caribbean soft coral species (Figure 2) [52]. These compounds possess notable anti-inflammatory and analgesic properties that exceed the potencies of existing cyclooxygenase- inhibiting non-steroidal anti-inflammatory drugs [53][54][55]. ...
Citations
... Ikarugamycin (40,Abb. 11) [30] Discodermid Der Naturstoff Discodermid (41) konnte 1991 von Gunasekera et al. aus dem karibischen Tiefseeschwamm Discodermia dissoluta (Abb. ...
... Abbildung 10: Struktur des Naturstoffs Discodermid (41) Abbildung 9: Tiefseeschwamm Discodermia dissoluta [40] ...
2,2-Dimethyl-5-(triphenylphosphoranyliden)acetyl-1,3-dioxan-4,6-dion ist ein neues aktiviertes β-Ketoacyl Äquivalent, welches in quantitativen Ausbeuten durch die Reaktion von Meldrumsäure und dem stabilen Ylid Ph3PCCO synthetisiert werden kann. Die Reaktion mit α-Aminoester erzeugt entsprechende N-(β-ketoacyl)aminoesterylid, welche mit verschiedenen Aldehyden und KOtBu simultan eine Wittig-Reaktion und Lacey-Dieckmann-Zyklisierung durchlaufen, um die korrespondierende 3-Enoyltetramsäure zu erhalten. Eine flexible Syntheseroute für das 16-gliedrige makrozyklische Grundgerüst, das in verschiedenen Polyzyklischen Tetramsäure Makrolactamen (PTMs) vorkommt wurde entwickelt, welche sich durch die eingesetzten Schutzgruppen und der Reihenfolge der Reaktionsschritte von den Arbeiten von Boeckman Jr. an der Totalsynthese von Ikarugamycin unterscheidet. Außerdem wurde ein Ansatz für die kurze Synthese verschiedener Stereoisomere des 5/5/6-Tricarbozyklischen Motivs ausgehend vom Weiss´schen Diketon entwickelt.
... A Sea whip known as Pseudopterogorgia elisabethae contains a bioactive compound called Pseudopterosins, that has proved to be a good analgesic and antiinflammatory agent (Mans, 2016). ...
The modern drugs commercially available nowadays are widely isolated from natural reservoirs. Penicillin was isolated from a mold and Aspirin was isolated from a willow tree. The recent advanced scientific research has further extended the explorations for medicinal drugs in the marine reservoirs. Some of the drugs based on marine organisms have proved to be quite effective in treating diseases like cancer and Human Immunodeficiency Virus. The different marine organisms like sponges, molluscs, echinoderms, tunicates and bryozoans are being actively used or trialled for the preparation of useful pharmaceutical drugs. The scientists, researchers and pharmaceutical corporations of the world compete to discover new drugs from global marine reservoirs. The marine organisms are freely available in the marine ecosystems and lack of global legislations provide free hands to the biopirates to exploit the marine reservoirs and isolate different organisms from it. The enormous explorations in the marine reservoirs by the biopirates are causing damage to its ecosystems and its lifeforms. In this investigation, it was concluded that though scientific explorations should be allowed in the marine reservoirs for producing lifesaving drugs but overexploitation of marine reservoirs should be prohibited. It is suggested through this investigation that proper tracking of marine reservoirs is the present requirement to face the challenges being laid down by the biopirates .
... As shown in the results of the potential test in figure 2, there were two bacterial isolates, Bvc1, and Bvc3, that showed more potent inhibitory ability than the positive control. According to [19], different degrees of activity shown by each bacterial isolate may be caused by differences in secondary metabolites produced by each isolate. The positive control used was penicillin 1 g diluted with 9 ml ddH2O. ...
... Gram-positive bacteria have a cell wall structure with a thick peptidoglycan content, thus unaffected during alcohol decolorization. Gram-positive bacteria will retain the purple color of crystal violet that when observed under a microscope it will show a purple color [19]. So it can be concluded that both Bvc1 and Bvc3 isolates are classified as specific in inhibiting Gram-positive bacteria, this shows the potential for antibiotics that have specifications in inhibiting MRSA pathogenic target bacteria as shown by the two isolates to have high activity compared to penicillin in inhibiting the growth of MRSA bacteria. ...
Abstract. Currently, infectious diseases are still a serious problem in Indonesia, especially with the wide spread resistance of microbes to antibiotics. Staphylococcus aureus as one of the common pathogens causing infection has experienced resistance to various classes of beta-lactam antibiotics known as Methicillin-resistant Staphylococcus aureus (MRSA). Therefore antibiotic alternatives sourced from nature are needed to treat the MRSA pathogenic infection. This study aims to explore the potential of bacteria in symbiosis with Pokea Shells (Batissa violacea celebensis Martens 1897) from Konawe Regency, Southeast Sulawesi Province to be used as the newest anti-MRSA. In this research, Pokea Shell's symbiont bacteria were isolated from Konawe Regency to obtain pure isolates. Pure isolates that have been produced from secondary metabolites to be tested for their potential in inhibiting the growth of pathogenic bacteria MRSA. The inhibition test was done qualitatively by using a paper disk. Based on the results five bacterial isolates were obtained with different abilities to inhibit MRSA bacteria. Based on the qualitative test obtained that the Bvc1 and Bvc3 bacterial isolates had the potency to be used as anti-MRSA agents. These isolates have an inhibition zone of 25 mm and 22 mm with a sensitive category according to CLSI standards (Sensitive =17 mm). Determination of the gram of these 2 isolates found as gram- positive bacteria in the form of bacilli so it can be concluded that the 2 isolates can be used as anti-MRSA agents.
Keywords: Anti-MRSA, Batissa violacea celebensis Martens 1897, Screening, Symbiont bacteria
... Similarly to those from many invertebrates [333][334][335] and amphibians [336], the exploration of bioactive compounds from reptiles may yield structurally novel and mechanistically unique lead compounds for developing breakthrough medicines. This paper has lifted a corner of the veil, reviewing the opportunities for the development of anticoagulants and antiplatelet drugs as well as wound healing-promoting, antileishmanial, antiviral, immunomodulating antimicrobial, and anticancer compounds from various species, genera, or families of reptiles. ...
Introduction New drug discovery and development programs have historically relied on the identification of novel lead compounds from plant origin. This is understandable when considering that plants have been the main, if not the only sources of therapeutics for managing human diseases for millennia [1]. Only in 1806, a pharmacologically active ingredient (morphine) from a plant (the opium poppy Papaver somniferum (Papaveraceae)) was for the first time isolated from a plant [2]. Currently, morphine is used for, among others, the palliation of severe chronic pain in, for instance, terminal cancer patients [2], and serves as a precursor for a large number of opioid medications such as the antitussive codeine and the antidiarreal agent loperamide [2]. The identification of morphine from P. somniferum was soon followed by many others such as, among others, the central nervous system stimulant caffeine from the beans of the coffee plant Coffea arabica (Rubiaceae) in 1819 [3], the antimalarial quinine from the bark of the cinchona tree Cinchona officinalis (Rubiaceae) in 1820 [4], and the analgesic salicin from the bark of the white willow Salix alba (Salicaceae) in 1828 [5]. Since then, many more breakthrough drugs have been developed from plants, including the antineoplastic agents vincristine and paclitaxel from the periwinkle plant Catharanthus roseus (Apocynaceae) [6] and the Pacific yew Taxus brevifolia (Taxaceae) [7], respectively; the phytoestrogen diosgenin from yam species in the genus Dioscorea (Dioscoreaceae) that serves as precursor for, among others, oral contraceptives and cortisone [8]; and the oral antihyperglycemic biguanide metformin from the French lilac Galega officinalis (Fabaceae) [9]. Other important sources of novel drugs were microorganisms. The fungus Penicillium rubens (Trichocomaceae) and the actinomycete bacterial species Saccharopolyspora erythraea (Pseudonocardiaceae) gave the antibacterial agents penicillin [10] and erythromycin Abstract New drug discovery and development efforts have traditionally relied on ethnopharmacological information and have focused on plants with medicinal properties. In the search for structurally novel and mechanistically unique lead compounds, these progams are increasingly turning to the bioactive molecules provided by the animal biodiversity. This not only involves bioactive constituents from marine and terrestrial invertebrates such as insects and arthropods, but also those from amphibians and other 'higher' vertebrates such as reptiles. The venoms of lizards and snakes are complex mixtures of dozens of pharmacalogically active compounds. So far, these substances have brought us important drugs such as the angiotensin-converting enzyme inhibitors captopril and its derivates for treating hypertension and some types of congestive heart failure, and the glucagon-like peptide-1 receptor agonist exenatide for treating type 2 diabetes mellitus. These drugs have been developed from the venom of the Brazilian pit viper Bothrops jararaca (Viperidae) and that of the Gila monster Heloderma suspectum (Helodermatidae), respectively. Subsequently, dozens of potentially therapeutically applicable compounds from lizards' and snakes' venom have been identified, several of which are now under clinical evaluation. Additionally, components of the immune system from these animals, along with those from turtles and crocodilians, have been found to elicit encouraging activity against various diseases. Like the venoms of lizards and snakes, the immune system of the animals has been refined during millions of years of evolution in order to increase their evolutionary success. This paper addresses some of the bioactive compounds from reptiles, and elaborates on the therapeutic potential of some of them as anticoagulants and antiplatelet drugs, as well as wound healing-promoting, antileishmanial, antiviral, immunomodulating, antimicrobial, and anticancer compounds.
... Topsentia pachastrelloides, a sponge, consists of two valuable bisindole alkaloids, namely cis-3,4dihydrohamacanthin B and bromodeoxytopsen tin, which have vital antibacterial activity against Staphylococcus aureus (Mans, 2016). Bisindole alkaloids have been reported to act as pyruvate kinase (PK) inhibitor. ...
The marine environment has always been an exceptional storehouse of potential bioactive natural metabolites due to its diversified environment in different oceanic zones. Marine pharmacology is a branch of pharmaceutical sciences which deals with active pharmacological metabolites present in marine species. Marine‐derived sulfated polysaccharides, peptides are exploited for their anticoagulant property and explored as a potential drug forvascular and embolic disorders. Their mechanism of action is similar to mammalian‐derived anticoagulants like heparin, with minimal side effects and cytotoxicity, and some of the compounds with their mechanisms are discussed. Naturally derived metabolites account for around 50% of cancer drugs and marine‐derived compounds are generally are less signified for their therapeutic importance. Nonetheless, these compounds represent an invaluable expediency of bioactive metabolites and can be targeted as anticancer drugs. Antithrombotic drugs work mainly by potentiation of plasma cofactors, and SERPIN inhibitors.
... Hasil penelitian menunjukkan bahwa organisme laut memiliki potensi yang sangat besar, dalam menghasilkan senyawa-senyawa aktif yang dapat digunakan sebagai bahan baku obatobatan. Beberapa organisme laut yang diketahui dapat menghasilkan senyawa aktif antara lain ialah spons, moluska, bryozoa, tunikata dan lain-lain (Radjasa et al., 2011;Mans, 2016). Invertebrata laut menyediakan nutrient yang baik bagi berbagai mikroba (Erwin et al,. ...
Tunicate is an invertebrate that lives in a coral reef ecosystem and produces many compounds such as, antibacterial, antitumor and anticancer. This study aimed to determine the antimicrobial activity of extracts and fraction of tunicate (Polycarpa aurata) collected in the Lembeh Strait, Bitung against Escherichia coli, Staphylococcus aureus and Candida albicans. Tunicate (Polycarpa aurata) was extracted by maceration method using 96% ethanol solvent, fractination using liquid-liquid partition method with n-hexane, chloroform and methanol solvent, and antimicrobial testing using Kirby Bauer’s disk diffusion method. The results showed that ethanol extract of tunicate (Polycarpa aurata) had antimicrobial activity againts Escherichia coli with an inhibition of 15.12 mm, and againts Candida albicans with an inhibition of 15 mm. While the methanol fraction showed antimicrobial with a strong category and inhibition of 16.17 mm againts Staphylococcus aureus. Keyword: Tunicate (Polycarpa aurata), Extraction, Fractination, Antimicrobials ABSTRAKTunikata merupakan invertebrata di ekosistem terumbu karang yang banyak menghasilkan senyawa seperti, antibakteri, antitumor dan antikanker. Penelitian ini bertujuan untuk mengetahui aktivitas antimikroba ekstrak dan fraksi tunikata (Polycarpa aurata) yang dikoleksi di Selat lembeh, Bitung terhadap Escherichia coli, Staphylococcus aureus dan Candida albicans. Tunikata (Polycarpa aurata) diekstraksi menggunakan metode maserasi dengan pelarut etanol 96%, fraksinasi menggunakan metode partisi dengan pelarut n-heksan, kloroform dan metanol, dan pengujian antimikroba menggunakan metode difusi agar Kirby Bauer. Hasil penelitian menunjukkan bahwa ekstrak etanol tunikata (Polycarpa aurata) memiliki aktivitas antimikroba kategori kuat pada fraksi metanol dengan daya hambat sebesar 16, 17 mm terhadap Escherichia coli, pada ekstrak etanol dengan daya hambat sebesar 15, 12 mm terhadap Staphylococcus aureus sedangkan pada Candida albicans aktivitas yang sangat baik terjadi pada ektraksi etanol sebesar 15 mm. Kata Kunci: Tunikata (Polycarpa aurata), Ekstraksi dan Fraksinasi, Antimikroba
... Even though it is widely accepted that plant and fungal extracts are the main natural sources of different bioactive compounds, today many animal species have become a focal point in the search for new biomolecules with promising properties [30,31]. In that regard, many invertebrates, especially arthropods, have been considered a promising source of various compounds capable of reducing the harmful effect of reactive oxygen species (ROS), either as food or as therapeutic products [32,33]. ...
Members of the millipede order Julida rely on dominantly quinonic defensive secretions with several minor, non-quinonic components. The free radical-scavenging activities of ethanol, methanol, hexane, and dichloromethane extracts of defensive secretions emitted by Pachyiulus hungaricus (Karsch, 1881) and Megaphyllum unilineatum (C. L. Koch, 1838) were investigated using the ABTS, DPPH, and total reducing power (TRP) tests. The obtained extracts were also tested for inhibition of acetylcholinesterase and tyrosinase activity. Finally, the antifungal potential of both julid extracts was evaluated against seven Fusarium species. Secretions of both species showed activity against free radicals, acetyl-cholinesterase, tyrosinase, and all of the selected fungal species. The secretions of P. hun-garicus exhibited a more potent antioxidative effect than did those of M. unilineatum, while there were no significant differences of antiacetylcholinesterase activity between the tested extracts. Only the hexane extract of M. unilineatum showed an effect on tyrosinase activity stronger than that of P. hungaricus. Fusarium sporotrichioides, F. graminearum, and F. ver-ticillioides were the fungi most resistant to secretions of both julids. The Fusarium species most susceptible to the secretion of P. hungaricus was F. avenaceum, while the concentrations of M. unilienatum extracts needed to inhibit and completely suppress fungal growth were lowest in the case of their action on F. lateritium. Our data support previous findings that julid defensive secretions possess an antimicrobial potential and reveal their anti-oxidative and antineurodegenrative properties. Bearing in mind the chemical complexity of the tested defensive secretions, we presume that they can also exhibit other biological activities.
... Also, it targets the proteins involved in the Erb3 and PI3 kinase-Akt/ PKB signaling pathways (Giddings and Newman 2013). It may also interfere with the gene expression of the proteins involved in DNA replication and cell proliferation (Mans 2016). Kahalalide F demonstrated to have potent antitumor activity in vitro and in vivo in various solid tumor models of breast cancer, colon cancer, NSCLC, and, exclusively, prostate cancer. ...
Cancer continues to be a global challenge to both clinicians and researchers with an increasing mortality rate. Despite the enormous progress made in the anticancer drug discovery, there is a constant demand for novel therapeutic agents, because of the development of resistance to the existing chemotherapeutic drugs and their adverse side effects. The anticancer drugs derived from the natural sources have shown to be effective and safe in the treatment of cancers. Secondary metabolite compounds from plants such as alkaloids, flavonoids, and carotenoids are known for their cancer prevention and antitumor properties. Peptides produced from marine organisms and anthracyclines synthesized by microbes as secondary metabolites are also known for their anticancer properties. Some of these natural compounds are widely used in cancer therapy, and some are under clinical or preclinical trials. Some of the potential anticancer agents from plants (paclitaxel, vincristine, vinblastine, irinotecan, etoposide, topotecan, and camptothecin), marines (dolastatin 10, cytarabine, and aplidine), and microorganisms (bleomycin, doxorubicin, and dactinomycin) have been used in cancer therapy. Cancers are characterized by the alterations in the cell signaling pathways. Most of the current anticancer therapies involve the modulation of altered signaling targets in cancers. The advantage of using natural compounds with antitumor properties for cancer therapy is that the compounds have well-defined signaling targets with a minimal toxicity. Natural anticancer drugs have been categorized based on their target-specific signaling pathways, which include DNA-damaging drugs, methyltransferase inhibitors, mitotic disrupters, and histone deacetylase inhibitors. Thus, the present chapter highlights the natural anticancer compounds and their derivatives which are under clinical trials and their mechanism of action in cancer therapy.
... A myriad of breakthrough therapeutics has been developed by following up naturally-derived leads with medicinal properties, not only from plants but also from microorganisms and marine species [3,4]. A few examples are the cardiac glycoside digoxin from the foxglove Digitalis lantana L. (Scrophulariaceae) for treating certain heart conditions [5]; the muscle relaxant D-tubocurarine derived from the Amazon plants Strychnos toxifera L. (Loganiaceae) and Chondrodendron tomentosum L. (Menispermaceae) [6]; the hypoglycemic agent metformin synthesized on the basis of the chemical structure of galegine in the French lilac Galega officinalis L. (Fabaceae) [7]; the antibiotic penicillin from the fungus Penicillium chrysogenum Thom, 1910 (Trichocomaceae) [8]; the powerful pain killer ziconotide molded on the basis of conotoxin in the venom of the cone snails Conus geographicus Linnaeus, 1758, and Conus magus Linnaeus, 1758 (Conidae) [9]; and the novel antineoplastic agent trabectedin (Yondelis ® ) originally isolated from the Caribbean sea squirt Ecteinascidia turbinata Herdman, 1880 (Perophoridae) [10]. ...
