▎ Nnyocha nyocha nke Dermorphin
Kedu ihe ndabere nyocha nke Dermorphin?
Nnyocha nke ihe ndị dị ndụ: Kemgbe 1970s, ndị ọkà mmụta sayensị raara onwe ha nye ịchọta ihe nwere mmemme physiological pụrụ iche sitere na ihe ndị dị ndụ. Ndị mmadụ ejirila nwayọọ nwayọọ ghọta na n'ime ogologo usoro evolushọn, ụmụ anụmanụ ga-emepụta biomolecules dị iche iche pụrụ iche iji mee mgbanwe na gburugburu ebe obibi ma nọgide na-arụ ọrụ ndụ, na ụmụ irighiri ihe ndị a nwere ike inwe ụkpụrụ ọgwụ dị mkpa.
Ihe dị mkpa nke akpụkpọ anụ Amphibian: Akpụkpọ anụ nke amphibians nwere ọtụtụ ọrụ, dị ka iku ume, nchebe, na nzuzo. Akpụkpọ anụ nke amphibians nwere ike zoo ọnụ ọgụgụ dị ukwuu nke ihe ndị na-emepụta ihe, nke na-arụ ọrụ dị mkpa n'ịgbachitere ndị iro eke na ime mgbanwe na gburugburu ebe obibi. Ihe nzuzo nzuzo nke ọtụtụ amphibians nwere peptide bara ụba, nke nwere ụdị dị iche iche na ihe omume dị iche iche nke ndụ, na-adọta uche nke ọtụtụ ndị ọkà mmụta sayensị.
Nchọpụta nke Dermorphin: Na 1981, ndị ọkà mmụta sayensị Ịtali buru ụzọ kewapụ Dermorphin site na nzuzo nzuzo nke frog osisi South America (Phyllomedusa sauvagii). Site na nyocha nke akụkụ nke nzuzo nzuzo nke osisi frog na nchọpụta nke ihe omume ndụ, a chọpụtara na Dermorphin n'ime ya nwere mmetụta analgesic dị ike na mmekọrịta dị elu maka ndị na-anabata opioid. Nchọpụta a meghere ụzọ nyocha ọhụrụ na ngalaba ọgwụgwọ mgbu.
Kedu ihe bụ usoro ọrụ Dermorphin?
1. Jide n'aka ndị na-anabata Opioid
Dermorphin bụ peptide dị ka opioid siri ike nke nwere ike ijikọta ya na ndị na-anabata μ-opioid. Njikọ a na-eme ka ndị na-anabata ya rụọ ọrụ, na-ebute usoro mmetụta physiological [1, 2] . Dịka ọmụmaatụ, na nnwale anụmanụ, o gosipụtara mmetụta analgesic dị ike [1, 2] . Enwere ike nweta mmetụta analgesic ya site na igbochi nnyefe nke mgbaàmà mgbu. Mgbe a na-ebufe ihe mgbaàmà mgbu na neurons, ọ ga-eme ka mkpali na ọkụ nke neurons. Mgbe Dermorphin jikọtara ya na onye na-anabata μ-opioid, ọ nwere ike igbochi mkpali nke neurons, si otú ahụ belata nnyefe nke mgbaàmà mgbu.
2. Mmetụta na sistemụ akwara
Mmetụta na Ọkwa Ọkpụkpụ Ọkpụkpụ
N'ime ọmụmụ ihe mmadụ, achọpụtara na infusion intravenous nke dermorphin nwere ike ime ka mmụba dị ịrịba ama na nke na-adịgide adịgide na ọnụ ọgụgụ nociceptive flexor reflex n'ime ndị ọrụ afọ ofufo dị mma [2] . Nke a na-egosi na dermorphin nwere ike igbochi nnyefe nke mgbaàmà nociceptive na ọkwa ọkpụkpụ azụ. Mmetụta a pụtakwara ìhè na isiokwu ndị nwere mmerụ ahụ zuru oke na-adịghị ala ala, na-ekwenyekwu na dermorphin na-arụ ọrụ na-egbochi nnyefe nociceptive na ọkwa ọkpụkpụ azụ.
Naloxone nwere ike ịtụgharị n'ụzọ ụfọdụ (ihe dị ka 50%) mmetụta mgbochi nke dermorphin na reflex spinal nociceptive. Nke a nwere ike ịpụta na dermorphin na-emekọrịta ihe na ọnụ ọgụgụ dị iche iche nke ndị na-anabata opioid spinal iji mepụta mmetụta analgesic [2].
Mmetụta na Central Nevous System
Nlekọta intracerebroventricular nke DM na-emepụta ọrụ antinociceptive na-adịte aka [1] . Nke a na-egosi na dermorphin nwere ike ịkpata mmetụta analgesic site n'ime ihe na Central ụjọ usoro. Otú ọ dị, a ka aghọtabeghị kpọmkwem usoro dermorphin na-eme n'ime usoro nhụjuanya nke etiti.
N'ime nnwale oke bekee, mgbe ịgbanye dermorphin intravenous, omume nke oke bekee gosipụtara mmụba dị ukwuu n'oge ịnọ jụụ na nke na-adịghị emegharị ahụ, yana mbelata ọrụ afọ ofufo, mana ọ nweghị mmetụta na ụkpụrụ na ugboro ole nke electroencephalogram hippocampal [3] . Nke a na-egosi na dermorphin nwere ike inwe mmetụta na ụfọdụ omume na akụkụ nke usoro ụjọ ahụ.
3. Mmetụta na tract intestinal
Dermorphin nwere mmetụta na mkpali eriri afọ na oke. E jiri ya tụnyere morphine, intracerebroventricular injection of dermorphin na-egbochi mkpali eriri afọ dị ka morphine, na ọrụ ya bụ ugboro 143 karịa nke morphine [4] . Mmetụta mmegide nke naloxone na dermorphin adịghị arụ ọrụ karịa nke ahụ na morphine. Intracerebroventricular nchịkwa nke naloxone quaternized nwere ike imegide mmetụta nke intracerebroventricular dermorphin na eriri afọ, ebe injection intraperitoneal na-arụ ọrụ naanị na dose 8mg/kg. Dermorphin nke a na-enye intraperitoneal adịghị arụ ọrụ kpamkpam na oke kachasị dị irè (0.56 micrograms kwa oke). Ịba ụba dose nke intraperitoneal injections nke dermorphin (site na 12 ruo 6400 micrograms kwa kilogram) nwere mmetụta mgbochi na mkpali eriri afọ nke na-anọghị na dose ahụ, ma ọ dịghị mgbe ọ gafere 50%. Naanị oke dose nke naloxone (30mg/kg, intraperitoneal injection) nwere ike imegide mmetụta nke ntụtụ intraperitoneal a. Nke a na-egosi na mmetụta dermorphin na eriri afọ nwere ike ịgụnye ma akụkụ etiti na akụkụ.
4. Mmetụta na Muscles
A mụrụ ihe omume Dermorphin na akụkụ obe nke akwara afọ frog site n'aka onye na-edekọ ihe [5] . Nsonaazụ nyocha na-egosi na dermorphin (10 (-5) -10 (-8) M) nwere ike igbochi ọrụ acetylcholine, ọrụ akpaghị aka, na mkpụkọ akwara kpatara site na mkpali ọkụ eletrik kpọmkwem. Mmetụta ndị a niile siri ike ịtụgharị. Ọ bụrụ na a na-agbanye dermorphin n'ime usoro ntinye n'oge K (+) depolarization (KCl - 100mM) nke uru ahụ, ọ nweghị ike igbochi ihe omume na-akpaghị aka. Ya mere, dermorphin nwere mmetụta na-adabere na voltaji ma nwee ike ime ihe na-adabere na voltaji Ca (2+) ọwa nke akpụkpọ ahụ cell muscle.
5. Mmekọrịta dị n'etiti Ọdịdị Molecular na Mechanism of Action
Emeela ihe nlegharị anya igwe na-ahụ anya na dermorphin (Pattabiraman N, 1986). Nnyocha ahụ na-egosi na D-Ala2 na N-terminus na L-Pro6 fọdụrụnụ na C-terminus na usoro dermorphin na-egosi na enwere ike ịdị adị nke β-turn. Site n'echiche stereochemical, enwere ike inwe ụdị atọ (II', III', na V') nke β-atụgharị na N-terminus nke peptide, na ụdị abụọ (I na III) nke β-atụgharị na C-terminus. N'ime usoro mgbako molikula, a tụlere conformations apịaji isii na otu conformation gbatịpụrụ iji nyochaa nkwụsi ike nke dermorphin. N'ime ha, nhazi atọ apịaji nwere ike dị ala ma nwee njirimara izugbe ndị a: ume yiri ya, njikọ hydrogen atọ, mpempe akwụkwọ β-ibe siri ike, na mmekọrịta Tyr1-Tyr5 dị mma. Ịdị adị nke nhazi akwụkwọ β nwere ike ịrụ ọrụ na mmekọrịta nhọrọ n'etiti dermorphin na μ-receptor.
Kedu ihe bụ ngwa Dermorphin?
Ejiri ya mee ihe maka nchịkwa mgbu na-aga n'ihu: Nnyocha a na-achịkwaghị achịkwa, nke a na-achịkwa ebebo na 1985 gosiri na Dermorphin nke a na-enye site na ụzọ intrathecal dị irè karịa placebo na morphine ntinye aka na nchịkwa mgbu na-esote [6, 7] . Nke a na-egosi na Dermorphin nwere ike inwe ikike dị ukwuu n'ibelata mgbu mgbe ịwachara ahụ. Maka ndị ọrịa na-aga n'ihu, nlekọta mgbu dị irè nwere ike ọ bụghị naanị imeziwanye nkasi obi nke ndị ọrịa kamakwa nyere ndị ọrịa aka ịgbake ma laghachi na ndụ nkịtị.
Ngwa na Nlekọta Palliative: N'ịtụle mmetụta analgesic ya magburu onwe ya, a na-atụkwa aro Dermorphin maka iji na-elekọta ndị ọrịa dị elu [6,7] . Na nlekọta palliative, iwepụ ihe mgbu nke ndị ọrịa bụ ihe mgbaru ọsọ dị oke mkpa, na Dermorphin, nke nwere mmetụta analgesic ya dị ike na obere ihe ize ndụ nke mmetụta dị n'akụkụ, na-enye nhọrọ nwere ike ime ka mgbu nke ndị ọrịa dị elu kwụsịlata.
Mmetụta Mgbochi na Ọrịa Spinal: Nnyocha egosiwo na Dermorphin nwere ike igbochi nnyefe nke nociception na ọkpụkpụ azụ. N'ime ndị ọrụ afọ ofufo dị mma, infusion intravenous nke 0.16mg / kg nke Dermorphin nwere ike ịba ụba nke ukwuu ma nọgide na-abawanye ọnụ ụzọ nke nociceptive flexor reflex [8] . A na-ahụkwa mmetụta ndị yiri ya na ndị nwere mmerụ ahụ na-adịghị ala ala, na-egosi na Dermorphin na-emekarị na ọkpụkpụ azụ azụ iji gbochie nnyefe nke mgbu. Ihe mgbochi a na-egbochi mgbu azụ na-enye olileanya ọhụrụ maka ọgwụgwọ nke ndị ọrịa na-arịa ọrịa mgbu metụtara ọkpụkpụ azụ.
N'ikpeazụ, Dermorphin bụ peptide dị ike nke opioid nwere ike jikọta na ndị na-anabata μ-opioid, na-egosi mmetụta analgesic dị ịrịba ama na igbochi nnyefe nke ihe mgbaàmà nociceptive na ọkpụkpụ azụ. Ọ nwere ike ngwa na njikwa mgbu na-esote, nlekọta palliative, wdg, na-eweta echiche ọhụrụ maka ọgwụgwọ mgbu.
Banyere Onye dere ya
Ihe niile a kpọtụrụ aha n'elu bụ Cocer Peptides na-enyocha, dezie ma chịkọta ya.
Onye ode akwụkwọ akụkọ sayensị
Giuliano Fontani bụ onye nyocha jikọtara ya na Mahadum Siena, Italy, na-elekwasị anya na neurosciences na physiology. Ọ mụọla mmetụta nke dermorphin, peptide na-emekarị, na omume na ọrụ eletriki hippocampal na rabbits, na-enye aka na nghọta nke ọrụ nnata opioid. Ọrụ ya na-enyochakwa mmekọrịta dị n'etiti ọrụ ụbụrụ na omume, na mbipụta na akwụkwọ akụkọ dị ka Life Sciences. Edepụtara Giuliano Fontani n'akwụkwọ ntụaka [3].
