MBCH-MBBS 300L - 2025 - Biochemistry of Bioactive Compounds - Lecture 1 PDF

BIOCHEMISTRY OF BIOACTIVE COMPOUNDS DR. KAYODE, A. A. Abolanle (Associate Professor) (Metabolism, Phytomedicine, Drug Discovery & Development Laboratory) DEPARTMENT OF BIOCHEM...

BIOCHEMISTRY OF BIOACTIVE COMPOUNDS DR. KAYODE, A. A. Abolanle (Associate Professor) (Metabolism, Phytomedicine, Drug Discovery & Development Laboratory) DEPARTMENT OF BIOCHEMISTRY , BABCOCK UNIVERSITY [email protected] 1 1/6/2025 [email protected]  BIOACTIVE COMPOUNDS OF PLANT ORIGIN Bioactive compounds are chemicals or components found in plants and animals that have effect on the body as a whole or specific tissues or cells. Bioactive compounds have actions in the body that may promote good health and wellness. Some have been found in the prevention of cancer, heart disease and other diseases. 3  Bioactive compounds of plant origin  Bioactive compounds of plant origin are those phytochemicals or secondary metabolites possessing desired health/wellness benefit effects in man and animals. 1/6/2025 3 1/6/2025 4 1/6/2025 5 1/6/2025 6 1/6/2025 7  INTRODUCTION (HERBAL MEDICINE)  Dr. Fereydoon Batmanghelidj  ‘The human body being Nature can only be cured by Natural substances and not by inorganic chemical drugs.’  Medicinal properties of the plants are from chemical compounds (Phytochemicals or Secondary metabolites)  that are naturally found in the plants. 1/6/2025 8  INTRODUCTION (Contd)  Herbal medicine can both be preventive and curative.  Herbs are essentially the vegetables that we consume on a daily basis.  If we consume them with understanding with intent to prevent disease(s),  then food would indeed have become our medicine and medicine our food.  Herbal medicine is one of the oldest forms of medicine in the world.  Indeed, it has been very well studied and documented in some countries of the world. 1/6/2025 9   For example, there is Ayurvedic medicine in India and the Chinese Traditional Herbal Medicine in China.  It is also widely used in other European and Asian countries.  Coming nearer Home in Africa, different African countries have for a long time used all sorts of herb for the treatment of different types of diseases. 1/6/2025 10   Nature has blessed humanity with a huge number of different herbs, Laden with tremendous amount of medicinal properties that can be deployed for the treatment and prevention of different ailments.  The rate at which Herbal medicine has been increasing in popularity is to say the least, alarming. Also, it is important to note that this popularity of herbal medicine as it is today, is backed by concrete evidence and testimonies. 1/6/2025 11  Herbal medicine: Definition and its Prospects ▪ The WHO refers to herbal medicine as preparations and/or finished products made of whole plants, ▪ parts of plants, ▪ or other plant materials, including leaves, bark, berries, flowers, and roots, ▪ and/or their extracts as active ingredients intended for human therapeutic use or for other benefits in humans ▪ and sometimes animals ▪ (WHO 2019; Bareetseng, 2022). 1/6/2025 12  Herbal medicine: Definition and its Prospects (Contd.)  It is also known as botanical medicine, phytomedicine or complementary medicine.  It is used globally as a source of well-being due to their antioxidant,  anti-inflammatory,  and pharmacological properties  to treat chronic diseases like HIV/AIDS, dementia, cancer, malaria, tuberculosis  (Reid et al., 2018) 1/6/2025 13  Herbal medicine: Definition and its Prospects (Contd.)  Traditional medicine refers to health practices and approaches which are based on knowledge and beliefs incorporating plants as medicines, spiritual therapies, and physical therapy; either applied singularly or in combination to treat, diagnose, and prevent illnesses or maintain well- being.  In developed countries, adaptations of traditional medicine are termed complementary and alternative medicine (Gunjan et al., 2015).  It is utilized in helping with health-associated problems and enhances general human health.  There has been increasing demands for herbal medicines, both in the developing and developed countries. 1/6/2025 14  Interesting facts on Herbal medicine Trending Primitive 1/6/2025 15  History  1805: Morphine isolated from opium (structure proposed 1935, synthesized. 1952)  Quinine 1825  Digitoxin 1841 (structure 1928)  Salicylic acid, antipyretic 1875  Cocaine isol. 1860, local anesthetic 1884  Benzyl penicillin 1941 1/6/2025 16   Antibiotics 1940 - 1960  Cyclosporin (immunomodulator) isolated from soil fungus  Taxol isolated 1960s, approved drug USA 1992 1/6/2025 17 Natural Products: Folk to Modern Medicines - Humans have long used chemicals in plant and animal extracts for many purposes: medicines, poisons, recreational stimulants - Since the 1800’s, chemists have characterized and synthesized such natural products, uncovering the basis for folk remedies - Identifying the mechanism of action of natural products was the genesis of modern drug discovery - - - The active ingredients in many ancient curatives are still used medicinally today 1/6/2025 18  Natural Products 1: Toxins Rotenone - Natural fish + insect poison Curare (Tubocurarine chloride) - Derived from 2 South American plant genera - Used as arrow-tip poison by native peoples - Blocks transmission of acetylcholine signal to muscles, causing instant paralysis - 1st drug used as muscle relaxant19in surgery 1/6/2025  Natural Products 1: Toxins Hyoscine (= scopolamine) - Derived from plants: deadly nightshade (belladonna), mandrake - In ancient Greece, mandrake was used as an anaesthetic (or poison, in higher doses) - “Witches” smeared extracts on their armpits: avoided toxic oral route, got maximum hallucinogenic effect = felt like they were flying - Blocks certain acetylcholine receptors -1/6/2025 DRM. KAYo ODde.Ar.An- BIuOAsCTeIV:E CpOMrPeOUvNeDSntion of motion2020sickness (patches behind the ea3/2r7/)2023 EA  Natural Products 2: Medicines COCH3 Salicin Acetyl-salicilic acid: aspirin - From Willow tree bark, which was used in folk remedies for treating fevers - Led to synthetic analogue, modern aspirin 1/6/2025 21  Natural Products 2: Medicines Ventolin Ephedrine - From Ephedra plants, basis of ancient Chinese herbal remedy “Ma Huang” (100 AD) for treating respiratory illness - Used clinically since 1926 as bronchodilator to treat asthma - Similar to adrenaline, but also stimulates heart (not good in a drug) - Stimulated research resulting in the non-stimulant drug Ventolin 1/6/2025 22  Natural Products 2: Medicines Quinine - Found exclusively in the bark of the Chinona tree - Used as a malaria treatment since 1600’s - Now synthetic derivatives used, due to widespread resistance 1/6/2025 23  Natural Products 3: Stimulants Caffeine Nicotine - Caffeine-containing plant leaves + seeds have long been brewed to produce stimulant drinks - Such stimulants naturally act as feeding deterrents to repel insect herbivores that consume plants leaves - Tobacco plant can up its production of nicotine 4-fold when under attack by insects; nicotine by-products are used as insecticides 1/6/2025 24  Natural Products 3: Stimulants Cocaine - Coca leaves have been used as a source of cocaine for > 2,000 yrs - Used by Incas in religious ceremonies - Introduced to Europe by conquistadores - Leaves chewed daily by >8 million native peoples in the Andes, to alleviate feelings of hunger and fatigue - Inhibits re-uptake of excitatory neurotransmitter dopamine 1/6/2025 25  Natural Products 4: Halucinogens Morphine (= opium) Heroin (synthetic derivative) - Found in only 2 species of poppy flower (Papaver) - Milky exudate of seed capsules is 25% opiate - Used as a baby calming treatment in ancient Egypt - Binds to brain receptors for short peptides called enkephalins, 1/6/2025 derived from endorphins 26  Natural Products 4: Halucinogens Similar spatial relationships of (*)-marked atoms responsible for similar pharmacological effects Enkephalin Morphine * * * 1/6/2025 * 27  Natural Products 4: Halucinogens Tetrahydrocannabinol Lysergic acid Lysergic acid Diethylamine - Lysergic acid is the parent compound from (LSD, synthetic) which ergot alkaloids are derived, such as LSD - Produced by fungus; often affected stored grain in Middle Ages - Such compounds found in Aztec “magical” preparation ololuiqui DR.- KAS tErAu.Ac.A t- BuIOrAaCTlIVEm YOD 1/6/2025 iPm COM OUi NcDSs of human neu28 rotransmitter 5-hydroxytryptam3/i27n/20e23 28  Pharmacological properti es  TERPENOID PHENOLICS  Antimicrobial, ACIDS Antiviral, Anthelmintic, Antibacterial, Anticancer, Antimalarial  Anticarcinogenic  Antiinflammatory eucalyptol, and antimutagenic menthol, lycopene, carotenoids  anti‐inflammation  anti‐allergic 1/6/2025 29  Phytochemicals and Reported Sources 1/6/2025 30 FLAVONOIDS ALKALOIDS  Antioxidant activity,  Antispasmodic, antimalarial, cardiovascular protective, analgesic, diuretic activities, local  anti‐inflammatory, anesthetic, antihypertensive, hepatoprotective, antiviral, antiasthma, antimalarials, diuretic, bactericidal  Antibacterial  morphine, quinine, cocaine,  silymarin,, quercetin,  nicotine, kaempferol 1/6/2025 31  Pharmacological properties  SAPONINS  Tannins  Antitumor, antiviral, antifungal, anti‐inflammatory,  Antioxidant, immunostimulant, Anti‐carcinogenic, Diuretics, antihypoglycemic,  antihepatotoxic and Hemostatic, Anti‐mutagenic, hepatoprotective, anticoagulant, neuroprotective,  Metal ion‐chelators, antioxidant Antiseptic,  Panaxadiol, diosgenin 1/6/2025 32  Benefits and Importance of Herbal medicine  Herbal medicine is the most popular form of traditional medicine and has an immense contribution to health particularly in resource-limited settings (Okumu et al., 2017)  It is estimated that natural products, as well as their derivatives, contribute up to 50 % of all drugs that find use in clinical settings. 1/6/2025 33  Benefits and Importance of Herbal medicine (cont.)  Cost effectiveness and affordability of Herbal products:  Its is freely available and at a low cost.  Modern medical practice and pharmaceutical drugs are becoming more expensive that the common man can hardly afford them.  Easily accessible and accepted.  Has apparently low toxicity  (Ndubisi and Kanu, 2021). 1/6/2025 34  Benefits and Importance of Herbal medicine (cont.)  Boosting the immune system:  In particular, Herbal products by their chemical components boost the immune system.  They work with every aspect of the system and enhance their function.  For example, they support the antioxidant immune system by supplying enough antioxidants.  (Ndubisi and Kanu, 2021). 1/6/2025 35  Benefits and Importance of Herbal medicine (cont.)  The growing testimonies of increasing effectiveness of herbal medicine, coupled with much lower occurrence of side effects, have made Herbal medicine a ready alternative indeed to Modern medicine.  Herbal products in form of supplements, herbal teas, extract, essential oils and so on, are easy to come by.  They are available in health food shops, springing up all over the place and on the Internet and pharmacy shops. 1/6/2025 36  Importance of herbal medicine (cont.)  According to WHO, at least 80% of Africans rely on medicinal plants for their healthcare.  The herbal medicine market is estimated to be a US$ 250 billion industry that is growing steadily at a rate of 7% (Gakuyaa et al., 2020). 1/6/2025 37  Challenges and limitations of herbal medicine  Poor knowledge/consultation on the uses of herbal medicines in the treatment of chronic diseases.  Non-scientific preparation procedures and incorrect dosage (Ndubisi and Kanu, 2021).  Stigmatization due to poor perceptions and attitudes (Gakuyaa et al., 2020). 1/6/2025 38  Trends and development in herbal medicine  Due to the advancement in technology,  development in society and around the world,  herbal medicine has evolved, undergone and still undergoing some innovation, upgrade and the modern use of it is becoming a trend  (Ndubisi and Kanu, 2021). 1/6/2025 39  Trends and development in herbal medicine (cont.)  This ancient use of traditional medicines resulted to the conceptualization and launching of Research and Development (R&D) programs to investigate the traditional uses of these products,  which consequently generated the requisite scientific data to commercialize traditional medicines within the herbal medicines market  (Bareetseng, 2022). 1/6/2025 40  Trends and development in herbal medicine (cont.)  There has been an upgrade in the tools and equipment used in the preparation and packaging of herbal medicines globally.  The use of clay pots and bowls has been replaced with iron pots and ceramic/stainless steel bowls respectively. 1/6/2025 41  Trends and development in herbal medicine (cont.)  Herbal medicines are now properly packaged in well secured glass bottles, plastic bottles. 1/6/2025 42  TRENDING HERBAL PRODUCTS 1/6/2025 43  Trends and development in herbal medicine (cont.) Herbal medicine modern manufacturing companies have been constructed globally for the following reasons;  correct selection of herbs  proper consultation  hygienic production of medicine  monitored prescription and sales of medicines 1/6/2025 44  Trends and development in herbal medicine (cont.) Examples of this manufacturing company and firms in NIgeria include;  Green Care Phytotherapy Industries Limited.  Greenlife herbal network limited.  Tiens Herbal Product.  Yemkem International Group of Companies.  Ayodele Slimmers and naturopathic Clinic. 1/6/2025 45 1/6/2025 46  Trends and development in herbal medicine (cont.)  Government accreditation of herbal manufacturing industries and their products by the food and drug organisations of each country in which they are situated, for close monitoring of their operations.  Use of modern day equipment and facilities to ensure hygienic production. 1/6/2025 47  Trends and development in herbal medicine (cont.)  Creation of herbal medicine database and information:  this is a trend globally, which allows proper documentation and storage of data used in the preparation,  distribution and possibly, prescription of medicines (Ndubisi and Kanu, 2021).  Data can be accessed locally and sometimes, globally.  An example is China’s Comprehensive Herbal Medicine Information System for Cancer (CHMIS-C). 1/6/2025 48  Trends and development in herbal medicine (cont.)  The inclusion of courses like Ethno-botany and Phytomedicine in tertiary and research institutes has facilitated enhanced study and knowledge of herbal medicine (Ndubisi and Kanu, 2021).  From R&D programs into traditional medicines hundreds of academic papers have been published in peer-reviewed journals and many students have obtained masters’ and doctoral degrees in herbal medicine (Bareetseng, 2022). 1/6/2025 49 1/6/2025 50 1/6/2025 51 1/6/2025 52 1/6/2025 53  Trends in Africa  A traditional Medical Directorate has been established in the ministry of health in Ghana which provides comprehensive, recognizable, and standardized complementary system of health, based on excellence in traditional and alternative medicine.  Centers for integrating scientific research into plant medicines and incorporating traditional medicine into university curricular have been established (Ezekwesili-Ofili et al., 2019). 1/6/2025 54  Trends in Africa Efforts are being made in Tanzania to scale up traditional medical practice by creating awareness of the importance of traditional medicine and medicinal plants in health care and training of traditional health practitioners on good practice, conservation, and sustainable harvesting (Ezekwesili-Ofili et al., 2019). 1/6/2025 55  Trends in Africa  Traditional Medicine Practitioners in Kenya far outnumber conventional or allopathic providers.  In majority of their cases, they combine both modern and herbal medicines, especially if they are afflicted by chronic ailments such as HIV/AIDS, hypertension, cancer, and diabetes (Ezekwesili-Ofili et al., 2019). 1/6/2025 56  Trends in Africa  The interest and involvement of educated and scientific-minded people in herbal medicine practice have to a great extent demystified and increased the acceptability of these medicines by a greater percentage of would-be skeptical populace.  However, the greatest problem facing herbal medicine in Nigeria still remains lack of adequate standardization and safety regulations. 1/6/2025 57  Future perspective in Herbal Medicine  All countries in the African region must seek to recognize traditional medical practice by putting out regulations and policies that will be fully implemented to ensure that the Herbal Medicines in African Traditional Medicine THPs are qualified and accredited but at the same time respecting their traditions and customs. They must also be issued with authentic licenses to be renewed frequently. 1/6/2025 58  Future perspective in Herbal Medicine  Raising the standards of African traditional herbal medicine to international standards through inter country collaboration. These if achieved would put African herbal medicine in an admirable position in the World health care system (Ezekwesili-Ofili et al., 2019). 1/6/2025 59  Future perspective in Herbal Medicine  Incorporation of systems that will provide an enabling environment to promote capacity building, research, and development, as well as production of traditional herbal medicines of high standards.  Harnessing the importance of traditional herbal medicine and integrating the conventional medicine to combat priority diseases such as malaria, HIV/AIDS, diabetes, sickle cell anemia, hypertension and tuberculosis (Ezekwesili-Ofili et al., 2019). 1/6/2025 60  References  WHO global report on traditional and complementary medicine. 2019. ISBN 978- 92-4-151543-6. https://tinyurl.com/4z3fx53  Reid A.M, Oosthuizen C.B, Fibrich B.D, Twilley D, Lambrechts I.A, Nuno de Canha M, Rademan S, Lall N. Traditional medicine: The Ancient Roots of Modern Practice In Traditional Medicine. South Africa: University of Pretoria. 2018; p.1-11. doi: 10.1016/ B978- 0-12-812475-8.00001-9 1/6/2025 61  References  Okumu M.O, Ochola F.O, Onyango A.O, Mbaria J.M, Gakuya D.W, Kanja L.W, Kiama S.G, Onyango M.A. The Legislative and Regulatory Framework Governing Herbal Medicine Use and Practice in Kenya: a Review. Pan African Medical Journal. 2017; doi:10.11604/pamj.2017.28.232.12585.  Bareetseng S. The Worldwide Herbal Market: Trends and Opportunities. J Biomed Res Environ Sci. 2022 May 21; 3(5): 575-584. doi: 10.37871/jbres1482, Article ID: JBRES1482, Available at: https://www.jelsciences.com/articles/jbres1482.pdf.] 1/6/2025 62  References  Gakuyaa Daniel Waweru , Okumu Mitchel Otieno, Kiamac Stephen Gitahi, Mbaria James Mucunu, Gathumbi Peter Karuri, Mathiuc Peter Mbaabu, Nguta Joseph Mwanzia. Traditional medicine in Kenya: Past and current status, challenges, and the way forward. Scientific African 8. 2020; https://doi.org/10.1016/j.sciaf.2020.e00360.  Ndubisi Ejikeuwa J.O, Kanu Ikechukwu Anthony. Innovative trends in African traditional medicine. 1/6/2025 Ekpoma Article Review. 2021;63 Volume (8).  References  Shewamene Z, Dune T, Smith C.A. The use of traditional medicine in maternity care among African women in Africa and the diaspora: a systematic review. BMC Complement Altern Med. 2017 Aug 2; 17(1):382. doi: 10.1186/s12906-017-1886-x. PMID: 28768534; PMCID: PMC5541739.  Ezekwesili-Ofili Josephine Ozioma and Okaka Antoinette Nwamaka Chinwe. Herbal Medicines in African Traditional Medicine. 2019; http://dx.doi.org/10.5772/intechopen.80348. 1/6/2025 64