Konstantinos Anastassakis's scientific contributions

Publications (79)

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Melatonin was first isolated from bovine pineal gland extracts in 1958 by the distinguished researcher and professor of Dermatology Aaron B. Lerner, who also described the chemical structure as N-acetyl-5-methoxytrypamine [1, 2]. The functions of melatonin were not initially evident, but it was soon discovered that it is a ubiquitous molecule, wide...
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Ginkgo Biloba is a dioecious tree that can live for more than 800 years and is the only living species in the division Ginkgophyta, all others being extinct. It is regarded as a “living fossil“because of the species’ uninterrupted existence for 270 million years and is the oldest tree in the world, with no living relative in existence. Mature trees...
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Progesterone is a natural hormone synthesized in the human body and is found in the serum of both sexes. In many species, including humans, progesterone is involved in the menstrual cycle, pregnancy and embryogenesis [1]. It is also an essential metabolic intermediate in the production of other endogenous steroids, including sex hormones and minera...
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Genetic factors, androgens, and follicular micro-inflammation play key roles in causing “androgenic” hair loss (see Chaps. 11 and 14, Vol. 1) In order to affect the course and progression of AGA through diet or lifestyle, the only parameter in AGA that could be “manipulated” is the hormonal one, which includes several sub-components:Only the produc...
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Saw Palmetto or Serenoa repens (also known by its botanical name, Sabal serrulatum) is a plant of the Arecaceae’s family, and it is an American bushy dwarf palm tree and cabbage palm. It is endemic to the subtropical Southeastern United States, most commonly along the south Atlantic and Gulf Coastal plains and sandhills, and in the West Indies isla...
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Caffeine is a bitter, white crystalline purine, a methylxanthine alkaloid, chemically related to the adenine and guanine bases of deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). Caffeine is found in different concentrations in seeds, leaves, and nuts of more than 60 different plant species. It acts as a naturally occurring pesticide since i...
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Capsicum species, also known as chili peppers, belong to the flowering Solanaceae family, originally native to the Americas, where they have been cultivated for thousands of years. Following the Colombian exchange -the widespread transfer of plants, animals, culture, human populations, technology, and ideas between the Americas and the Old World du...
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Pygeum Africanum (PygA) extract is a popular phytotherapy agent that has been used in Europe since the early 1970s to treat mild to moderate lower urinary tract symptoms (LUTS) attributable to Benign Prostatic Hyperplasia (BPH), but with unconfirmed efficacy.
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Selenium is a non-metal essential trace element with the symbol Se and atomic number 34. It was first described in 1818 by the Swedish chemist Jöns Jacob Berzelius (1779–1848), who began his career as a physician. He named this element after the Greek moon goddess Selene (Greek “σελήνη” (Selene) meaning Moon). Selenium seldom occurs in its elementa...
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Proanthocyanidins, also known as condensed tannins, are a group of polyphenolic secondary metabolites synthesized in plants as oligomers (or polymers) of flavan-3-ol units (also known as epicatechin) via the flavonoid pathway [1, 2]. Proanthocyanidins are widely distributed in fruits, legume seeds, cereal grains and can be found in the respective b...
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Vit Α and its derivatives (retinoids) have been known since the beginning of the twentieth century to be essential for developing and maintaining various tissues, including the skin and hair [1, 2]. Retinoic acid, also known as Tretinoin, or all-trans-retinoic acid (ATRA) in its pharmaceutical form, is the carboxylic acid, an acidic, active metabol...
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Azelaic acid (AzA) is an organic compound found in abundance in nature and physiologically in low systemic levels in humans. Many food sources, such as wheat, barley, and rye, regularly expose humans to AzA through dietary intake. AzA is a saturated dicarboxylic acid, much weaker than household vinegar. Available data show that AzA appears to be de...
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Vit C or L-ascorbic acid is a weak sugar acid that can occur in reduced or oxidized form structurally related to glucose. Vit C is a collective term describing several vitamers with Vit C activity in animals, including ascorbic acid, ascorbate, their salts, and some oxidized forms of the molecule, such as dehydroascorbic acid (DHA). The name “Vit C...
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Silicon is a non-metallic element with an atomic weight of 28 and is the second most abundant chemical element in the Earth’s crust. It accounts for more than 27% percent of the crust’s mass, only following oxygen at 45.5% [1].
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Zinc is a chemical element with the symbol Zn and atomic number 30. In the periodic table, Zn belongs in group IIb, along with toxic heavy metals such as Cadmium and Mercury. Yet, zinc is relatively non-toxic for humans and living creatures in general [1].
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Cimetidine was discovered in 1971 and came into commercial use in 1977. It belongs in the imidazole-group of molecules, and more specifically to the category of histamine H2-receptor antagonists, which, until the beginning of the twenty-first century, constituted the highest selling pharmaceutical category worldwide. The development of longer-actin...
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Food supplement, according to the Dietary Supplement Health and Education Act (DSHEA) of 1994 (Public Law 103–417) [1], is a product that is not a pharmaceutical drug, a food additive (spice or preservative), or “conventional food,” and which meets the following criteria:Multivitamins are the most popular food supplements worldwide [2] and represen...
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Rosemarinus officinalis, commonly known as rosemary, is one of the most popular perennial culinary herbs cultivated worldwide. The name comes from Latin “ros marinus”, literally meaning “dew of the sea” since originally the plant was native along the eastern Mediterranean coastline. It is a woody, perennial herb with evergreen, fragrant, needle-lik...
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Latanoprost (Xalatan®, Pharmacia Upjohn Co.) is a prostaglandin-F2α (PGF2α) analog discovered in the early 1990s. It was explicitly developed as an ocular hypotensive agent for the treatment of open-angle glaucoma. The FDA initially approved it as a second-line drug with that indication in 1996. However, in 2003, after reviewing the 5-year safety d...
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Cysteine is a sulfur-containing, α-amino acid with the chemical formula O2CCH(NH2)CH2SH. Cysteine is unique amongst the 20 natural amino acids as it contains a thiol group. It is classified as a conditionally non-essential amino acid since the human body can naturally synthesize it [1, 2]. Like other amino acids, cysteine has an amphoteric characte...
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In 1849, Thomas Addison discovered the link between chronic insufficiency of the adrenals and certain—unclear at the time—systemic features. This condition was later named Addison’s disease, but the mechanism of this deadly condition remained elusive. By 1894, other researchers concluded that the adrenal cortex produced a hormone, which they named...
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Biotin is a water-soluble vitamin, also called Vit B7, and formerly known as Vit H or Coenzyme R, with the different names attesting to the confusion surrounding its role in normal metabolism. Biotin was initially discovered in 1927 in raw egg white, where it is bound to the protein avidin [1]. Even though it has been identified as a necessary nutr...
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Allium cepa is one of the oldest domesticated and cultivated vegetables in human history. It has been grown and selectively bred in cultivation for at least 7000 years, but the onion’s geographic origin is uncertain because the wild onion is nowadays extinct [1]. According to archaeologists, botanists, and food historians, the first cultivated, far...
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Pantothenic acid or Vit B5 is a water-soluble vitamin and an essential nutrient. Vit B5 was discovered in 1933 by Williams et al. during their studies on microbial growth factors [1]. Pantothenic acid is the amide between pantoic acid and β-alanine, with the latter playing a vital role in the crystallization and subsequent artificial production of...
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Vit B3, also known as niacin or nicotinic acid, is a water-soluble member of the Vit B3 complex, a family of vitamins that includes nicotinamide and nicotinamide riboside. Niacin was first described by chemist Hugo Weidel in his studies of nicotine [1]. It was later extracted from liver tissue by biochemist Conrad Elvehjem in 1937, who later identi...
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Bimatoprost (Lumigan®, Allergan Inc., Irvine, CA) is a synthetic analog of prostamide and prostaglandin. It was initially developed to reduce intraocular pressure (IOP) in glaucoma by increasing the outflow of aqueous humor through both the trabecular meshwork and the uveoscleral route [1–4]. Bimatoprost is stereo-chemically similar to other prosta...
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The following pharmaceuticals/cosmetics have also been reported to possess hair-growth properties in a few studies. Therefore their results are reported in summary.
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Sophora flavescens is a deciduous, slow-growing shrub, growing to 1.5 m high by 1 m wide, with deltoid-sword-like leaves, 3–5 cm long and 1–2 cm wide. It belongs to the genus of the Fabaceae family, in which more than 15 members have a long history of use in traditional Chinese medicine. It is endemic in Asia, Oceanica, and the Pacific islands, pre...
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Tripeptide Glycyl-L-histidyl-L-lysine (GHK) is a naturally occurring tripeptide that was initially isolated in the human serum [1] at a concentration of 200 ng/mL and was later isolated in the saliva and urine [2]. GHK is a matrix-derived tripeptide which may originate from several extracellular matrix macromolecules. It spontaneously forms a high-...
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Marine extract compounds are products that have appeared in the scientific literature since the early 1990s. Even though their ingredients are not fully disclosed and are allegedly based on patented, “secret” formulas, they share too many similarities. Some of these similarities are the similar design of the published studies, the unknown -but spec...
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Estrogens are hormones with wide-ranging and significant biological effects on many tissues. Major target organs are the reproductive tract, genitals, bone, blood vessels, and skin. In humans, estrogens influence all skin elements in various ways, but mostly the dermal papilla (DP) and the connective tissue are affected. Estrogens increase overall...
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Magnesium (Mg+2) is the most common intracellular divalent cation and the second most abundant cation in intracellular fluid, essential to every human body cell. The adult human body contains approximately 24 g (1 mol) of Mg+2; about 60% is found in bone tissue, and the rest 40% in all other soft tissues [1].
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Copper is a transition metal with the symbol Cu and atomic number 29. It is an essential trace element in all known organisms and is found in all human body tissues, with the highest concentrations measured in the liver and brain [1]. Cu is mostly present in biological systems as cupric form (Cu++), although several distinct types of the bound cati...
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Alternative medicine is a misnomer because it suggests that there are two kinds of medicine, alternative to each other. However, the author trusts there is no such thing as conventional/orthodox, alternative or complementary, integrative, or holistic medicine. There is one medicine, the one we have discovered through centuries of trial and error of...
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Products classified as cosmeceuticals [1] are skincare products that lie in a gray area between cosmetics and drugs. Most ingredients have been added to these products based on the theoretical benefits discovered from in vitro studies [2]. Most of these ingredients are of botanical origin, and their use is not supported by evidence-based science [3...
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Spironolactone is the prototypic mineralocorticoid receptor antagonist (MRA), is structurally a synthetic derivative of progesterone, patented over 50 years ago and still in widespread clinical use [1]. It is a potassium-sparing diuretic, developed in 1960, and is mostly used to manage hypervolemia, congestive heart failure, and arterial hypertensi...
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Oral contraceptives (OCs) were first approved for use in the U.S. in 1960 [1]. The OC pill is colloquially referred to as “the pill,” and it is the second most popular form of contraception in the Western world. It is used by more than 100 million women worldwide, and according to the U.S. Center for Disease Control (CDC), 12.6% of the 72.2 million...
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Flutamide (Eulexin™, Schering-Plough Int.) was initially synthesized as a bacteriostatic agent, and it was later was found to possess potent antiandrogenic properties [1]. Flutamide is a weak nonsteroidal, antiandrogen (NSAA) with a nitroaromatic chemical structure. When orally administered, it undergoes extensive first-pass metabolism into an acti...
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In the 1970s, the American pharmaceutical company Upjohn & Pharmacia developed the antihypertensive drug Minoxidil and launched it under the brand name Loniten®, in the form of 2.5 mg and 10 mg tablets. Minoxidil is a pyrimidine derivative (2,4 diamino-6-piperidinopyrimidine-3-oxide), has a molecular weight of 209.25, and its action is focused on v...
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The following herbs have also been reported to possess hair-growth properties, and their results are reported in summary and in alphabetical order. The reason these herbs do not “entertain” a dedicated chapter is because there is no available data on use in humans for most of these herbs. Also, their safety, adequate concentration, required dosage...
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Calcium (Ca+2) is the most abundant major mineral in the human body and accounts for 1–2% of adult human body weight [1]. No less than 99% of Ca+2 is found in bones and teeth where it supports their structure and function, while 1% is found in plasma and soft tissues. Despite the large amount of Ca+2 in the human body, intra- and extracellular Ca+2...
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Finasteride is the result of a long-term research program by Merck & Co., dating back to 1950 when their R&D department got engaged in the study of androgen effects in Benign Prostatic Hyperplasia (BPH). BPH is defined as an increase in the prostate’s size caused by the growth of the prostatic periurethral transition zone, is due to androgen action...
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Cyproterone acetate (CPA) is a very potent synthetic analog of progesterone, classified as a progestin. It was discovered in 1962 by the German company Schering. CPA was developed from 17α-hydroxyprogesterone, and it is estimated to be approximately 1200 times more potent as an antiandrogen than 17α-acetoxyprogesterone [1]. CPA is marketed under th...
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Vit E is a collective term referring a group of 8 naturally occurring lipid-soluble molecules (homologs), of which 4 are tocopherols (α, β, γ, and δ tocopherols) and 4 are tocotrienols (α, β, γ and δ tocotrienols) [1]. Vit E was discovered in 1922 by Evans and Bishop, of the University of California in Berkeley, and the name “tocopherol” they propo...
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Tea is the most popular beverage globally, with areas of Asia reporting the highest consumption per capita. In 2013, the global production of green tea was approx. 1.7 million tons, with a forecast to double in volume by 2023 [1]. Green tea, just like all types of tea, is made from the processed leaves of evergreen shrub Camellia sinensis. The leav...
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Vit A is a fat-soluble vitamin with a wide range of actions since it regulates a variety of essential functions throughout the human body. The story of Vit A goes back to the Ancient Egyptians, who recognized that liver consumption, known today to be a source of high levels of Vit A, could cure night blindness. The scientific characterization of Vi...
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Vit B6 is a water-soluble vitamin, but the name refers to a group of at least ten chemically similar pyridine derivatives (vitamers), which can be interconverted in biological systems.
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Ginseng is a deciduous perennial plant belonging to the genus Panax of the family Araliaceae. Thirteen plants are affiliated with the genus Panax, and just five of them are used therapeutically, namely Korean ginseng (Panax ginseng C.A. Meyer, named by the Russian scientist Carl Anton Meyer in 1843), South China ginseng, American ginseng, Japanese...
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Dutasteride is a synthetic 4-azasteroid, developed by GlaxoSmithKline, and it is an orally-administered, second generation inhibitor of the 5α-R enzymatic complex that leads to near-maximal Dihydrotestosterone (DHT) suppression. The compound appeared in the medical literature initially under the name GG-745, later as GI198745, and was finally named...
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Ketoconazole is an antifungal agent, which belongs to the group of azoles (imidazole) [1], was discovered in 1976 by Janssen Pharmaceutica, and was first introduced in 1977. Ketoconazole has a prominent place in Clinical Dermatology, as the first orally-active antifungal azole, used both orally and topically to combat numerous types of moderate or...
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Iodine is a chemical element with symbol I, atomic number 53. It is an essential element for life and is the heaviest trace element commonly needed by living organisms. It is required for the synthesis of the growth-regulating thyroid hormones triiodothyronine and thyroxine, named T3 and T4, respectively, after their number of iodine atoms [1].
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Polysorbates are oily liquids deriving from Polyethylene glycol and sorbitan (a sorbitol derivative), esterified with fatty acids. Sorbitan esters, also known as Spans [1] or Polysorbates, contain less than 20 moles of ethylene oxide per mole of ester, according to the Food Chemicals Codex (FCC) [2]. Polysorbates are emulsifiers used in the food an...
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In 1970, several new strains of fungi were isolated from soil samples taken from Norway and from Wisconsin in the USA by employees of the pharmaceutical company Sandoz Inc. (today Novartis). Both strains produced a family of natural products called Cyclosporins. Cyclosporin A (CyA) was first isolated in 1972, and it is a highly lipophilic, cyclic u...
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Iron is a chemical element with the symbol Fe and atomic number 26. It is the most common element on Earth by mass, forming most of Earth’s outer and inner core. Iron is an essential trace element and the most important transition metal found in all living organisms (archaeans, bacteria, and eukaryotes), including humans [1]. Iron is the primary in...
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Inositol exists in nature in nine stereoisomers, with cis-1,2,3,5trans-4,6-cyclohexanehexol or myo-inositol being the most widely occurring form. Inositol is a sugar alcohol, closely related to glucose and is not considered a real vitamin, in the strict sense of the word, since it can be synthesized in the human body using glucose-6-phosphate as su...
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Sulfur is a chemical element with the symbol S and atomic number 16. It is a multivalent, nonmetallic element found in large amounts in the human body. It is the third most abundant mineral based on the percentage of total body weight, representing 0.25% of the average body weight, slightly higher than sodium [1]. Sulfur-containing compounds are fo...
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A full head of hair is an essential part of the general body image ideal, it has always been regarded as a symbol of virility and strength and is closely related to physical attractiveness. In contrast, baldness has always been associated with unfavorable meanings and negative feelings.
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The sebaceous gland almost always accompanies a hair follicle, vellus or terminal, and the resulting complex is called pilosebaceous unit; independent sebaceous glands freely secreting on the skin surface are rare.
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In the human body, hair follicles, and hence, the hair shafts that grow from them vary, depending on location, age, and sex. Moreover, each hair follicle may produce different hair types throughout its lifetime [1]: lanugo hair is produced during intrauterine life, vellus hair in childhood and pre-puberty, and terminal hair in adulthood are all pro...
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Over the past six decades, there is increasing evidence on the epidemiological association and dose-response relationship between AGA and cardiovascular disease (CVD), metabolic syndrome (MetS), hypertension, and insulin resistance (IR).
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The physiologic function of hair follicles, hair growth, circularity, and hair loss do not depend solely on the actions of androgens but are coordinated by additional hormonal parameters through complex physiological mechanisms.
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Evidence suggests that AGA and prostate disease, namely Prostate Cancer (PCa) and Benign Prostatic Hyperplasia (BPH), share similar pathophysiological mechanisms concerning heritability and endogenous hormones.
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Solar radiation can readily influence the physiology of the scalp skin, the hair follicle, and the physical properties of the hair shaft.
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The skin is a target-organ for systemic and local reactions to stress, and hair loss may indeed occur after acutely stressful conditions, such as trauma and severe disease.
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Hair loss in children and adolescents is more common than previously estimated, and counterintuitively, AGA may begin in adolescence or even in childhood. However, little is known about its prevalence, characteristics, and natural history in the pediatric and adolescent population.
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Androgenetic Alopecia (AGA) is by far the most common cause of hair loss in men, and its high prevalence has been reported in detail for many decades [1]. Several different terms in international medical bibliography have been suggested by several authors, such as androgenic alopecia, male pattern baldness, androgen-dependent alopecia, common baldn...
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Ηardy described the hair follicle as “a treasure waiting to be discovered by even more molecular biologists” [1]. And there is nothing more intriguing about hair follicle physiology than its life cycle.
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The pilosebaceous unit is a complex mini-organ consisting of three anatomic components: hair follicle, sebaceous gland, and arrector pili muscle. The proportions of these components vary among the different types of hair follicles. In this chapter, some interesting anatomical details of this impressively complex organ will be presented.
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Under physiological conditions, the scalp is perfused ten times more extensively than other areas of the human skin; in contrast, AGA-affected scalp areas have 260% lower blood flow compared to other scalp areas.
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Female Pattern Hair Loss (FPHL) is by far the most common cause of hair loss affecting otherwise healthy women. For decades it has been considered the female “counterpart” of male AGA despite weaker androgenic parameters than AGA since most women with FPHL do not have an underlying hormonal abnormality; recent research shows that AGA and FPHL are e...
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Humans have always attributed great importance to their appearance, driven by the innate desire to demonstrate their beauty and fitness. Hair is a crucial aspect of one’s appearance and has always carried great symbolic importance. Thus, grooming, styling, adorning, or even removing unwanted hair were standard practices in all civilizations and cul...
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Diagnosis of AGA and FPHL is mostly a matter of knowledge, common sense and practice, Only rarely, will further examination be required to exclude other disorders affecting scalp and/or hair, depending on the patient’s medical history and clinical assessment.
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As humans grow older, signs of aging become evident in all the organs of the human body. The first visible signs of aging appear on the skin. The aging skin changes due to a combination of endogenous factors (gene mutations, cellular metabolism, hormonal environment) and exogenous ones (chemicals, toxins, pollutants, UV radiation, smoking, diet, li...
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Hair follicles are complex, minuscule, dynamic organs found only in mammals, representing one of their most defining features. Despite their tiny size, they possess impressive physiological properties, often overlooked by those who can be misled by their small size. Some properties of the hair follicle in mammals are unique and extremely diverse: s...
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The hair follicle enjoys the benefits of the “Immune Privilege”, which allows the produced hair not to be recognized as an antigen during anagen stage. The flip side of this privilege is that the hair follicle is insufficiently protected from exogenous, harmful stimuli.
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Over the last few decades, recent advances in molecular biology and genetics, as well as the development of new experimental techniques, have brought together scientists from all fields of biological science [1]. Developmental biologists, geneticists, endocrinologists, and dermatologists now study the many diverse facets of hair follicle biology, i...
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Even though hair exhibits no biochemical activity and is considered metabolically “dead”, it is produced by an impressively dynamic organ: the hair follicle. In fact, hair can be described as the holocrine secretion of the follicular bulb. Each strand of hair on the body is truly unique in terms of length, size, caliber, color, etc., but also in te...
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Hair disorders include hair loss, increased hair growth, hair structure defects with increased breakage, as well as undesirable cosmetic appearance resulting from reduced shine, strength, curliness, or elasticity. The diagnosis of diseases of the hair follicle is one of the oldest medical practices and the reliable the diagnosis of hair disorders i...
Book
This reference volume conveys complete understanding and management of Androgenetic Alopecia and Female Pattern Hair Loss (AGA/FPHL). These are probably the most common adult (18-50 yrs.) health disorders besides dental caries, accounting for over 98% of hair loss cases in males and over 70% cases in females. The present volume, the first of three...

Citations

... Small (saw palmetto) and Sabal etonia Swingle ex Nash (scrub palmetto) are nearly omnipresent components of upland vegetation throughout much of the Florida peninsula. Serenoa repens is widespread on the coastal plain from South Carolina to Louisiana (Small 1926, Corner 1966, Hilmon 1969, Moore and Uhl 1982, Henderson et al. 1995 while Sabal etonia is a Florida endemic that occurs only on the white or yellow sands of upland areas of peninsular Florida's central and Atlantic coast ridges (Zona andJudd 1986, Zona 1990). Serenoa repens and Sabal etonia co-occur on the Florida peninsula's central and Atlantic-coast ridges, and they have many traits in common including growth form, reproductive strategy, persistence following fire, reproductive response to fire, and habitat preference (Abrahamson 1995(Abrahamson , 1999(Abrahamson , 2007Abrahamson 2002, 2006). ...
... In our everyday lives, human hair is important. Hair is an epidermal derivative created when ectoderm-derived germinative cells undergo keratinization [8,10]. Only the fingers, soles, and palms of the human body lack hair. ...
... Cytoplasmic 5α-reductase enzymes convert testosterone to the potent DHT, which is more potent and has higher affinity towards AR than testosterone [7,42]. The androgen/AR complex binds the androgen response element and recruits transcriptional co-regulators of the target genes [43]. Subsequently, the deregulation of HFDPCsecreted factors, including TGF-β, insulin-like growth factor 1 (IGF-1), WNT family member, and (DKK-1), results in the attenuating proliferation and differentiation of hair follicle stem cells (HFSC) [7]. ...
... Furthermore, it has been established that AGA-scalp skin is extremely sensitive to androgen, with androgen production and androgen receptor response significantly increasing in these areas, particularly in hair follicle dermal papilla cells (HFDPC) [6]. Enzyme 5α-reductases convert testosterone into the most potent androgen, dihydrotestosterone (DHT) [15]. Androgen receptor (AR) affinity of DHT is roughly five times higher than that of testosterone [16]. ...