Pharmacognosy-II Lecture 4-Marines PDF 2024-2025

Pharmacognosy-II Fall Semestre 2024-2025 Shaza Hussiny Aly, PhD Lecturer of Pharmacognosy Faculty of Pharmacy Badr University in Cairo 2024 Lecture 4 21-10-2024  Herbs ✓ Lectures outline: I. Introduction to herbs. II. Herbs containing Volatile...

Pharmacognosy-II Fall Semestre 2024-2025 Shaza Hussiny Aly, PhD Lecturer of Pharmacognosy Faculty of Pharmacy Badr University in Cairo 2024 Lecture 4 21-10-2024  Herbs ✓ Lectures outline: I. Introduction to herbs. II. Herbs containing Volatile oil: Mentha & Thyme III. Herbs containing Alkaloids: Hyoscyamus, Vinca, Lobelia, Ephedra IV. Herbs containing Resin: Cannabis V. Miscellaneous herbs VI. Thallophytes (Ergot) VII. Marines  VI. Marine Natural Products ✓ In the 20th century scientists separated the pharmacologically active compounds from natural sources and developed new medicines synthetically or semi-synthetically to be more effective and less harmful e.g. morphine and morphine like analogues. ✓ By the end of the 20th century, disease resistance to antibiotics, to anti-virals, to anti- inflammatory and to anticancer drugs continues to grow at an alarming rate. So Natural products chemists were increasingly turning to new sources in the search for biologically and pharmacologically active compounds. Introduction ✓ As oceans represent more than 70% of the earth surface, they can be considered as a wealth source of bioactive natural products. ✓ Before early 1970th, there was no SCUBA Diving, no submarines, so marine natural products science is a modern science started in the late 1970th. ✓ Till now, 10 marine biopharmaceutical compounds are approved and marketed to treat different human diseases, 22 marine biopharmaceutical compounds are under the late clinical trials stages. Introduction Samples of marine organisms near shores are collected by hand or by snorkeling. Deeper water samples {up to 100 feet} can be done by SCUBA diving (Self-Contained Underwater Breathing Apparatus). Divers can dive only up to 100 feet as if they are going deeper than that, they will suffer from Azotemia "a medical condition characterized by abnormally high levels of nitrogen gas in the blood". He will suffer from narcotism, will be staggered and can die. For samples from depths that cannot be achieved by SCUBA diving, submersibles may be used. Classification of Marine Creatures ✓ Marine creatures are keeping their pharmacologically active 2ry metabolites inside their bodies not secreting them continuously to water. ✓ These metabolic compounds are water insoluble compounds. ✓ In extraction step, the sample may be homogenized then extracted with the suitable organic solvent to dissolve the pharmacologically active organic compounds.  The most famous preliminary biological screening for biological activity of extracts or isolated pure compounds is the screening for toxicity to Brine shrimps. If the extract or fraction is toxic to Brine shrimp, so it must contain pharmacologically active compounds that are toxic to Brine shrimps in large doses After Brine Shrimp Toxicity Screening, there are many other assays like cytotoxicity, anti- microbial, anti-viral, anti- inflammatory and anti-parasitic activities.  Algae Sponges Corals Polyhalogenated monoterpens [from red algae] Cytotoxic Nucleosides [Adenine and cytosine derivatives from sponges] For Cancer. Polyethers or Polyketides [Halichondin B from sponges] For Cancer. Terpenoids [from corals, Sponges, green algae and brown algae] Anti-inflammatory. Sterols [from Soft Corals] Marine Algae = Seaweed Multicellular, marine algae which are large enough to be seen by the eye unaided. Some can grow to up to 60 metres in length. Seaweeds include members of the red, brown and green algae. They are members of the kingdom Protista meaning they are not Plants. Not Like Plants Like plants Use the pigment chlorophyll for No vascular system (internal transport photosynthesis but also contain other system) pigments which may be coloured red, No roots, stems, leaves and flowers. blue, brown or gold. They are divided into three groups: 1. Brown Algae (Phaeophyta) 2. Green Algae (Chlorophyta) 3. Red Algae (Rhodophyta) Sponges Corals ✓ 10 Approved products ✓ 22 Compounds advanced clinical trials Nucleosides (Adenine and cytosine Polyhalogenated monoterpens derivatives) Sponge Red Algae Antiviral and anticancer Cytotoxic Polyethers or Polyketides Terpenoids Sponges Corals, Sponges, Green Algae and Brown Algae Anticancer Anti-inflammatory Polyhalogenated monoterpens ✓ Source: Red Algae ✓ Use: Cytotoxic Terpenoids ✓ Source: Corals, Sponges, Green Algae and Brown Algae ✓ Use: Anti-inflammatory Sterols ✓ Source: Soft Corals and Green algae  Marine Toxins Tetrodotoxin (TTX) Tetrodotoxin(TTX) isolated from Pufferfish,octopuses and seastars. The true producer of tetrodotoxin is a gram-ve organism Pseudoaltermonas, a micro-organism living on all of these creatures. Tetrodotoxin acts in large dose as a very strong Sodium Channel Blocker compound, leading to respiratory paralysis and death. Now it is manufactured by Wex Pharmaceuticals and approved by Health Canada as a strong pain killer drug in cancer{Halneuron }in very low concentration. It is 3000 times more active painkiller than morphine.  Marine Toxins Jelly fish toxins Polypeptides{main one is a 47 amino acids polypeptide}act by increasing K+ influx in nerves and cells leading to severe irritation and edema in large dose. In low concentration Potassium is very important in regulating heart beats in arrhythmia. So Jelly fish toxins, may be used in the future as lead drugs {pharmacophore} for treatment of cardiac arrhythmia by drug targeting.  Approved {Marketed} Marine Drugs Cytosine derivative 1- Cytarbrine - Cytosar-U®- Ara C ✓ Nature A Nucleoside isolated from a Caribbean marine sponge Cryptotethya crypta ✓ Uses 1. Anticancer 2. Antimetabolite inhibits DNA polymerase 3. Used in acute myelocytic leukemia [lymphoma]. 2-Vidarabine - Vira-A® - Zovirax - Ara A Adenine derivative ✓ Nature A Nucleoside isolated from a Streptomyces antibioticus living on Caribbean marine sponge Cryptotethya crypta ✓ Uses 1. Antiviral 2. Inhibits DNA polymerase 3. Used in herpes simplex virus and Varicella zoster [Chickenpox virus]. 3- Eribulin – Halaven ® ✓ Nature A Polyketide macrocyclic polyether compound inspired from Halichondrin B from Halichondra sponge ✓ Uses 1. Anti-cancer – Breast cancer 2. Microtubule destabilization (Anti-mitotic) Pseudopterosine A ✓ Nature Diterpene phenolic glycoside isolated from the soft coral Pseudoterogorgia elisabethae ✓ Uses 1. Inhibits COX I and COX II 2. Anti-inflammatory for skin care.